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| ID | PMID | YEAR | Sequence | Name | Length | N-ter MOD | C-ter MOD | Linear/Cyclic | Chirality | Chem-MOD | Origin | Nature | Incubation Time | Concentration | Half Life | Units Half Life | Protease | Assay | Test Sample | Vivo/Vitro | Reference | Patent No. | Activity |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 20844765 | 2010 | Lfc1 | 6 | Free | Free | Linear | L | None | Bovine lactoferricin | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=60μM for E.coli | |||
| 20844765 | 2010 | Lfc1 | 6 | Free | Free | Linear | L | None | Bovine lactoferricin | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=30μM for S. aureus | |||
| 20844765 | 2010 | Lfc1 | 6 | Free | Free | Linear | L | None | Bovine lactoferricin | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=7.5 μM for B. subtilis | |||
| 20844765 | 2010 | Com1 | 6 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=60μM for E.coli | |||
| 20844765 | 2010 | Com1 | 6 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=7.5μM for S. aureus | |||
| 20844765 | 2010 | Com1 | 6 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=1.9 μM for B. subtilis | |||
| 20844765 | 2010 | Lfc2 | 6 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=15μM for E.coli | |||
| 20844765 | 2010 | Lfc2 | 6 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=15μM for S. aureus | |||
| 20844765 | 2010 | Lfc2 | 6 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=1.9μM for B. subtilis | |||
| 20844765 | 2010 | Com2 | 6 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=30μM for E.coli | |||
| 20844765 | 2010 | Com2 | 6 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=30μM for S. aureus | |||
| 20844765 | 2010 | Com2 | 6 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | <30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=0.9 μM for B. subtilis | |||
| 20844765 | 2010 | Lfc3 | 6 | Acetylation | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | ~60 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=120μM for E.coli | |||
| 20844765 | 2010 | Lfc3 | 6 | Acetylation | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | ~60 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99>120μM for S. aureus | |||
| 20844765 | 2010 | Lfc3 | 6 | Acetylation | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | ~60 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=60 μM for B. subtilis | |||
| 20844765 | 2010 | Com3 | 6 | Acetylation | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | ~60 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=120μM for E.coli | |||
| 20844765 | 2010 | Com3 | 6 | Acetylation | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | ~60 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=30μM for S. aureus | |||
| 20844765 | 2010 | Com3 | 6 | Acetylation | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | ~60 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=7.5μM for B. subtilis | |||
| 20844765 | 2010 | Lfc7 | 11 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | >30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=15μM for E.coli | |||
| 20844765 | 2010 | Lfc7 | 11 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | >30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=7.5μM for S. aureus | |||
| 20844765 | 2010 | Lfc7 | 11 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | >30 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=0.9μM for B. subtilis | |||
| 12270169 | 2002 | Peptide 1a | 18 | Acetylation | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 5mg/kg | 7.6 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=1.1nM for fVIIa binding assay | |||
| 12270169 | 2002 | Peptide 1b | 18 | Acetylation [(C6H6)2-CO-] | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 5mg/kg | 15 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=4nM for fVIIa binding assay | |||
| 12270169 | 2002 | Peptide 1c | 18 | Acetylation [(CH3)2-CH-CH2-(C6H6)-CH(CH3)-CO] | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 4.9mg/kg | 24 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=14.6nM for fVIIa binding assay | |||
| 12270169 | 2002 | Peptide 1c | 18 | Acetylation [(CH3)2-CH-CH2-(C6H6)-CH(CH3)-CO] | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 2mg/kg | 17 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=14.6nM for fVIIa binding assay | |||
| 12270169 | 2002 | Peptide 1m | 18 | Acetylation (Napthalene acyl sulfonamide) | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 2mg/kg | 30 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=1.0nM for fVIIa binding assay | |||
| 12699744 | 2003 | Peptide 1a | 18 | Acetylation | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 1.11mg/kg | 4.18 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=9.7nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin | |||
| 12699744 | 2003 | Peptide 1b | 18 | Acetylation(Naphthalene acylsulfonamide) | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 2mg/kg | 30 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=24nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin | |||
| 12699744 | 2003 | Peptide 5b | 18 | Acetylation (Naphthalene) | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 2mg/kg | 34.8 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=9.2nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin | |||
| 15322125 | 2004 | Aβ(1 €“ 40) | 40 | Free | Free | Linear | L | None | Derivative of human A precursor protein APP770 | Neurodegenerative | 120 minutes | 2x107 cpm of 125I-Aβ42 peptide | 2.4 | Mouse plasma proteases | Radioactivity measured by scintillation counter | Intravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samples | in vivo | None | None | Neurodegeneration caused by oligomerization | |||
| 15322125 | 2004 | Aβ(1 €“ 42) | 42 | Free | Free | Linear | L | None | Derivative of human Aprecursor protein APP771 | Neurodegenerative | 121 minutes | 2x107 cpm of 125I-Aβ40 peptide | 2.8 | Mouse plasma proteases | Radioactivity measured by scintillation counter | Intravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samples | in vivo | None | None | Neurodegeneration caused by oligomerization | |||
| 15012592 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 25 nM/kg body weight | < 2 | Adult obese diabetic (ob /ob ) mice blood protease | LC/MS equipped with a microbore C-18 HPLC | Intraperitoneally administered to adult obese diabetic (ob /ob ) mice | in vivo | None | None | IC50 = 0 ·37 nM of binding to a receptor | |||
| 2147696 | 1990 | Control peptide | 8 | Free | Free | Linear | L | None | Synthetic peptide (scrambled amino acids of human protein S) | Anticoagulant | Not reported | Not mentioned | 15 | Rabbit blood proteases | Spectrofluorometry | Intravenously injected in male New Zealand white rabbits and blood samples withdrawn and plasma sample prepared | in vivo | None | None | No activity found | |||
| 2147696 | 1990 | Control peptide | 10 | Free | Free | Linear | L | None | Synthetic peptide (amino acids 400-407 of human protein S) | Anticoagulant | Not reported | Not mentioned | 15 | Rabbit blood proteases | Spectrofluorometry | Intravenously injected in Male New Zealand white rabbits and blood samples withdrawn and plasma sample prepared | in vivo | None | None | No activity found | |||
| 11553691 | 2001 | APP-C59 | 59 | Free | Free | Linear | L | None | Amyloid precursor protein derivative | Regulator of synapse formation | 2 hours | Not mentioned | ~5 | Fetal calf serum proteases | Pulse chase experiment | BHK cell line | in vitro | None | None | Not reported | |||
| 11553691 | 2001 | APP-C59 | 59 | Free | Free | Linear | L | None | Amyloid precursor protein derivative | Regulator of synapse formation | 2 hours | Not mentioned | ~5 | Fetal calf serum proteases | Pulse chase experiment | Primary cultures of neurons from PS1 knockout mice's 14 day embryos | in vitro | None | None | Not reported | |||
| 12039708 | 2002 | Glucagon-like peptide-1 (GLP-1) | 30 | Free | Amidation | Linear | L | None | Derived from proteolytic cleavage of proglucagon | Insulinotropic | Not reported | Not mentioned | 1.5 €“5 | Plasma proteases | Radioimmunoassay | Rat plasma | in vivo | 24199154 | None | GLP-1 normalizes blood glucose levels | |||
| 12859428 | 2003 | BNP-32 | 32 | Free | Free | Linear | L | None | Canine B-type natriuretic peptide | Diuretic, natriuretic, hypotensive and smooth muscle relaxant activities | Not reported | Not mentioned | 1.57 ± 0.14 | Dog plasma proteases | Radioimmunoassay | Injected intravenously into dogs | in vivo | None | None | 44.7 ±0.3% RBC during BNP-32 infusion | |||
| 12578830 | 2003 | iAβ5p-C1 | 5 | Free | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 5 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p | 5 | Free | Free | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 15 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | 100% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C1 | 5 | Free | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | <1 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C2 | 5 | Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 41 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C3 | 5 | (NMe)Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 25 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=4 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=7 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3 µg/ml for M. Luteus ATCC 9343 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6 µg/ml for M. Luteus ATCC 9345 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for S. Aureus ATCC 6538 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=9 µg/ml for S. Aureus ATCC 6538 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=19 µg/ml for S. Aureus ATCC 6539 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for S. Aureus ATCC 6542 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=11 µg/ml for S. Aureus ATCC 6544 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12228 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12229 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3.12 µg/ml for S. Epidemidis ATCC 12228 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12229 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | Not reported | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for MRSA SR 1550 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=50 µg/ml for MRSA SR 1551 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=100 µg/ml for MRSA SR 1552 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=42 µg/ml for MRSA SR 1555 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=16 µg/ml for MRSA SR 1557 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=>100 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. smegmatis ATCC 612 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | Not reported | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=23 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=21 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=11 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=4 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=20 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=5 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL | 10 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 6 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL1 | 10 | Free | Free | Linear | L | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 14 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=9 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL2 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=17 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL5 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 23 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL7 | 10 | Free | Free | Linear | Mix | None | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 22 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for C. albicans ATCC 36232 | |||
| 10773009 | 2000 | TX14(A) | 14 | Free | Free | Linear | Mix | None | Synthetic derivative of prosaposin | Neurotrophic factor | 9 minutes | Not mentioned | 4.2 ±0.3 | Rat serum proteases | Radioactivity measured with a gamma counter | Injected in jugular vein of male Sprague-Dawley rats | in vivo | None | None | ED50=1.00 ±0.11ng/ml | |||
| 10773009 | 2000 | TX15-2 | 15 | Free | Free | Linear | Mix | None | Synthetic derivative of prosaposin | Neurotrophic factor | 9 minutes | Not mentioned | 2.5 ±0.3 | Rat serum proteases | Radioactivity measured by a gamma counter | Injected in jugular vein of male Sprague-Dawley rats | in vivo | None | None | ED50=1.00 ±0.09ng/ml | |||
| 11054637 | 2000 | Human brain natriuretic peptide (hBNP) | 32 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 12.7 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | 2136732 | None | Kd=8pM for receptor binding | |||
| 11054637 | 2000 | Ovine Brain natriuretic peptide (oBNP) | 29 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 2.6 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | None | None | Kd=16pM for receptor binding | |||
| 11054637 | 2000 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | 1826098 | None | Kd=10pM for receptor binding | |||
| 11054637 | 2000 | Human brain natriuretic peptide (hBNP) | 32 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3.1 | Human blood proteases | HPLC | Injected in humans | in vivo | 2136732 | None | Kd=8pM for receptor binding | |||
| 11054637 | 2000 | Ovine Brain natriuretic peptide (oBNP) | 29 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3.1 | Human blood proteases | HPLC | Injected in humans | in vivo | None | None | Kd=16pM for receptor binding | |||
| 11054637 | 2000 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 22 | Human blood proteases | HPLC | Injected in humans | in vivo | 1826098 | None | Kd=10pM for receptor binding | |||
| 10670753 | 1999 | Human thyrotropin-releasing hormone (TRH)-associated peptide 3 (hTAP-3) | 9 | Free | Free | Linear | L | None | Product of proteolysis of preproTRH | Serum hTAP-3 concentration was increased in patients with hyperthyroidism | 15 min | Not mentioned | 3.5 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | None | None | Not reported | |||
| 14980787 | 2004 | Leucyl-tryptophane | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 7.4 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=15 µM | |||
| 14980787 | 2004 | Seryl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 5.2 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=41 µM | |||
| 14980787 | 2004 | Valyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 15 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=11 µM | |||
| 14980787 | 2004 | Leucyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 4.3 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=44 µM | |||
| 14980787 | 2004 | Alanyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 9.4 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=40 µM | |||
| 14980787 | 2004 | Tyrosyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 16 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=9 µM | |||
| 20382695 | 2010 | hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | None | Glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 50 | Rat plasma protease | RP-HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.08nM for stimulating cAMP production | |||
| 20418955 | 2010 | Glucagon | 29 | Free | Free | Linear | L | None | Glucagon | Regulate blood glucose | Not mentioned | Not mentioned | <10 | Not reported | Not mentioned | Not reported | in vivo | None | None | Elevated blood glucose levels for <2 hours | |||
| 21114599 | 2010 | hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | None | Glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 0.9 ±0.1 | Rat plasma proteases | HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.08 ±0.03nM for cAMP stimulation | |||
| 20587645 | 2010 | HM-3 | 16 | Free | Free | Linear | L | None | Derivative of endostatin | Anti-angiogenetic | Not mentioned | Not mentioned | 10 to 27 | SD rat plasma proteases | RP-HPLC | SD rat plasma | in vitro | http://pubs.rsc.org/En/content/articlepdf/2014/tb/ | None | 39.68% inhibitory effect on mouse tumors | |||
| 20593470 | 2010 | Peptide 1 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.9 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 3 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.7 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 4 | 41 | Free | Amidation | Linear | Mix | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.9 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 8 | 41 | Free | Amidation | Linear | L | PhG=phenylglycine | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.5 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 9 | 41 | Free | Amidation | Linear | L | Aib=α-aminoisobutyric acid | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.8 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 17292977 | 2007 | AC3174 | 39 | Free | Amidation | Linear | L | None | Analog of exendin-4 | Regulates blood glucose | Not mentioned | Not mentioned | 42 ±3.4 | Rat plasma proteases | ELISA | Subcutaneously administion of 10 µg/kg dose to Sprague Dawley rats | in vivo | None | None | ED50=1.2 µg/kg for glucose lowering in db/db mice | |||
| 17292977 | 2007 | AC3174 | 39 | Free | Amidation | Linear | L | None | Analog of exendin-4 | Regulates blood glucose | Not mentioned | Not mentioned | 43 ±4.0 | Rat plasma proteases | ELISA | Subcutaneously administion of 100 µg/kg dose to Sprague Dawley rats | in vivo | None | None | ED50=1.3 µg/kg for glucose lowering in C57BL/6 mice | |||
| 22286034 | 2012 | Motilin | 22 | Free | Free | Linear | L | None | Motilin is a gastro-intestinal peptide hormone | Endocrine regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 3.3 ±1.0 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.9x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(6 €“28) | 35 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 11.7 ±3.4 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.5x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(8 €“28) | 33 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 11.1 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.4x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(10 €“28) | 31 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.6x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“28) | 29 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.6x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(14 €“28) | 27 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.0 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=6.1x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(16 €“28) | 25 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 9.4 ±0.6 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.2x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(18 €“28) | 23 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 5.3 ±1.3 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.0x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(19 €“28) | 22 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 6.0 ±0.3 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.1x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“26) | 27 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 10.4 ±0.1 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.5x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“24) | 25 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 5.8 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=4.8x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“22) | 23 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 6.3 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=2.4x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“20) | 21 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 7.0 ±2.6 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=7.3x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“18) | 19 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 3.1 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.8x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“16) | 17 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 2.4 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.2x10-10nM for GPR38 agonist activity | |||
| 17107718 | 2006 | Glucagon-like peptide-2 (GLP-2) | 33 | Free | Free | Linear | L | None | Posttranslational processing of proglucagon | Stimulate intestinal growth | Not mentioned | Not mentioned | 6.8 ±0.8 | Pig plasma proteases | ELISA | Infused into blood of pigs | in vivo | None | None | Not reported | |||
| 17107718 | 2006 | Glucagon-like peptide-2 (GLP-2) | 33 | Free | Free | Linear | L | None | Posttranslational processing of proglucagon | Stimulate intestinal growth | Not mentioned | Not mentioned | 9.9 ±0.8 | Pig plasma proteases with valine-pyrrolidide (DPP-IV inhibitor) | ELISA | Infused into blood of pigs | in vivo | None | None | Not reported | |||
| 14499707 | 2003 | GRF1-29 | 29 | Free | Amidation | Linear | L | None | Growth hormone-releasing hormone (GRF) analogue | Stimulates release of growth hormone | Not mentioned | Not mentioned | 10 to 20 | Human plasma proteases | Not mentioned | Human plasma | in vivo | None | None | EC50=0.18nM | |||
| 22592200 | 2012 | Ghrelin | 28 | Free | Free | Linear | L | Fatty acid ie n-octanoic acid present at serine at position 3, (125)I labelling | Ghrelin | GH-releasing and appetite stimulating peptide | Not reported | Not mentioned | 15-18 | Rat blood proteases | Radioactivity measured by scintillation counter | Administered into blood of rats | in vivo | 15788704 | None | Not reported | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.17 ±0.08 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | Intraperitoneal hypoglycemic efficacy in db/db mice was 30 ±7.2% | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.34 ±0.07 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | Intraperitoneal hypoglycemic efficacy in db/db mice was 30 ±7.2% | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 4.34 ±0.21 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | Oral hypoglycemic efficacy in db/db mice was 25.3 ±6.6% | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 2.77 ±0.05 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | Oral hypoglycemic efficacy in db/db mice was 25.3 ±6.6% | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.17 ±0.08 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | EC50=3.82 ±0.32nM insulinotropic activity | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.34 ±0.07 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | EC50=3.82 ±0.32nM insulinotropic activity | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 4.34 ±0.21 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | EC50=3.85 ±0.21nM insulinotropic activity | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 2.77 ±0.05 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | EC50=3.85 ±0.21nM insulinotropic activity | |||
| 20585128 | 2010 | Sub3 | 12 | Free | Amidation | Linear | L | None | Derived from bovine peptide bactenecin | Antimicrobial | Not reported | 150 µg/ml | ~60 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=1 µg/ml for S. Aureus | |||
| 20585128 | 2010 | Sub3-D | 14 | Free | Amidation | Linear | Mix | None | Derivative of Sub4 | Antimicrobial | Not reported | 150 µg/ml | ~60 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=1 µg/ml for S. Aureus | |||
| 20585128 | 2010 | Sub3 | 12 | Free | Amidation | Linear | L | None | Derived from bovine peptide bactenecin | Antimicrobial | Not reported | 150 µg/ml | ~60 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=2 µg/ml for P. Aeruginosa | |||
| 20585128 | 2010 | Sub3-D | 14 | Free | Amidation | Linear | Mix | None | Derivative of Sub4 | Antimicrobial | Not reported | 150 µg/ml | ~60 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=2 µg/ml for P. Aeruginosa | |||
| 9740616 | 1998 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Angiotensinogen | Antihypertensive | 30 min | 10 µg | ~60 ±1 | Angiotensin-converting enzyme and lisinopril(inhibitor) | Radioimmunoassay and HPLC | Blood sample of normotensive Sprague-Dawley rat | in vivo | None | None | Not mentioned | |||
| 9806949 | 1998 | MEN 11420 | 6 | Glycosylation | Free | Cyclic | L | Dpr-2,3-Diaminopropionic acid | MEN 10627 | Tachykinin NK2 receptor antagonist | Not reported | Not mentioned | 44 ±3 | Not mentioned | HPLC | Rat blood plasma | in vivo | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 8 | γ-secretase | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 1 | γ-secretase (protease) Lactacystin(protease inhibitor) | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 659633 | 1978 | C-peptide | 31 | Free | Free | Linear | L | None | Proinsulin | Not mentioned | Not reported | 0.75pmol/ml | 33.5(mean) | Not mentioned | Single-dose injection technique | 6 Normal human male blood plasma sample | in vivo | None | None | Not mentioned | |||
| 659633 | 1978 | C-peptide | 31 | Free | Free | Linear | L | None | Proinsulin | Not mentioned | Not reported | 0.9pmol/ml | 42.5(mean) | Not mentioned | Single-dose injection technique | 7 Diabetic human male blood plasma sample | in vivo | None | None | Not mentioned | |||
| 3343338 | 1987 | Anti-cell adhesive pentapeptide | 5 | Free | Free | Linear | L | None | Central cell- binding domain of fibronectin | Anti metastatic | Not reported | 6 µmol | 8 | Not mentioned | Radioactivity measured by scintillation counter | Blood sample of C57BL/6 mice | in vivo | None | None | Percentage inhibition of melanotic colony formation=90 | |||
| 6086405 | 1984 | Hydra head activator | 11 | Free | Free | Linear | L | Glp-Pyroglutamic acid | Hydra but also found in rat intestine,human and bovine hypothalamus | In hydra-stimulatory effects on growth and differentition,in human-in digestion control process | 2 hour | 20-100 fmol/ml | 7 | Not mentioned | Radioimmunoassay | Human plasma | in vitro | None | None | Not mentioned | |||
| 6117506 | 1981 | Somatostatin | 14 | Free | Free | Cyclic (C3-C14) | L | None | Ovine | Local transmitters either paracrine or neurocrine | 5 days | 100ng | 1.0 ±0.2 | Not mentioned | Radioimmunoassay | Blood plasma sample from five mongrel dogs | in vivo | 4682131 | None | Not mentioned | |||
| 7439398 | 1980 | Glutathione | 3 | Free | Free | Linear | L | Gamma peptide linkage between the carboxyl group of the glutamate side-chain and the amine group of cysteine | Synthetic | Not mentioned | Not reported | 25 ng/kg/min of Bradykinin and the rate doubled every 5 min until a final rate of 200 ng/kg/min was | 1.6 | Not mentioned | Kinetic assay | Human blood plasma sample | in vivo | None | None | Not mentioned | |||
| 8257427 | 1993 | AcSDKP | 4 | Acetylation | Free | Linear | L | None | Human bone marrow | Negative regulator of proliferation of haematopoietic stem cells | Not reported | 10nM conc. | 50 | None | Radioactivity measured with liquid-scintillation counter | Human venous blood sample | in vitro | None | None | Not mentioned | |||
| 8257427 | 1993 | AcSDKP | 4 | Acetylation | Free | Linear | L | None | Human bone marrow | Negative regulator of proliferation of haematopoietic stem cells | Not reported | 10-4M conc | 10 | Rabbit lung angiotensin I converting enzyme | Radioactivity measured with liquid-scintillation counter | Human venous blood sample | in vitro | None | None | Not mentioned | |||
| 8257427 | 1993 | AcSDKP | 4 | Acetylation | Free | Linear | L | None | Human bone marrow | Negative regulator of proliferation of haematopoietic stem cells | Not reported | 10-7M conc. | 25 | Rabbit lung angiotensin I converting enzyme | Radioactivity measured with liquid-scintillation counter | Human venous blood sample | in vitro | None | None | Not mentioned | |||
| 10611139 | 1999 | Hexarelin | 6 | Free | Amidation | Linear | Mix | 2me-2-methyl(tryptophan) | Analog of GHRP-6 | Peptidyl growth hormone causing GH releasing effect. | Not reported | 50 µg/kg | 57.0 ±9.1 | Blood proteases | LC-MS/MS | Intravenous injection,Blood sample from male Sprague-Dawley rats | in vivo | None | None | Not mentioned | |||
| 10647619 | 2000 | TP 850 | 10 | Free | Free | Linear | Mix | 4-aminobutyric acid (Aba) | Modified fibrin α chain N-terminal peptide | Blood Coagulation | Not reported | 11 to 25 iu of oxytocin | 4 | Blood proteases | Radiolabelling and HPLC | Intravenous injection,Blood sample of rabbit | in vivo | None | None | Platelet aggregation inhibition, IC50=236μm for dog and IC50=167μm for rabbit. | |||
| 12119302 | 2002 | 1a | 18 | Acetylation | Amidation | Linear | L | None | Synthetic | Coagulation factor VIIa peptide exosite inhibitor | Not reported | 106 cpm/200μl/mouse | 7.6 | Blood proteases | ESI-LC ˆ’MS/MS | Rabbit blood sample | in vivo | None | None | Not mentioned | |||
| 3799211 | 1986 | (I-deamino-8-D-arginine vasopressin)DDAVP | 9 | 1-β-mercaptopropionic acid | Free | Linear | Mix | None | Modified form of Vasopressin | Antidiuretic agent | Not reported | 45mg | 55 | Plasma proteases | Radioimmunoassay | Human blood sample | N.A. | None | US 5500413 A patent | Not mentioned | |||
| 10454085 | 1999 | Oxytocin | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Hypothalamus | Involved in aiding mechanical clearance mechanism and improving fertility | 60 minutes | 90mg | 6.78 | Blood protease | Radioimmunoassay | Intravenous injection of oxytocin in normal mares | in vivo | None | None | Prostaglandin F metabolite(PGFM) release on administeration of 10 iu of oxytocin= 18.48 ±3.62 pg/ml | |||
| 10454085 | 1999 | Oxytocin | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Hypothalamus | Involved in aiding mechanical clearance mechanism and improving fertility | 60 minutes | 180mg | 6.78 | Blood protease | Radioimmunoassay | Intravenous injection of oxytocin in normal mares | in vivo | None | None | Prostaglandin F metabolite(PGFM) release on administeration of 25 iu of oxytocin= 20.09 ±3.29 pg/ml | |||
| 10544005 | 1999 | YIGSR | 5 | Free | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | <1 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 1.5μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 50% | |||
| 10544005 | 1999 | PEG5000 -YIGSR | 5 | Pegylated by addition of PEG5000 | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | 2.2 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 0.15μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx. | |||
| 10544005 | 2000 | PEG12,000 -YIGSR | 5 | Pegylated by addition of PEG12,000 | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | 2.5 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 0.15μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 50% | |||
| 10544005 | 2001 | PVP6,000 -YIGSR | 5 | Addition of Polyvinyl pyrrolidone(PVP6,000) | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | 14.5 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 0.015μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx. | |||
| 1697165 | 1990 | ANP' | 26 | Free | Free | Cyclic | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 1.04 | Rat blood proteases | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 7.81 ± 0.38 | Kallikrein and Endopeptidase 24.11 in presence of inhibitor Phosphoramidon | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 2.51 ±0.25 | Kallikrein and Endopeptidase 24.11 in presence of inhibitor Aprotinin | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 15.2 ± 1.01 | Kallikrein and Endopeptidase 24.11 in presence of inhibitors phosphoramidon and aprotinin both | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1939259 | 1991 | α-bag cell peptide α-BCP(1-9) | 9 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 26 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-bag cell peptide α-BCP(1-9) | 9 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-6 M conc. of peptide | 35 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(1-8) | 8 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 27 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(1-6) | 6 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 11 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(1-5) | 5 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 16 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(3-9) | 7 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 2.1 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(3-9) | 7 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-6 M conc. of peptide | 2.7 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(4-9) | 6 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 2.7 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(5-9) | 5 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 1.5 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(7-9) | 3 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 9.7 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(3-8) | 6 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 1.5 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 1939259 | 1991 | α-BCP(4-8) | 5 | Free | Free | Linear | L | None | Bag cells in the abdominal ganglion of the marine snail Aplysia | Neurotransmitter | Not reported | 10-5 M conc. of peptide | 1.5 | Aplysia haemolymph proteases | HPLC | Heamolymph of Aplysia | in vitro | None | None | Not given | |||
| 15769092 | 2005 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 10 µg/kg | 9.09 | Rat blood proteases | ELISA | Rat blood plasma (Subcutaneous Injection) | in vivo | None | None | 100nmol/L GLP-1 enhanced insulin release by 3.4 ±0.7-fold per islet in presence of 16.8mmol/L glucose | |||
| 15769092 | 2005 | PEG2k-Lys-GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at Lysine | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 10 µg/kg | 21.67 | Rat blood proteases | ELISA | Rat blood plasma (Subcutaneous Injection) | in vivo | None | None | 100nmol/L GLP-1 stimulated insulin release of 306.6 ±72.8 pmol/L per islet in presence of 16.8mmol/L glucose | |||
| 15769092 | 2005 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 1 µg/kg | 2.61 | Rat blood proteases | ELISA | Rat blood plasma (Intravenous injection) | in vivo | None | None | 100nmol/L GLP-1 enhanced insulin release by 3.4 ±0.7-fold per islet in presence of 16.8mmol/L glucose | |||
| 15769092 | 2005 | PEG2k-Lys-GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at Lysine | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 1 µg/kg | 33.36 | Rat blood proteases | ELISA | Rat blood plasma (Intravenous injection) | in vivo | None | None | 100nmol/L GLP-1 stimulated insulin release of 306.6 ±72.8 pmol/L per islet in presence of 16.8mmol/L glucose | |||
| 15882144 | 2005 | Ucn1 (urocortin 1) | 40 | Free | Free | Linear | L | None | Urocortin 1 | Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetite | Not reported | 50 μg | 54 ±3 | Human blood proteases | Not mentioned | Human blood plasma(Male patients with stable congestive heart failure) (Intravenous injection) | in vivo | None | None | Not given | |||
| 15882144 | 2005 | Ucn1 (urocortin 1) | 40 | Free | Free | Linear | L | None | Urocortin 1 | Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetite | Not reported | 50 μg | 52 ±3 | Human blood proteases | Not mentioned | Human blood plasma (Normal humans) (Intravenous) | in vivo | None | None | Not given | |||
| 16099941 | 2005 | proADM 45 €“92 (Adrenomedullin) | 48 | Free | Free | Linear | L | None | Synthetically synthesised proADM 45 €“92 | Vasodilatory peptide | Not reported | 0.29nmol/L | 22 | Human blood proteases | Sandwich immunoluminometric Assay | Human blood plasma | in vitro | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 5.6 ±0.45 | Human blood proteases | Not mentioned | Human plasma of patients with mild, stable heart failure | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 11 ±1.3 | Human blood proteases | Not mentioned | Human plasma of patients with mild, stable heart failure given infusion of metoprolol | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 5.7 ±0.8 | Human blood proteases | Not mentioned | Human plasma (Normal humans) | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 6.6 ±1.3 | Human blood proteases | Not mentioned | Human plasma (Normal humans given infusion of metoprolol) | in vivo | None | None | Not given | |||
| 16472750 | 2006 | E2-PESTE304Q | 29 | Free | Free | Linear | L | None | E2 protein from papillomavirus | Gene transcription | Not reported | Not mentioned | 24 | Not mentioned | Pulse chase experiment | pMEP-E2 CV-1 cell lines | in vitro | 15014086 | None | Not mentioned | |||
| 16586064 | 2006 | GLP1 | 30 | Free | Amidation | Linear | L | None | Synthetically synthesized Glucagon-like peptide-1 | Insulinotropic | Not reported | Not mentioned | 6 ±0.5 | Rat liver proteases | RP-HPLC | Rat liver homogenate | in vitro | 16505481 | None | 380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | GLP1 | 30 | Free | Amidation | Linear | L | None | Synthetically synthesized Glucagon-like peptide-1 | Insulinotropic | Not reported | Not mentioned | 1 ±0.2 | Rat kidney proteases | RP-HPLC | Rat kidney homogenate | in vitro | 16505481 | None | 380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | N-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at N terminus His7 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 23 ±7 | Rat kidney proteases | RP-HPLC | Rat kidney homogenate | in vitro | 16505481 | None | 290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | Lys-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation on Lys34 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 28 ±1 | Rat kidney proteases | RP-HPLC | Rat kidney homogenate | in vitro | 16505481 | None | 150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16990557 | 2006 | cNGR | 8 | Acetylation | Amidation | Cyclic | L | None | Synthetic peptide | Targets CD13/APN which is present on angiogenic vessels so used for molecular imaging | Not reported | 0.75μg/g | 15.4 ±3.4 | Mouse plasma proteases | Fluorometery | Mouse plasma of Murine myocardial infarction (MI) model | in vivo | None | None | Not given | |||
| 17374660 | 2007 | IPP | 3 | Free | Free | Linear | L | None | Lactotripeptide | ACE(Angeotensin converting enzyme)-inhibiting peptide | Not reported | Not mentioned | ~ 30 | Pancreatic proteases | RP-HPLC | Human blood plasma (oral) | in vivo | None | None | Not given | |||
| 17479256 | 2007 | ANP | 26 | Free | Free | Linear | L | None | Synthetic peptide | Atrial natriuratic peptide | Not reported | 0.05 μg/kg per minute | 2.4 ±0.7 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not given | |||
| 17479256 | 2007 | BNP | 32 | Free | Free | Linear | L | None | Synthetic peptide | Vasodilator | Not reported | 0.01 μg/kg per minute | 12.1 ±3.0 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not given | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.008 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.033 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.060 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.151 µg/ml against 098-T1249 virus virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=7.599 µg/ml against 098-T651 virus | |||
| 18085721 | 2007 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Counter-regulatory hormone | Not reported | Not mentioned | ~2 | DPP-IV | ELISA | Mouse plasma | in vivo | None | None | Not given | |||
| 18307313 | 2007 | CAP 1 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 83 µM for S.aureus | |||
| 18307313 | 2007 | CAP 1 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 50 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 1 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 25 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 5 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 11 µM for S.aureus | |||
| 18307313 | 2007 | CAP 5 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 9 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 5 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 6 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 6 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 14 µM for S.aureus | |||
| 18307313 | 2007 | CAP 6 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 9 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 6 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 1 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 6 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 19 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 29 µM for S.aureus | |||
| 18307313 | 2007 | CAP 19 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 29 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 19 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 20 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 19 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 29 µM for S.aureus | |||
| 18307313 | 2007 | CAP 19 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 29 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 19 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 20 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 20 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 50 µM for S.aureus | |||
| 18307313 | 2007 | CAP 20 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 50 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 20 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 10 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 20 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 50 µM for S.aureus | |||
| 18307313 | 2007 | CAP 20 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 50 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 20 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 0.6 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 10 µM for Methicillin- resistant S.epidermis | |||
| 18481852 | 2008 | 3A | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 580 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | 3A' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 910 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | 3B | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 345 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | 3B' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 655 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A.A.B | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 190 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A.A.B' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 300 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A'.A'.B | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 325 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18481852 | 2008 | A'.A'.B' | 117 | Acetylation | Amidation | Linear | L | None | Synthetic Collagen peptide | Structural component of connective tissues | Not reported | Not mentioned | 470 | Not mentioned | HPLC and MALDI-TOF | Not reported | in vitro | None | None | Not available | |||
| 18553094 | 2008 | BNP | 32 | Free | Free | Linear | L | None | Pro-Brain natriuretic peptide | Vasodilator | Not reported | Not mentioned | ~22 | Human blood proteases | ELISA | Human plasma | in vitro | None | None | Not available | |||
| 19223422 | 2009 | HBP-1 | 13 | Free | Free | Linear | L | None | Synthetic peptide | Not mentioned | Not reported | Not mentioned | 55 | Not mentioned | HPLC | Human serum | in vitro | None | None | IC50=38.9nM | |||
| 19403044 | 2008 | GLP-1/Fc | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | 16nM | ~20 | Rabbit serum proteases | Luciferase reporter assay | Rabbit serum | ex vivo | None | None | Not available | |||
| 19403044 | 2008 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | 0.4nM | <5 | Rabbit serum proteases | Luciferase reporter assay | Rabbit serum | ex vivo | None | None | Not available | |||
| 19413309 | 2009 | HM3 | 17 | Free | Free | Linear | L | None | RGD- modified endostatin derived peptide | Antitumor | Not reported | 1mg/ml | 27.66 ± 7.37 | Rat blood proteases | RP-HPLC | Rat blood serum (Intravenous injection) | in vivo | None | None | Less active in the inhibition of angiogenesis in the chorioallantoic membrane of chick embryos | |||
| 19458086 | 2009 | ANP | 28 | Free | Free | Cyclic (C7-C23) | L | None | C terminus of atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 1 µM | 2.6 | Human kidney membrane proteases | Radioimmunoassay | Human kidney membranes | in vitro | None | None | IC50=2.4nM | |||
| 19458086 | 2009 | fsANP | 40 | Free | Free | Cyclic (C7-C23) | L | None | C terminus of atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 1 µM | 4.5 | Human kidney membrane proteases | Radioimmunoassay | Human kidney membranes | in vitro | None | None | IC50=3.2nM | |||
| 19531053 | 2009 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | Not mentioned | 20 | DPP IV | ELISA | Mice (Subcutaneous injection) | in vivo | None | None | Not available | |||
| 19552923 | 2011 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Insulinomimetic and insulinotropic | Not reported | 27.9 ± 5.8 μg/ml | 1 to 2 | Rabbit blood proteases | ELISA | Rabbit blood | in vivo | None | None | Not available | |||
| 19572636 | 2009 | N-WASP181-200 | 20 | Free | Free | Linear | L | None | Synthetic peptide | Inhibits renal accumulation of aminoglycoside antibiotics | Not reported | 1 mg/mL | 6.7 | Not mentioned | HPLC | Rat renal brush border membrane suspension | in vitro | None | None | IC50=0.041 mM with gentamicin | |||
| 19572636 | 2009 | PEG1k-N-W | 20 | Pegylation | Free | Linear | L | None | Synthetic peptide | Inhibits renal accumulation of aminoglycoside antibiotics | Not reported | 100 µg/mL | 12.9 | Not mentioned | HPLC | Rat renal brush border membrane suspension | in vitro | None | None | IC50=0.128 mM with gentamicin | |||
| 19572636 | 2009 | N-WASP181-200 | 20 | Free | Free | Linear | L | None | Synthetic peptide | Inhibits renal accumulation of aminoglycoside antibiotics | Not reported | 100 µg/mL | 6.7 | Not mentioned | HPLC | Rat renal brush border membrane suspension | in vitro | None | None | IC50=46.1 mg/kg with Arbekacin | |||
| 19572636 | 2009 | N-WASP181-200 | 20 | Free | Free | Linear | L | None | Synthetic peptide | Inhibits renal accumulation of aminoglycoside antibiotics | Not reported | 100mg/kg | 2.7 | Not mentioned | HPLC | Rat blood plasma (Intravenous) | in vivo | None | None | IC50=46.1 mg/kg with Arbekacin | |||
| 19572636 | 2009 | PEG1k-N-W | 20 | Pegylation | Free | Linear | L | None | Synthetic peptide | Inhibits renal accumulation of aminoglycoside antibiotics | Not reported | 100mg/kg | 4.6 | Not mentioned | HPLC | Rat blood plasma (Intravenous) | in vivo | None | None | IC50=17.8 mg/kg with Arbekacin | |||
| 19572636 | 2009 | PEG1k-N-W | 20 | Pegylation | Free | Linear | L | None | Synthetic peptide | Inhibits renal accumulation of aminoglycoside antibiotics | Not reported | 100 µg/mL | 12.9 | Not mentioned | HPLC | Rat renal brush border membrane suspension | in vitro | None | None | IC50=17.8 mg/kg with Arbekacin | |||
| 11962721 | 2001 | CTR-S domain | 124 | Free | Free | Linear | L | None | CTR (Calreticulin) | It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathway | Not reported | Not mentioned | 1.21 ± 0.34 in distribution phase | Serine Proteases | Radioactivity measured with a gamma counter | Rat plasma | in vivo | None | None | Biological activity =2 m Ci/nmol | |||
| 11962721 | 2001 | CTR-S domain | 124 | Free | Free | Linear | L | None | CTR (Calreticulin) | It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathway | Not reported | Not mentioned | 40.5 ± 2.7 in elimination phase | Serine Proteases | Radioactivity measured with a gamma counter | Rat plasma | in vivo | None | None | Biological activity =2 m Ci/nmol | |||
| 11976797 | 2002 | GLP-1 | 30 | Free | Amidation | Linear | L | Radiolabelling of GLP-1by [123I] | Proglucagon molecule | Antidiabetic | Not reported | 10 MBq of the radiolabelled peptides | 7.0 ±2.1 for É‘ phase | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 11976797 | 2002 | Exendin 3 | 39 | Free | Free | Linear | L | Radiolabelling of exendin 3 at position 1 (histidine) | Heloderma horridum venom | GLP-1 agonist | Not reported | 10 MBq of the radiolabelled peptides | 13 ±3.2 | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 15587934 | 2004 | Human BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 3.1 | Not mentioned | EIA | Mice plasma (Intravenous injection) | in vivo | None | None | EC50 =0.46 ± 1.1 nM | |||
| 17292492 | 2007 | NT-ANP | 98 | Free | Free | Linear | L | None | ANP (A- type natriuretic peptide) | Natriuretic, diuretic and vasorelaxant | Not reported | 650fmol/ml | 1 | Human blood proteases | Radioimmunoassay | Human blood | in vitro | None | None | Not mentioned | |||
| 18353507 | 2008 | PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | 23 ±6 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 7.7 ±1.4 nM | |||
| 18353507 | 2008 | PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 4.3 ±0.3 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 7.7 ±1.4 nM | |||
| 18353507 | 2008 | [ψCH2-NH21-22]PACAP38 | 38 | Free | Amidation | Linear | L | [ψCH2-NH21-22] | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 18 ±2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 59 ±17 nM | |||
| 18353507 | 2008 | [Ala20]PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 8.3 ±1.2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 1.2 ±0.4 nM | |||
| 18353507 | 2008 | [Ala21]PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 6.6 ±0.5 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 2.0 ±0.5 nM | |||
| 18353507 | 2008 | Acetyl-[Ala14, Ala20]PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 15 ±2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 5.3 ±1.7 nM | |||
| 18353507 | 2008 | Acetyl-[Ala15, Ala20]PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 25 ±2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 1.8 ±0.7 nM | |||
| 18353507 | 2008 | PACAP27 | 27 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | 39 ±4 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 9.6 ±2.4 nM | |||
| 19041716 | 2009 | SST (Somatostatin) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Somatostatin | Neurotransmitter | Not reported | 1.8 mg/ml | 7.6 | Rat blood proteases | ELISA | Rat plasma (Intravenous injection) | in vivo | None | None | Not available | |||
| 19041716 | 2009 | LCNP/SST (Somatostatin adsorbed on Liquid crystalline nanoparticles for 10 min) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Somatostatin adsorbed on Liquid crystalline nanoparticles | Neurotransmitter | Not reported | 1.8 mg/ml | 0.73 ±0.03 | Rat blood proteases | ELISA | Rat plasma (Intravenous injection) | in vivo | None | None | Not available | |||
| 19041716 | 2009 | LCNP/SST (Somatostatin adsorbed on Liquid crystalline nanoparticles for 18 hours) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Somatostatin adsorbed on Liquid crystalline nanoparticles | Neurotransmitter | Not reported | 1.8 mg/ml | 0.79 ±0.17 | Rat blood proteases | ELISA | Rat plasma (Intravenous injection) | in vivo | None | None | Not available | |||
| 19836183 | 2010 | BNP | 32 | Free | Free | Linear | L | None | Porcine brain | Vasodilator | Not reported | 31.2ng/ml | 3.1 | Mouse plasma proteases | ELISA | Mouse plasma | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 52.1 | Mouse blood proteases | EIA | Mice blood serum (oral delivery in 0.5% Intravail) | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 25.8 | Mouse blood proteases | EIA | Mice blood serum (oral delivery in 1.5% Intravail) | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 23.6 | Mouse blood proteases | EIA | Mice blood serum (oral delivery in 3.0% Intravail) | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 1.3 | Mouse blood proteases | EIA | Mice blood serum (Subcutaneous injection) | in vivo | None | None | Not mentioned | |||
| 22934681 | 2012 | DAMGO | 5 | Free | Free | Linear | Mix | Methylation at phenylalanine | Synthetic peptide | Opioid peptide | Not reported | 5.0 mg/kg | 9.2 ± 2.1 | Rat blood proteases | ESI-LC ˆ’MS/MS | Rat blood plasma (Intravenous) | in vivo | None | None | Not mentioned | |||
| 23836030 | 2013 | HNG ( substitution at position 14 (Gly for Ser) in HN seq) | 24 | Free | Free | Linear | L | None | Synthetic peptide | Cytoprotective | Not reported | 16 fold higher than original concentration | ~30 | Mouse plasma proteases | ELISA | Mice plasma | in vitro | 15655255 | None | Not available | |||
| 24378440 | 2013 | EGFR2R-lytic peptide | 32 | Free | Free | Linear | Mix | None | Synthetic peptide | Cytotoxic and antitumor | Not reported | Not mentioned | 9.4 ± 1.5 | Not mentioned | Not mentioned | Bovine serum | in vivo | None | None | Not available | |||
| 24378440 | 2013 | EGFR2R-lytic peptide-gelatin complex | 32 | Free | Free | Linear | Mix | None | Synthetic peptide | Cytotoxic and antitumor | Not reported | Not mentioned | 19.3 ±2.9 | Not mentioned | Not mentioned | Bovine serum | in vivo | None | None | Not available | |||
| 3348603 | 1987 | DihydromycoplanecinA (DHMP A) | 10 | alpha-hydroxybutyric acid | Free | Cyclic | L | N-MeVal; N-methylvaline, EtPro; Ethylproline, N-MeThr; N-methylthreonine MePro; Methylproline, AMHA; 2-amino-5-methylhexanoic acid, N-MeLeu; N-methylleucine | Active metabolite in urine of mice and dogs | Antibiotic | Not reported | 10 mg/kg | 0.5 | Mouse blood proteases | Not mentioned | Mice serum (Intravenous) | in vivo | None | None | LD50>6000mg/kg administered orally to mice | |||
| 6117506 | 1981 | Vasoactive Intestinal Peptide | 28 | Free | Amidation | Linear | L | None | Porcine vasoactive intestinal peptide | Vasoactive intestinal peptide | Not reported | 103.7 ± 14.8 ml/kg | 1.80 ± 0.1 | Dog blood proteases | Radioimmunoassay | Dog plasma (Intravenous) | in vivo | None | None | 150-220 µci/ µg | |||
| 8181115 | 2014 | Atrial natriuretic factor (ANF) | 28 | Free | Free | Linear | L | None | Cardiac atria | Peptide hormone | Not reported | Not mentioned | 2.5 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not available | |||
| 8406670 | 2014 | Atrial natriuretic factor (ANF) | 28 | Free | Free | Linear | L | None | Cardiac atrium in response to myocardial stretch | Peptide hormone | Not reported | Not mentioned | 20 to 180 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not available | |||
| 8910426 | 1996 | LL:36 €“45 | 10 | Free | Free | Linear | L | None | Analogue of Limulus anti-lipopolysaccharide factor | Antibacterial | Not reported | 2.5 µg/ml | 17 | Proteases present in fetal calf serum | RP-HPLC | Fetal calf serum | in vitro | None | None | No cell lysis done by this peptide | |||
| 9067297 | 1996 | E-2078 [N-methyl-Tyr1, N-methyl-Arg7-D-Leu8] Dyn A (1 €“8) ethylamide] | N.A. | Methylation | Ethylamide | Linear | Mix | Methylation on Arg7 and Tyr1 | Dynorphin A (1 €“ 8) analog | Analgesic | Not reported | 10 mg/kg | 44 | Monkey blood proteases | MALDI-MS | Rhesus monkey blood plasma (Intravenous) | in vivo | 7479294 | None | Not available | |||
| 20418955 | 2010 | Glucagon | 29 | Free | Free | Linear | L | None | Pancreas | Plays a major regulatory role in controlling hypoglycemia | Not reported | Not mentioned | <10 | Human blood proteases | ELISA | Human serum | in vitro | None | None | Not available | |||
| N.A. | 2004 | Melan-A27-35 | 9 | Free | Free | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 5 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 4 nM | |||
| N.A. | 2004 | Melan-A26-35 | 10 | Free | Free | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 45 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.25 nM | |||
| N.A. | 2004 | Melan-A26-35 A27L | 10 | Free | Free | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 40 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.01 nM | |||
| N.A. | 2011 | Motilin | 22 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 3.26 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin A | 35 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.74 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin B | 34 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin C | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.9 ±0.53 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin D | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.9 ±0.50 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin E | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin F | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.37 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin G | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.25 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin H | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.43 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin I | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.76 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin J | 25 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 6.34 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin K | 23 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 6.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin L | 21 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 4.89 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin M | 19 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 2.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin N | 28 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.12 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin O | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.73 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin P | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.67 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Q | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.65 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin R | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.13 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin S | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.29 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin T | 29 | Free | Free | Linear | L | Ornithine | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.47 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin U | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.66 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin V | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin W | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin X | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.89 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Y | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.6 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Z | 30 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.53 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-i | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.55 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-ii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.5 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-iii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.65 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-iv | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.73 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-v | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.94 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-vi | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.94 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-vii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 12.78 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-viii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.56 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-ix | 26 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 4.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-x | 28 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.25 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xi | 26 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.29 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xii | 33 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 13.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xiii | 34 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 13.09 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 2.88 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-A | 39 | Free | Free | Cyclic (C1-C17) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 24 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-B | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 40 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-C | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 27.2 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 11.2 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-A | 39 | Free | Free | Cyclic (C1-C17) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 46.4 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-B | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 57.3 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-C | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 37.8 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 7.8 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-A | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 20.7 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-B | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 24 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 2.93 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-A | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 21.7 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-C | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 15.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-D | 37 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 20.3 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-E | 46 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 18.4 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-F | 51 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 17.38 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-G | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 17.75 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-H | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 14.86 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-I | 34 | Free | Amidation | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 14.5 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-J | 39 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 20 nm/ Kg | 31.24 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-K | 35 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 20 nm/ Kg | 18.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-53 (C-type natriuretic peptide) | 58 | Free | Free | Cyclic (C42-C58) | L | None | CNP-58 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 15.72 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-58 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 1.11 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2012 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | 520 micro g/Kg | 0.8 | Not mentioned | EIA | Rat plasma (Subcutaneous) | in vivo | None | EP2423233A2 | Blood glucose after 24 hour >25 mM | |||
| N.A. | 2006 | Derivative of Glucagon Like Peptide-2 (GLP-2) | 33 | Free | Amidation | Linear | L | None | GLP-2 | Intestine function modulator | N.A. | 500 nM/ Kg | 0.9 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | US7112567B2 | Not mentioned | |||
| N.A. | 2009 | Modified Dynorphin (1-13) | 13 | Free | Addition of hydroxyl group | Linear | L | None | Dynorphin peptide | Endogenous opioid found in CNS | N.A. | 4 mg/ ml | 10 | Not mentioned | LC/MS | plasma | in vitro | None | US 20090175821Al | Not mentioned | |||
| N.A. | 2009 | Modified Dynorphin(1-13) | 13 | Free | Amidation | Linear | L | None | Dynorphin peptide | Endogenous opioid found in CNS | N.A. | 4 mg/ ml | 30 | Not mentioned | LC/MS | plasma | in vitro | None | US 20090175821Al | Not mentioned | |||
| N.A. | 2012 | Val8-GLP-1-OH | 31 | Free | Addition of hydroxyl group | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 10 micro g/ kg | 0.05 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 100% (as reference) | |||
| N.A. | 2012 | Exendin-4 | 39 | Free | Free | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 0.7 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 100% (as reference) | |||
| 15369394 | 2004 | Interferon α2 (IFNα2) | 146 | Free | Free | Cyclic(C1-C98, C29-138) | L | Glycosylation at Thr-105 | IFNα2 | Antiviral and antiproliferative | 0-25 hours | 10 μg/rat in 0.2 mL of PBS | ~1 | Rat blood proteases | BIAcore binding assay | Intravenously administered to wistar rats | in vivo | http://www.uniprot.org/uniprot/P01563 | None | Following administration of IFNα2 (100 μg/rat), the circulating antiviral activity declined with a t1/2 value of ˆ¼1 h, reaching a level lower than 20 pM IFNα2, 12 h after administration. | |||
| 730072 | 2001 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | None | Porcine VIP | Antiinflammatory and vasodilatory | 0 5, 1, 2,3, 4, 5, 6, 7, 8, 9, 10, 12, 15, 20, and 30 minutes | 0.6, 1.3, and 3.3 pmol/kg/min infused over 30 minutes | ~1 | Human blood proteases | Radioimmunoassay | Intravenous infusion to humans | in vivo | http://www.uniprot.org/uniprot/P01282 | None | Infusion of the highest dose of VIP, plasma concentrations of glucose were significantly raised from a basal level of 5.05 ± 0.29 to 5.61 ± 0.27mmol/l. Plasma levels of free fatty acids were increased from 0.40 ± 0.06 to 0.96 ± 0.09 mmol/l | |||
| 12954066 | 2003 | Neurotensin | 13 | Free | Free | Linear | L | None | Bovine hypothalamus | Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis | Not mentioned | 1.07mM | 5.9 ±0.2 | Rat serum protease | MALDI-TOF-MS | Rat serum | in vitro | None | None | Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells. | |||
| 12954066 | 2003 | KK16 | 13 | Free | Free | Linear | L | COOH-CH(NH2)-CH-CH-CH(NH)-C=NR(H2N) at 8th arginine position | Derivative of Bovine hypothalamus | Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis | Not mentioned | 1.07mM | 14.2 ±0.3 | Rat serum protease | MALDI-TOF-MS | Rat serum | in vitro | None | None | Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells. | |||
| 12954066 | 2003 | KK17 | 13 | Free | Free | Linear | L | COOH-CH(H2N)CH-CH-CH(HN)-CH(imidazole) at 8th arginine position | Derivative of Bovine hypothalamus | Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis | Not mentioned | 1.07mM | 31.5 ±0.6 | Rat serum protease | MALDI-TOF-MS | Rat serum | in vitro | None | None | Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells. | |||
| 12954066 | 2003 | KK18 | 13 | Free | Free | Linear | L | COOH-CH(NH2)CH-CH-CH(N-CH-CH-NH-C=NH-CH) at 8th arginine position | Derivative of Bovine hypothalamus | Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis | Not mentioned | 1.07mM | 15.9 ±1.6 | Rat serum protease | MALDI-TOF-MS | Rat serum | in vitro | None | None | Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells. | |||
| 12954066 | 2003 | KK19 | 13 | Free | Free | Linear | L | COOH-CH(NH2)CH-CH-CH(N-CH-CH-NH-C=NH-CH) at 8th arginine position | Derivative of Bovine hypothalamus | Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis | Not mentioned | 1.07mM | 16.5 ±0.6 | Rat serum protease | MALDI-TOF-MS | Rat serum | in vitro | None | None | Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells. | |||
| 14640680 | 2003 | cycloCP-11 | 15 | Free | Amidation | Cyclic (C2-C14) | L | None | Analogue of indolicidin | Antibacterial | 0,5,10,20,40,60 minutes | 50 µg/mL peptide and 0.2 µg/mL trypsin in 100 mM Tris buffer | 18 | Trypsin | HPLC and MALDI-TOF | cycloCP-11 in presence of trypsin | in vitro | None | None | MIC for E.coli=16 µg/ml | |||
| 14640680 | 2003 | CP11 | 13 | Free | Amidation | Linear | L | None | Indolicidin analogue | Antibacterial | 0,5,10,20,40,60 minutes | 50 µg/mL peptide and 0.2 µg/mL trypsin in 100 mM Tris buffer | 4 | Trypsin | HPLC and MALDI-TOF | CP-11 in presence of trypsin | in vitro | None | None | MIC for E.coli=8 µg/ml | |||
| 12220890 | 2002 | Influenza hemagglutinin [(HA) 91 €“108] derivative | 18 | Acetylation | Amidation | Linear | L | None | Derivative of B-cell epitope hemagglutinin (HA) 91 €“108 from influenza | Modulate immune response | Not mentioned | 1 mg/ml | 2 | Mice lung homogenate proteases | RP-HPLC | BALB/c mice lung homogenate | in vitro | None | None | IFN-y production in presence of peptide was measured. Splenocyte was collected after 12 days of immunization, cultured in presence / absence of Inactivated virus(500 HAU/well). Level of IFN-y in presence of virus is ~2500 pg/ml as measured by ELISA. | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 21.2 ±1.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Thioridazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 19.6 ±1.0 | Human blood plasma proteases | TLC | Human plasma mixed with drug Fluphenazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 17.2 ±0.9 | Human blood plasma proteases | TLC | Human plasma mixed with drug AS-1397 | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 17.1 ±1.0 | Human blood plasma proteases | TLC | Human plasma mixed with drug Promethazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 17.1 ±1.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Chlorpromazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.5 ±0.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Methotrimeprazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.1 ±0.2 | Human blood plasma proteases | TLC | Human plasma mixed with drug Methotrimeprazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.9 ±0.2 | Human blood plasma proteases | TLC | Human plasma mixed with drug Prochlorperazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.4 ±0.3 | Human blood plasma proteases | TLC | Human plasma mixed with drug Trifluoperazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.4 ±0.3 | Human blood plasma proteases | TLC | Human plasma mixed with drug Molindone | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.4 ±0.4 | Human blood plasma proteases | TLC | Human plasma mixed with drug Loxapine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.1 ±0.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Clozapine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.9 ±0.3 | Human blood plasma proteases | TLC | Human plasma mixed with drug Haloperidol | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.9 ±0.4 | Human blood plasma proteases | TLC | Human plasma mixed with drug Sulpiride | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.3 ±0.4 | Human blood plasma proteases | TLC | Human plasma mixed with drug Thiothixene | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 31.3 ±0.7 | Human blood plasma proteases | TLC | Human plasma mixed with Bacitracin | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 41.1 ±0.9 | Human blood plasma proteases | TLC | Human plasma mixed with Bacitracin | in vitro | None | None | Not mentioned | |||
| 385880 | 1979 | 5-Fluoro-4-(N-succinamoylglycylglycine benzyl ester)-2(1H)-pyrimidone (compound 11) | 2 | 5-Fluoro-4-N-succinamoyl | Benzyl ester-2(1H)-pyrimidone | Linear | L | Conjugation of peptide C terminal carboxyl group with amino group of 5 Fluorocytosine | Synthetic | Anticandidal | Not given | Not mentioned | 0.3 | Sample cells proteases | Spectrophotometry | Sample cells | in vivo | None | None | 5-FC peptide were tested for antifungal activity agaainst S. cerevisiae, Candida albicans and candida. The MIC was 0.62,0.62 and 20 µg/mL respectively. | |||
| 641324 | 1983 | Peptide histidine isoleucine | 27 | Free | Free | Linear | L | None | Porcine intestine | Neurotransmitter | 1, 2, 3, 4, 5, 10 and 15 min. | 4.7 pmoles/kg | 3.1 ±0.5 | Human plasma proteases | Radioimmunoassay | Intravenous administration to human plasma | in vivo | None | None | PHI effect on secretion on gastrointestinal hormone and monitor its effect on gastric secretion of pepsin. PHI infused at 4.7pmoles/kg in human and gastric juice were aspirated by suction, gastric secretion was improved to be in case of PIH. | |||
| 3922013 | 1984 | Calcitonin gene related peptide | 37 | Free | Free | Linear | L | None | Human non-thyroidal tissue | Vasoactive neuropeptide | Not given | 0.32 pmol/kg | 6.9 ±0.9 (first phase) | Human blood plasma proteases | Radioimmunoassay | Intravenous injection into human | in vivo | http://physrev.physiology.org/content/94/4/1099 | None | CGRP infusion reduces gastric acid output as measured by plasma concentration of CGRP against time data obtained during infusion. | |||
| 3922013 | 1984 | Calcitonin gene related peptide | 37 | Free | Free | Linear | L | None | Human non-thyroidal tissue | Vasoactive neuropeptide | Not given | 2.56 pmol/kg | 26.4 ±4.7 (first phase) | Human blood plasma proteases | Radioimmunoassay | Intravenous injection into human | in vivo | http://physrev.physiology.org/content/94/4/1099 | None | CGRP infusion reduces gastric acid output as measured by plasma concentration of CGRP against time data obtained during infusion. | |||
| 4034413 | 1985 | Leucine enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Analgesic | 20 minutes | 0.9 nM | 14.7 | Human serum protease | HPLC | Human serum | in vitro | None | None | Not reported | |||
| 4070016 | 1985 | DTγE( Des-Tyr1-γ-Endorphin) (β-endorphin-(2-17)) | 16 | Free | Free | Linear | L | None | CNS and piyuitary gland of Humans | Neuropeptide, non-opioid y-type endorphins | Not given | 3.1-7.1 µg | 5.5 (elimination phase) | Rat blood proteases | RP-HPLC | Male wistar Rats (intravenously) | in vivo | None | None | Not reported | |||
| 6121002 | 1982 | PLG peptide | 3 | Free | Free | Linear | L | Tritium labeling at Proline | Hypothalamus and pineal gland | Interact with dopaminergic system and improve patients of parkinson disease | Not given | 2 - 2.5 μg | 20 (t1/2 elimination) | Rat plasma proteases | Radioimmunoassay | Subcutaneously injected to rat plasma | in vivo | None | None | Radiolabelled peptide was administered in rats and blood plasma was taken and analysed by HPLC. Brain level of radioactivity increased with time. | |||
| 6127205 | 1982 | Somatostatin 14 | 14 | Free | Free | Cyclic (C3-C14) | L | None | Ovine hypothalamus | Regulates the endocrine system and affects neurotransmission and cell proliferation | 30-45 minute | 10 µg | 1.7 ±0.2 | Dog blood proteases | SS Radioimmunoassay assay | Intravenous infusion in Dog plasma | in vivo | http://www.anaspec.com/products/product.asp?id=574 | None | Radiolabelled peptide was administered in rats and blood plasma was taken and analysed by HPLC. Brain level of radioactivity increased with time. | |||
| 6127205 | 1982 | Somatostatin 28 | 28 | Free | Free | Cyclic (C17-C28) | L | None | Ovine hypothalamus | Regulates the endocrine system and affects neurotransmission and cell proliferation | 30-45 minute | 20 µg | 2.8 ±0.3 | Dog blood plasma | SS Radioimmunoassay assay | Intravenous infusion in Dog plasma | in vivo | http://www.anaspec.com/products/product.asp?id=574 | None | When 50ng of SS14 was injected there is 85.1% decreasedportal venous blood flow was observed as compared to percentage of basal flow. | |||
| 6128770 | 1982 | Somatostatin 14 | 14 | Free | Free | Cyclic (C3-C14) | L | None | Ovine hypothalamus | Regulates the endocrine system and affects neurotransmission and cell proliferation | 1 hour | 1.7nmol | 2.4 | cat blood protease | Not mentioned | Intravenous infusion to cat plasma | in vivo | http://www.anaspec.com/products/product.asp?id=574 | None | When 100ng of SS28 is injected there is 73% decreased portal venous blood flow as compared to basal blood flow. | |||
| 6128770 | 1982 | Somatostatin 28 | 28 | Free | Free | Cyclic (C17-C28) | L | None | Ovine hypothalamus | Regulates the endocrine system and affects neurotransmission and cell proliferation | 1 hour | 4.8nmol | 6.1 | cat blood protease | Not mentioned | Intravenous infusion to cat plasma | in vivo | http://www.anaspec.com/products/product.asp?id=574 | None | Gastrin exocrine inhibitor assay were performed. 80 % gastric inhibition observed at 7ug/kg of peptide. | |||
| 6239307 | 1984 | Atrial Natriuretic peptide | 28 | Free | Free | Cyclic (C7-C23) | L | None | Human heart | Depressor and natriuretic activity | 2 hours | 1nmol | 30 | Rat blood proteases | RP-HPLC | Intravenous administered to Rat | in vivo | None | None | Gastric exocrine inhibitory assay was performed. 80 % inhibition observed at 8ug/kg body weight of peptide | |||
| 6239307 | 1984 | Atriopeptin 3 | 24 | Free | Free | Cyclic (C3-C19) | L | I125 radiolabeled | Human heart | Depressor and natriuretic activity | 2 hours | 1nmol | 2.5 | Rat blood proteases | RP-HPLC | Intravenous administered to Rat | in vivo | None | None | Time course depression is seen and Atropeptin 3 shows 2 time more depressor activity as compared to control alpha heart ANP. | |||
| 6291099 | 1982 | Cholecystokinin-4 (CCK4) | 4 | Free | Amidation | Linear | L | None | Deudenum of pig | Intestinal hormone | Not given | 50 µM | 13 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | Cholecystokinin-4 (CCK4) | 4 | Free | Amidation | Linear | L | None | Deudenum of pig | Intestinal hormone | Not given | 50 µM | <1 | Rat plasma protease | HPLC | Rat Plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK7 (Cholecystokinin-7) | 7 | Free | Amidation | Linear | L | None | Deudenum of pig | Intestinal hormone | Not given | 50 µM | 2.5 | Human blood proteases | HPLC | Human plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK8 (Cholecystokinin-8) | 8 | Free | Amidation | Linear | L | None | Deudenum of pig | Intestinal hormone | Not given | 50 µM | 18 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK8 (Cholecystokinin-8) | 8 | Free | Amidation | Linear | L | Sulphation of Tyrosine residue at position 2 | Derivative of natural cholecytokinin | Intestinal hormone | Not given | 50 µM | 50 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK8 (Cholecystokinin-8) | 8 | Free | Amidation | Linear | L | None | Deudenum of pig | Intestinal hormone | Not given | 50 µM | 5 | Rat plasma protease | HPLC | Rat Plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK8 (Cholecystokinin-8) | 8 | Free | Amidation | Linear | L | Sulphation of Tyrosine residue at position 2 | Derivative of natural cholecytokinin | Intestinal hormone | Not given | 50 µM | 17 | Rat plasma protease | HPLC | Rat Plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK9 (Cholecystokinin-9) | 9 | Free | Amidation | Linear | L | Sulphation of Tyrosine residue at position 3 | Derivative of natural cholecytokinin | Intestinal hormone | Not given | 50 µM | 2.7 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK10 (Cholecystokinin-10) | 10 | Free | Amidation | Linear | L | Sulphation of tyrosine residue at position 4 | Derivative of natural cholecytokinin | Intestinal hormone | Not given | 50 µM | 30 | Human blood proteases | HPLC | Human plasma | in vitro | None | None | Not reported | |||
| 6291099 | 1982 | CCK10 (Cholecystokinin-10) | 10 | Free | Amidation | Linear | L | Sulphation of tyrosine residue at position 4 | Derivative of natural cholecytokinin | Intestinal hormone | Not given | 50 µM | 45 | Rat plasma protease | HPLC | Rat Plasma | in vitro | None | None | Not reported | |||
| 6344071 | 1983 | E.Coli leader peptide of tryptophan operon | 14 | Free | Free | Linear | L | None | E.coli trp operon | Regulatory peptide | Not given | Not mentioned | 03-Apr | Cell-free (S-30) extracts prepared from E. coli strain W3110 trpR tnaA2 AtrpEA2 rna | Radioactivity decay assay (3H) .Leader peptide is radiolabelled and then decay in radioactivity is measured. | Not reported | in vitro | None | None | Not reported | |||
| 6522442 | 1984 | Dermorphin | 7 | Free | Free | Linear | L | I125 radiolabeled | Frog skin | Opiod receptor agonist | 60 minute | 500 μg/kg | 1.3 | Rat blood proteases | Radioimmunoassay and HPLC | Intravenous injection into tail of rats | in vivo | http://www.anaspec.com/products/product.asp?id=450 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 76 μg | 16.2 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 85 μg | 13.3 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 75 μg | 12.4 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 75 μg | 12.7 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 90 μg | 5.6 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 80 μg | 9.4 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 80 μg | 11.6 (mean t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 85 μg | 49.5 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 90 μg | 47.9 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6658706 | 1983 | 125I-labeled desamino-tyrosyl (DAT-FPA) FPA | 16 | Free | Free | Linear | L | DAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-T | Desaminotyrosine Fibrinopeptide derivative | Blood clotting | 6 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 min | Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA | 7 (radioactivity) | Normal rabbit blood proteases | Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma. | Intravenous injection in lateral vein of normal rabbit | in vivo | http://search.anaspec.com/?keywords=fibrinopeptide | None | Not reported | |||
| 6658706 | 1983 | 125I-labeled desamino-tyrosyl (DAT-FPA) FPA | 16 | Free | Free | Linear | L | DAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-T | Desaminotyrosine Fibrinopeptide derivative | Blood clotting | 7 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 min | Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA | 30 (radioactivity) | Normal rabbit blood proteases | Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma. | Intravenous injection in lateral vein of normal rabbit | in vivo | http://search.anaspec.com/?keywords=fibrinopeptide | None | Not reported | |||
| 6658706 | 1983 | Human Fibrinopeptide A (FPA) | 16 | Free | Free | Linear | L | None | N terminal end of the A-alpha chain of fibrinogen | Blood clotting | 10 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 min | Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA | 3.5 | Normal rabbit blood proteases | Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma. | Intravenous injection in lateral vein of normal rabbit | in vivo | None | None | Not reported | |||
| 6658706 | 1983 | Human Fibrinopeptide A (FPA) | 16 | Free | Free | Linear | L | None | N terminal end of the A-alpha chain of fibrinogen | Blood clotting | 11 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120,150,210 and 240 min | Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA | 15 | Normal rabbit blood proteases | Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma. | Intravenous injection in lateral vein of normal rabbit | in vivo | None | None | Not reported | |||
| 6658706 | 1983 | 125I-labeled desamino-tyrosyl (DAT-FPA) FPA | 16 | Free | Free | Linear | L | DAT-FPA was labeled with 125-iodine or with 123-iodine by chloramine-T | Desaminotyrosine Fibrinopeptide derivative | Blood clotting | 3 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120 min | Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA | 7 (radioactivity) | Nephrectomized rabbits blood proteases | Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma. | Intravenous injection in lateral vein of nephrectomized rabbits | in vivo | None | None | Not reported | |||
| 6658706 | 1983 | Human Fibrinopeptide A (FPA) | 16 | Free | Free | Linear | L | None | N terminal end of the A-alpha chain of fibrinogen | Blood clotting | 5 sec and at 10 sec intervals upto 2 mins, then after 6,10,20,30,40,60,90,120 min | Labeled 125-I-FPA (0.1 mCi) in 1 ml of 1 µg of FPA | 4 | Nephrectomized rabbits blood proteases | Gel filtration chromatography of blood plasma at different time interval show that rapid clearence of peptide from blood plasma. | Intravenous injection in lateral vein of nephrectomized rabbits | in vivo | http://search.anaspec.com/?keywords=fibrinopeptide | None | Not reported | |||
| 6736205 | 1984 | Gastrin releasing peptide | 27 | Free | Free | Linear | L | None | Porcine nonantral gastric juice | Stimulate release of gastrin | Not given | GRP I (0-30 min) bolus injection of 1.41 pmol kg-1, followed by an infusion of 0.12 pmol kg-1 x min- | 2.8 ±0.4 min | Human serum proteases | Radioimmunoassay | Human serum | in vivo | http://www.anaspec.com/products/product.asp?id=301 | None | Plasma gastrin concentration increased immediately after administration of peptide intravenously. After two doses of peptide(1.50pmol/kg) gastrin concentration found to be 1551pmol as compared to basal level of 370pmol. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-36)) | 36 | Free | Amidation | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 2.1 ±0.1 (for first phase) | Dog plasma proteases | Radioimmunoassay and HPLC | Intravenous injection to dogs plasma | in vitro | None | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-37)) | 37 | Free | Free | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 2.4 ±0.3 (for first phase) | Dog plasma proteases | Radioimmunoassay and HPLC | Intravenous injection to dogs plasma | in vitro | http://www.anaspec.com/products/product.asp?id=324 | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 15, 30, 45, and 60min | 0.10mg/kg | 1 (t1/2 α) | Rat blood plasma proteases | HPLC-MS | Intravenous administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min | 0.10mg/kg | 13 (t1/2 α) | Dog blood plasma proteases | HPLC-MS | Intravenous administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min | 0.10mg/kg | 4 (t1/2 α) | Rabbit blood plasma proteases | HPLC-MS | Intravenous administered to Rabbit | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 10, 30, 60, 90, 120, 180, 240, 300, 360, 480, and 1440min | 0.10mg/kg | 5 (t1/2 α) | Monkey blood plasma proteases | HPLC-MS | Intravenous administered to Monkey | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2, 5, 15, 30, 45, and 60min | 0.10mg/kg | 15 (t1/2 β) | Rat blood plasma proteases | HPLC-MS | Intravenous administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 2,5,10,20,30,45,60,90,120,180,240,300,360, 480,600, and 1440min | 5 mg/kg | 45 (t1/2 β) | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 5, 10, 20, 30, 45, 60, 90, 120, 150, and 180min | 5 mg/kg | 51 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 5 mg/kg | 51 | Rat blood plasma proteases | HPLC-MS | Orally administered to Rat | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 5 mg/kg | 45 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 5 mg/kg | 44 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 1 day | 50 mg/kg | 48 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 8991489 | 1996 | IRI-695 peptide | 3 | Acetylation | Isobutyl citrate | Linear | L | C14 Radiolabeling | Synthetic | Anxiolytic and antidepressant | 28 day | 50 mg/kg | 50 | Dog blood plasma proteases | HPLC-MS | Orally administered to Dog | in vivo | None | None | Not tested | |||
| 9062685 | 1997 | [pGIu4,Cyt6]AVP(4-9) | 6 | Free | Amidation | Linear | L | pGlu = pyroglutamate | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 10 ng/kg | 40 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs. | |||
| 9062685 | 1997 | [Cys6]AVP(5-8) | 4 | Free | Free | Linear | L | At 2 position cystine is replaced by cysteine | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 1 ng/kg | 10 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs. | |||
| 9062685 | 1997 | No.302 | 6 | Free | Amidation | Linear | L | pGlu = pyroglutamate | Human kidney cells | Antidiuretic hormone | 5, 10, 30, 60 and 120 min | 0.1, 1 and 10ng/kg | 9 | Rat blood proteases | HPLC | Subcutaneously injected to rat | in vivo | None | None | Passive avoidance test to check the learning behaviour and response latency is measured of movement from light compartement to dark compartement. The peptide decreased the latency period significantly and also effective at 100 fold lower cincentration than then other drugs. | |||
| 9357069 | 1997 | [D-Arg1,D-Phe5,D-Trp7,9,Leu11]Substance P | 11 | Free | Amidation | Linear | Mix | None | Substance P | Neuropeptide growth factor antagonist | upto 360 minutes | 12 µg/g body weight of mice | 45.9 (terminal t1/2) | Mice blood proteases | RP-HPLC | Intraperitonial injection to Nu/Nu mice | in vivo | http://www.abcam.com/d-arg1d-phe5d-trp79leu11-subs | None | Not reported | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 7.7 ±0.8 (t1/2 slow phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats treated with carvedilol | in vivo | None | None | ANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 4.9 ±0.5 (t1/2 slow phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats | in vivo | None | None | ANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group. | |||
| 10354413 | 1999 | Thioimreg compound 11 | 3 | Free | Free | Linear | L | Peptide bonds at position 1,2 was replaced by thioamide linkages | Thioanalogue of natural Imreg | Immunostimulant | 3.5 hours | Not given | 46 | Rat blood proteases | HPLC | Rat whole blood | in vitro | None | None | 125 mg/kg of 11 resulted in a significant increase in activated T helper cells (CD4+CD45+, 28%, P e 0.048). This is accompanied by a significant reduction in NK cells (20-27%, P e 0.02) at 50 and 100 mg/kg | |||
| 10354413 | 1999 | Imreg | 3 | Free | Free | Linear | L | None | Human leucocyte | Immunostimulant and in clinical trial to treat AIDS | 3.5 hours | Not given | <1 | Rat blood proteases | HPLC | Rat whole blood | in vitro | None | None | Immunophenotyping assay is performed to study immunological effect like stimulation of NK cells and lymphoproliferative properties. T cell proliferation was observed at even at 100mg/kg | |||
| 10573295 | 1999 | Enkephalin | 6 | Free | Amidation | Linear | L | None | Natural (Human brain) | Analgesic | 0, 60, 120, 180, and 300 min | 1mM | 30 | Mouse plasma proteases | HPLC , reverse phase HPLC, Partition coefficient | Mouse plasma | in vitro | None | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling and encapsulation of VIP in Liposome | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 5.29 ±0.62 (t1/2 elimination) | Rat plasma proteases | Not mentioned | Intravenously administration to rat plasma | in vivo | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling and encapsulation of VIP in Liposome | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 9.28 ±0.76 (t1/2 elimination) | Rat lung proteases | Not mentioned | Intravenously administration to rat lung | in vitro | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 3.18 ±0.22 (t1/2 elimination) | Rat lung proteases | Not mentioned | Intravenously administration to rat lung | in vitro | PMID 5450698 | None | Not tested | |||
| 10973845 | 2000 | Alpha 2-antiplasmin (α2AP ) | 24 | Free | Free | Linear | L | I125 radiolabeling | Human SERPINF2 gene | Clotting factor | 2 hours | 2 mg/ml | 19 | Mouse blood proteases | Not mentioned | Mouse blood fibrin clots | in vitro | None | None | Immunoblotting assay was done by taking 50 µL of fibrin clots with 2mg/ml of alpha2 AP and alpha2 AP peptide and cross linking was determined by electroblotting to PVDF membrane and detected by streptavidin-peroxidase. | |||
| 10973845 | 2000 | Alpha 2-antiplasmin peptide (α2AP13-24 ) | 12 | Free | Free | Linear | L | Biotinylation at lysine residue(position 24) | Human SERPINF2 gene | Clotting factor | 2 hours | 0.5mMol/L | 21 | Mouse blood proteases | Not mentioned | Mouse blood fibrin clots | in vitro | None | None | Immunoblotting assay was done by taking 50 µL of fibrin clots with 2mg/ml of alpha2 AP and alpha2 AP peptide and cross linking was determined by electroblotting to PVDF membrane and detected by streptavidin-peroxidase. | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.033 ±0.004 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.064 ±0.052 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.971 ±0.336 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.032 ±0.005 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.321 ±0.0.091 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 4572061 | 1972 | Luteinizing Hormone Releasing Hormone(LHRH) | 10 | Free | Amidation | Linear | L | pGlu=pyroglutamic acid, Tritium labeling | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 2 minutes | 1 .0 μCi | 6.97 ±0.4 | Female Sprague Dawley rats blood protease | Radioimmunoassay | Intarvenous administration to Female Sprague Dawley rats | in vivo | None | None | LH-RH acts on the anterior pituitary to evoke the release of LH | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 10 μg/kg | 5.9 ±2.5 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Intravenous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 1 μg/kg | 6.6 ±2.7 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 10 μg/kg | 5.3 ±1.1 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 9040091 | 1997 | Meterelin | 9 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid | Gonadotropic cells in the anterior pituitary gland | Behavior influencing hormones | 5, 1, 3, 5, 7, 10, 15, 20, 30, 45, 60, 75, and 90 min, then every 30 min until 3 h postinjection, an | 100 μg/kg | 7.8 ±2.0 (t1/2 α) | New Zeland female rabbits blood protease | Radioimmunoassay | Subcutaneous injected in New Zeland female rabbits | in vivo | None | None | Castrate levels of testosterone were attained 10 days after sc administration of the implant, lasted for up to 247 days | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 8 | Rat Stomach luminal flushing proteases | TCA precipitation | Rat Stomach luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 5 | Rat Stomach luminal flushing proteases | Antibody assay | Rat Stomach luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 2.5 | Rat Stomach luminal flushing proteases | Receptor-precipitable radioactivity | Rat Stomach luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | TCA precipitation | Rat Duodenum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | Antibody assay | Rat Duodenum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | Receptor-precipitable radioactivity | Rat Duodenum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | TCA precipitation | Rat Ileum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | Antibody assay | Rat Ileum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | Receptor-precipitable radioactivity | Rat Ileum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 38 | Rat Colon luminal flushing proteases | TCA precipitation | Rat Colon luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 33 | Rat Colon luminal flushing proteases | Antibody assay | Rat Colon luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 16 | Rat Colon luminal flushing proteases | Receptor-precipitable radioactivity | Rat Colon luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 50 | Rat Stomach luminal flushing proteases | TCA precipitation | Rat Stomach luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | TCA precipitation | Rat Duodenum luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | TCA precipitation | Rat Ileum luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 60 | Rat Colon luminal flushing proteases | TCA precipitation | Rat Colon luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7529108 | 1994 | Human endothelin-1 (Human ET-1) | 21 | Free | Free | Linear | L | None | Human Endothelin-1 | Vasoconstricting peptide | 180 minute | 3 nmol of peptide with 200 ng of enzyme | 37 (t1/2 of hydrolysis) | Endopeptidase-24.11(E-24.11) | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | C-terminal fragment of Human Endothelin-1 (CTF) | 17 | Free | Free | Linear | L | None | Human Endothelin-1 | Vasoconstricting peptide | 180 minute | 3 nmol of peptide with 200 ng of enzyme | 57 (t1/2 of hydrolysis) | Endopeptidase-24.11(E-24.11) | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | Porcine big endothelin-1 (Porcine big-ET-1) | 39 | Free | Free | Linear | L | None | Porcine Endothelin-1 | Vasoconstricting peptide | 80 minute | 3 nmol of peptide with 50 ng of enzyme | 25 (t1/2 of hydrolysis) | Thermolysin | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | Porcine endothelin-1 (Porcine ET-1) | 21 | Free | Free | Linear | L | None | Porcine Endothelin-1 | Vasoconstricting peptide | 80 minute | 3 nmol of peptide with 50 ng of enzyme | 56 (t1/2 of hydrolysis) | Thermolysin | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | C-terminal fragment of Porcine Endothelin-1 (Porcine CTF) | 18 | Free | Free | Linear | L | None | Porcine Endothelin-1 | Vasoconstricting peptide | 80 minute | 3 nmol of peptide with 50 ng of enzyme | 47 (t1/2 of hydrolysis) | Thermolysin | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | Substance P | 11 | Free | Free | Linear | L | None | Spinal cord | Vasoconstricting peptide | 180 minute | 3 nmol of peptide with 200 ng of enzyme | 2.1 (t1/2 of hydrolysis) | Endopeptidase-24.11(E-24.11) | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | None | None | Not reported | |||
| 7689499 | 1993 | Galanin | 30 | Free | Free | Linear | L | None | Human tissue | Neuropeptide | 60 minutes | 74 pmol/kg | 3.7 ±0.4 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | 1370155 | None | Growth hormone concentrations increased markedly during galanin infusion reaching a plateau value eight times the pre-infusion concentrations after 40-min infusion p < 0.01 | |||
| 7714746 | 1994 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Opoid | Nociception regulating peptide | Not mentioned | 0.10mM, 10 mL | 17.7 | Aminopeptidases present in nasal mucosa of rat | HPLC | Nasal administration to Male Sprague Dawley derived rats | in vivo | None | None | Not reported | |||
| 7714746 | 1994 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Opoid | Nociception regulating peptide | Not mentioned | 0.10mM, 10 mL | 23.9 | Aminopeptidases present in nasal mucosa of rat | HPLC | Nasal administration to Male Sprague Dawley derived rats | in vivo | None | None | Not reported | |||
| 7714746 | 1994 | Leu-enkephalin analogue | 5 | Free | Free | Linear | L | None | Opoid | Nociception regulating peptide | Not mentioned | 0.10mM, 10 mL | 21.2 | Aminopeptidases present in nasal mucosa of rat | HPLC | Nasal administration to Male Sprague Dawley derived rats | in vivo | None | None | Not reported | |||
| 7957536 | 1994 | Hexarelin | 6 | Free | Amidation | Linear | Mix | Trp methylated at position 2 | Growth hormone-releasing hormone-6 | Growth hormone-releasing peptide | 24 hours | 0.5 μg/kg | 50 | Human serum proteases | Chemiluminescence immunometric assay | Twelve adult male volunteers | in vivo | None | None | Mean ED50 values were 0.50 μg/kg and Emax values were 55.1 μg/kg | |||
| 7957536 | 1994 | Hexarelin | 6 | Free | Amidation | Linear | Mix | Trp methylated at position 2 | Growth hormone-releasing hormone-6 | Growth hormone-releasing peptide | 24 hours | 1 μg/kg | 51 | Human serum proteases | Chemiluminescence immunometric assay | Twelve adult male volunteers | in vivo | None | None | Mean ED50 values were 0.50 μg/kg and Emax values were 55.1 μg/kg | |||
| 7957536 | 1994 | Hexarelin | 6 | Free | Amidation | Linear | Mix | Trp methylated at position 2 | Growth hormone-releasing hormone-6 | Growth hormone-releasing peptide | 24 hours | 2 μg/kg | 58 | Human serum proteases | Chemiluminescence immunometric assay | Twelve adult male volunteers | in vivo | None | None | Mean ED50 values were 0.50 μg/kg and Emax values were 55.1 μg/kg | |||
| 7991443 | 1994 | C-20 Sorbin | 20 | Free | Amidation | Linear | L | None | Derived from Sorbin | Electrolyte absorbing peptide | 1, 2, 4, 8, 16, and 32 min | 200 μg/kg/h | 9.5 ±1.8 | Rat blood proteases | Radioimmunoassay | Male Sprague-Dawley rats blood | in vivo | None | None | Increases absorption of water and ions | |||
| 7991443 | 1994 | C-7 Sorbin | 7 | Free | Amidation | Linear | L | None | Derived from Sorbin | Electrolyte absorbing peptide | 1, 2, 4, 8, 16, and 32 min | 200 μg/kg/h | 7.5 ±1.5 | Rat blood proteases | Radioimmunoassay | Male Sprague-Dawley rats blood | in vivo | None | None | Increases absorption of water and ions | |||
| 7991443 | 1994 | Tritiated C-7 Sorbin | 7 | Free | Amidation | Linear | L | [2-dehydro-Pro1.5]C is attached and tritiated | Derived from Sorbin | Electrolyte absorbing peptide | 1, 2, 4, 8, 16, 32, and 64 min | 2.8 MBq | 17.9 ±1.5 | Rat blood proteases | Radioimmunoassay | Male Sprague-Dawley rats blood | in vivo | None | None | Increases absorption of water and ions | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 32 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 20.7 (slow component) | None | Not mentioned | None | in vitro | 2136732 | None | Not reported | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 32 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 3.9 (fast component) | None | Not mentioned | None | in vitro | 2136732 | None | Not reported | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 28 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 13.3 (slow component) | None | Not mentioned | None | in vitro | 6223192 | None | Not reported | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 28 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 1.7 (fast component) | None | Not mentioned | None | in vitro | 6223192 | None | Not reported | |||
| 8082705 | 1994 | Facteur thymique serique | 9 | Free | Free | Linear | L | None | Thymic peptide hormone | Thymic hormone used to treat autoimmune disorder | 5 minutes | 300-500 kBq/kg | 02-Mar | Rats blood proteases | Radioimmunoassay | Intravenouly injected in male Wistar rats | in vivo | 7011613 | None | The basal IRI level at 24 h after alloxan injection was significantly lower in alloxan-treated samples than in controls (12.1 + 5.2 vs. 28.7 + 6.3/zU/ml, P < 0.05) | |||
| 8194082 | 1993 | Epidermal Growth Factor (EGF) | 53 | Free | Free | Linear | L | I125 labeling | Epidermal Growth Factor | Growth factor | 135 minutes | 1420 Ci/mmol | 12.4 (dissociation t1/2) | Proteases present in human meningioma | Autoradiography | Fresh surgically excised human meningioma specimens | in vitro | 4636327 | None | High concentrations (10-4-10 -2 M) of suramin inhibited 125I-EGF binding to meningioma sections with ICs0's of 3.2 + 0.4 × 1 0 - 4 M | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 50 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 1.05 ±0.04 | Rat blood proteases | Radioimmunoassay | Spontaneously hypertensive rats (SHR) | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg. | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 51 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 1.19 ±0.09 | Rat blood proteases | Radioimmunoassay | Wistar-Kyoto rats | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were - 12.4, -46.6, -61.6 mmHg. | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 52 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 18.1 ±1.4 | Rat blood proteases | Radioimmunoassay | Spontaneously hypertensive rats (SHR) | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg. | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 53 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 16.3 ±1.2 | Rat blood proteases | Radioimmunoassay | Wistar-Kyoto rats | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were - 12.4, -46.6, -61.6 mmHg. | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-1 | 17 | Free | Free | Linear | L | None | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 42 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-3 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 3-4 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 43 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545255 | 1995 | Hexarelin | 6 | Free | Free | Linear | Mix | Methylated at position 2 of D-trp | Growth hormone-releasing hormone-6 | Growth hormone-releasing peptide | 1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose. | 1 μg/kg | 25 ±5.02 | Dog blood proteases | Radioimmunoassay | Subcutaneous injection to male and female dogs | in vivo | None | None | Not reported | |||
| 8545255 | 1995 | Hexarelin | 6 | Free | Free | Linear | Mix | Methylated at position 2 of D-trp | Growth hormone-releasing hormone-6 | Growth hormone-releasing peptide | 1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose. | 10 μg/kg | 33.3 ±8.83 | Dog blood proteases | Radioimmunoassay | Subcutaneous injection to male and female dogs | in vivo | None | None | Not reported | |||
| 8545255 | 1995 | Hexarelin | 6 | Free | Free | Linear | Mix | Methylated at position 2 of D-trp | Growth hormone-releasing hormone-6 | Growth hormone-releasing peptide | 1, 3, 5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 120, 150, 180, 240, 300, 360, and 420 min postdose. | 100 μg/kg | 36.7 ±12.01 | Dog blood proteases | Radioimmunoassay | Subcutaneous injection to male and female dogs | in vivo | None | None | Not reported | |||
| 9234336 | 1993 | Vasoactive intestinal peptide (VIP) | 28 | Free | Free | Linear | L | None | Small intestinal mucosa | Vasoactive peptide | 2,3,6,10,20,40,60 minutes | 250 μg | 2.3 ±0.8 | Rat blood proteases | Radioimmunoassay | Intravenous injection to Rat blood | in vivo | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Regulate of blood flow and smooth muscle relaxation in specific mammalian organs | |||
| 12852770 | 2003 | Neurotensin | 13 | Free | Free | Linear | L | Post translationaly modified Glu residue at first position | Bovine hypothalamus | Neuromodulator peptide | 24 hour | 50 μg/well | 1.5 | Mice blood proteases | HPLC | NTR-positive HT29 tumor- bearing SCID mice | in vivo | None | None | IC50 value reported was 0.2 nM | |||
| 15740458 | 2005 | Rat AM (Adrenomedullin) | 50 | Free | Free | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 200 μl | 2 (distribution t1/2) | Rat blood proteases | Competitive Radioimmunoassay | Intravenous administration in Rat | in vivo | http://www.anaspec.com/products/product.asp?id=304 | None | Not reported | |||
| 15740458 | 2005 | Rat AM (Adrenomedullin) | 50 | Free | Free | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 200 μl | 15.9 (elimination t1/2) | Rat blood proteases | Competitive Radioimmunoassay | Intravenous administration in Rat | in vivo | http://www.anaspec.com/products/product.asp?id=304 | None | Not reported | |||
| 16302271 | 2006 | Human Glandular Kallikrein 2 (hK2)-activated thapsigargin prodrug | 6 | Acetylation | Free | Linear | L | Ligated with potent cytotoxin thapsigargin, L12ADT | Human glandular kallikrein 2 (hK2) | Antitumor peptide | 24 hours | 6 mg/kg | 40 | Mice blood proteases | Not mentioned | Balb-C mice | in vivo | None | None | Intratumoral concentrations reached levels comparable to the in vitro IC50 of the prodrug with concentrations of 1.25 mM seen at 1 and 4 hr. | |||
| 17065394 | 2006 | Porcine PYY (Peptide YY) | 34 | Free | Amidation | Linear | L | None | Porcine intestine | Neuropeptide | 120 minutes | 25 mg/kg BW per min | 15 | Pigs blood proteases | Double-antibody Radioimmunoassay | Intravenously administred to Crossbred (Large White!Landrace!Duroc) castrated male pigs | in vivo | http://www.genscript.com/peptide/RP10354-Peptide_Y | None | Plasma GH levels significantly increased 30 min after PYY3 €“36 injection compared with the saline-injected group (7.8 ± 2.1 vs 3.0 ± 0.6 ng/ml, P<0.05) | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 15 mg/kg | 0.40 ±0.05 (t1/2 α) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 30 mg/kg | 0.63 ±0.02 (t1/2 α) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 8388403 | 1993 | ANP (Atrial natriuretic Peptide) | 28 | Free | Free | Linear | L | None | Human Heart | Diuretic,natriuretic and vasodilatory peptide | 2 hours | 1.5 pmol/lg/min | 4.1 ±0.4 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No significant differences in systolic blood pressure, diastolic blood pressure or pulse rate were observed when values on active and placebo infusions were compared (P = 0.85) | |||
| 3871610 | 1985 | Rat α1- proteinase inhibitor | 60 | Free | Free | Linear | L | None | Rat serum | Protelytic activities regulating peptide | 5 minutes, 30 minutes, 1 hour, 4 hour and 7 hour | Not mentioned | 30 (for unglycosylated α1- proteinase inhibitor) | Rat serum proteases | Radioimmunoassay | Wistar rats | in vivo | http://www.uniprot.org/uniprot/Q9JMK6 | None | Protect tissue against proteolytic attack by leukocyte elastase | |||
| 6433008 | 1984 | TAP-144 | 10 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid, des-Gly | LHRH derivative | Gonadotrophins secreting hormone | 10 days | 10μg/100g body wt | 32 (t1/2 terminal phase) | Rat serum proteases | Not mentioned | Subcutaneous administration to Sprague-Dawley rats | in vivo | None | None | Serum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration | |||
| 6433008 | 1984 | TAP-144 | 10 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid, des-Gly | LHRH derivative | Gonadotrophins secreting hormone | 10 days | 100μg/100g body wt | 55.5 (t1/2 terminal phase) | Rat serum proteases | Not mentioned | Rectal administration to Sprague-Dawley rats | in vivo | None | None | Serum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration | |||
| 6433008 | 1984 | TAP-144 | 10 | Free | Ethylamide | Linear | Mix | pGlu=pyroglutamic acid, des-Gly | LHRH derivative | Gonadotrophins secreting hormone | 10 days | 100μg/100g body wt | 43.7 (t1/2 terminal phase) | Rat serum proteases | Not mentioned | Nasal administration to Sprague-Dawley rats | in vivo | None | None | Serum LH and FSH concentrations declined to about the same low level by 8 h after the TAP- 144 administration | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 3.2 ±0.1 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 4.9 ±0.02 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 2.8 ±0.1 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 4.6 ±0.5 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid. | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | 2U | 7.32 (steriodigenic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Shows activity of 80~180USP Units/mg | |||
| 4327730 | 1971 | ACTH analogue- 3 | 18 | Free | Amidation | Linear | L | None | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | 5 μg | 2.6 (steriodigenic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | No odification in the activity of ACTH analog-2 peptide | |||
| 4327730 | 1971 | ACTH analogue- 4 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 7.32 (steriodigenic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Showed higher potencies than Native ACTH in all the method tested | |||
| 4327730 | 1971 | ACTH analogue- 5 | 18 | Free | Amidation | Linear | L | Ibu = α-aminoisobutyric acid | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 9.6 (steriodigenic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | The intravenous and intramuscular potencies of peptide V, Ibu1 ACTH (1-18) amide were 480-757U/mg, 4-5 times higher than the values for native hormone but subcutaneous potency was rather low (264U/mg) and in vitro potency was much lower (83U/mg) than the intravenous and intramuscular potencies. | |||
| 4327730 | 1971 | ACTH analogue- 6 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine, Orn = Ornithine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 10.06 (steriodigenic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Showed an activity about 2/3 of that of the original Lys15 peptides IV | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 4.43 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Shows activity of 80~180USP Units/mg | |||
| 4327730 | 1971 | ACTH analogue- 3 | 18 | Free | Amidation | Linear | L | None | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 1.95 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Shows activity less than ACTH | |||
| 4327730 | 1971 | ACTH analogue- 4 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 3.08 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Shows activity less than ACTH | |||
| 4327730 | 1971 | ACTH analogue- 5 | 18 | Free | Amidation | Linear | L | Ibu = α-aminoisobutyric acid | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 3.32 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Shows activity less than ACTH | |||
| 4327730 | 1971 | ACTH analogue- 6 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine, Orn = Ornithine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 4.53 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Shows activity less than ACTH | |||
| 4327730 | 1971 | ACTH analogue- 7 | 18 | Free | Amidation | Linear | L | Ibu = α-aminoisobutyric acid | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 6 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | 4286483 | None | Shows activity more than ACTH | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1,2,3 and 4 hours | 200 mU | 59.22 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Not mentionedtive ACTH shows similar activity to rat and rabbit fats when compared in terms of the minimal effective dose (rat = 6*10-6mg/50mg tissue and rabbit = 5*10-6mg/50mg tissue) | |||
| 4327730 | 1971 | ACTH analogue- 3 | 18 | Free | Amidation | Linear | L | None | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 30 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | 4286483 | None | Showed much higher activity in rabbit fat than in rat fat (rat = 6*10-6mg/50mg tissue and rabbit = 0.4*10-6mg/50mg tissue) | |||
| 4327730 | 1971 | ACTH analogue- 4 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | 20 μg | 35.4 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | 4286483 | None | Showed much higher activity in rabbit fat than in rat fat (rat = 0.6*10-6mg/50mg tissue and rabbit = 0.07*10-6mg/50mg tissue) | |||
| 4327730 | 1971 | ACTH analogue- 5 | 18 | Free | Amidation | Linear | L | Ibu = α-aminoisobutyric acid | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | 20 μg | 32.43 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | 4286483 | None | Showed much higher activity in rabbit fat than in rat fat (rat = 0.2*10-6mg/50mg tissue and rabbit = 0.002*10-6mg/50mg tissue) | |||
| 4327730 | 1971 | ACTH analogue- 3 | 18 | Free | Amidation | Linear | L | None | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 42.6 (lipolytic activity t1/2) | Rat muscle proteases | Not mentioned | Rat muscle slices | in vitro | 4286483 | None | Showed much higher activity in rabbit fat than in rat fat (rat = 6*10-6mg/50mg tissue and rabbit = 0.4*10-6mg/50mg tissue) | |||
| 17283237 | 2007 | Glucagon like peptide-1 (GLP-1) | 37 | Free | Free | Linear | L | None | Human GLP-1 | Growth Hormone | 3 hours | 100 μg/kg peptide in mice | <5 | Mice blood proteases | Radioimmunoassay | Subcutaneously injected in mice | in vivo | http://www.uniprot.org/blast/?about=P01275[92-128] | None | Promotes glucose-depen- dent insulin secretion from the pancreas | |||
| 8218482 | 1993 | RGD containing peptide | 5 | Free | Free | Linear | L | I125 radiolabeling, covalently attached to an isocyanate-containing poly urethane prepolymer | Extra Cellular Matrix proteins | Antitumor peptide | Not mentioned | 0.2 mL | 0.5 (t1/2 first phase) | Mice blood proteases | Radioimmunoassay | Intravenously injected to C57BL6 mice | in vivo | None | None | Less effective in in blocking peptide-mediated attachment of B16-FlO melanoma cells to a surface. | |||
| 17258819 | 2007 | Vasopressin, 8-L-Arginine | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min | 15 μCi (555 kBq) | 1.06 ±0.19 (fast phase) | Rat blood proteases | Radioimmunoassay | Female homozygous Brattleboro rats and male Wistar rats | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antidiuretic activity 408 IU/mg | |||
| 17258819 | 2007 | Vasopressin, 8-L-Arginine | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min | 15 μCi (555 kBq) | 5.96 ±0.58 (slow phase) | Rat blood proteases | Radioimmunoassay | Female homozygous Brattleboro rats and male Wistar rats | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antidiuretic activity 408 IU/mg | |||
| 17258819 | 2007 | Vasopressin, 8-L-Arginine | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min | 15 μCi (555 kBq) | 1.00 ±0.15 (fast phase) | Rat blood proteases | Radioimmunoassay | Female homozygous Brattleboro rats and male Wistar rats along with OPC-31260 | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antidiuretic activity 408 IU/mg | |||
| 17258819 | 2007 | Vasopressin, 8-L-Arginine | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 20, 40 seconds and1, 2, 4, 8, 16, 32 and 60 min | 15 μCi (555 kBq) | 8.90 ±0.37 (slow phase) | Rat blood proteases | Radioimmunoassay | Female homozygous Brattleboro rats and male Wistar rats along with OPC-31261 | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antidiuretic activity 408 IU/mg | |||
| 17684103 | 2007 | 125I-vasopressin | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 1,2 and 3 minutes | 50 or 0.4 pmol of vasopressin with 33 kBq | ~ 1.5 | Mice blood proteases | Radioimmunoassay | Saline treated IRAP+/+ mice | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antiduretic activity | |||
| 17684103 | 2007 | 125I-vasopressin | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 1,2 and 3 minutes | 50 or 0.4 pmol of vasopressin with 33 kBq | 1 | Mice blood proteases | Radioimmunoassay | Insulin-treated IRAP+/+ mice | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antiduretic activity | |||
| 17684103 | 2007 | 125I-vasopressin | 9 | Free | Free | Cyclic (C1-C6) | L | I125 labeling | Human Vasopressin | Anti-diuretic peptide | 1,2 and 3 minutes | 50 or 0.4 pmol of vasopressin with 33 kBq | 3 | Mice blood proteases | Radioimmunoassay | Insulin-treated IRAP-/- mice. | in vivo | http://www.polypeptide.com/vasopressin-8-l-arginin | None | antiduretic activity | |||
| 15828822 | 2005 | Peptide1 | 7 | Acetylation | N-Ethylmaleimidation | Linear | Mix | None | Second type 1 repeat of thrombospondin-1 | Antiangiogenic activity | Not mentioned | 5mg/kg | <1 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = >100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.2 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.5 | Monkey plasma proteases | Not mentioned | Monkey plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.5 | Proteases from dog plasma | Not mentioned | Dog plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.2 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.15 | Mouse plasma proteases | Not mentioned | Mouse plamsa | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.8 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compund 4 | 8 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine, Nva-Norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.3 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.07 ± 0.004 nM, | |||
| 15828822 | 2005 | Compound 7 | 9 | NHIsp | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , Nva-Norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.9 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =29 ± 0.003 nM, Inhibition of HMVEC tube formation with IC50 = >1000nM | |||
| 15828822 | 2005 | Compound 8 | 9 | Succinylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine ,Nva-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.2 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.26 ± 0.110 nM, Inhibition of HMVEC tube formation with IC50 = 10-5nM | |||
| 15828822 | 2005 | Compound 9 | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , NMeNva- N-methyl-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 1 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.54 ± 0.150 nM, Inhibition of HMVEC tube formation with IC50 = 50-25nM | |||
| 15828822 | 2005 | Compound 11 | 9 | Succinylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , NMeNva- N-methyl-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.3 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.06 ± 0.030 nM, Inhibition of HMVEC tube formation with IC50 = 0.25- 0.10nM | |||
| 17408666 | 2007 | Cydiastatin 4 | 8 | Free | Amidation | Linear | L | None | Synthetic | Neuropeptides | 30 °C for 20 minutes | 1nmol | 16.5 | M. sexta larval midgut tissue proteases | RP-HPLC | Midgut tissues of M. sexta | in vitro | None | None | Not reported | |||
| 17408666 | 2007 | Cydiastatin 5 | 8 | Free | Amidation | Linear | L | None | Synthetic | Neuropeptides | 30 °C for 20 minutes | 1nmol | 2.5 | M. sexta larval midgut lumen proteases | RP-HPLC | Midgut Lumen of M. sexta | in vitro | None | None | Not reported | |||
| 17408666 | 2007 | Cydiastatin 4-alpha | 13 | Free | Amidation | Linear | L | None | Synthetic | Neuropeptides | 30 °C for 20 minutes | 1nmol | 4.5 | M. sexta larval midgut lumen proteases | RP-HPLC | Midgut lumen of M. sexta | in vitro | None | None | Not reported | |||
| 17408666 | 2007 | Cydiastatin 4-alpha | 13 | Free | Amidation | Linear | L | None | Synthetic | Neuropeptides | 31 °C for 20 minutes | 1nmol | 52 | M. sexta haemolymph proteases | RP-HPLC | Haemolymph of M. sexta | in vitro | None | None | Not reported | |||
| 17408666 | 2007 | Cydiastatin 4-alpha | 12 | Free | Amidation | Linear | L | Acpc=cyclopropylalanine | Synthetic | Neuropeptides | 30 °C for 20 minutes | 1nmol | 7.5 | M. sexta larval midgut lumen proteases | RP-HPLC | Midgut lumen | in vitro | None | None | Not reported | |||
| 17498958 | 2007 | Thyrotropin-releasing hormone (TRH) | 3 | Free | Amidation | Linear | L | Pyr=pyroglutamic acid | Hypothalamus | Stimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland | 37 °C for 1-120 minutes | 200μM | ~3 | Homogenate of Caco-2 cells proteases | LC-MS | Homogenate of Caco-2 cells | in vitro | None | None | Not reported | |||
| 17498958 | 2007 | Peptide1 (Thyrotropin-releasing hormone (TRH) analogue) | 3 | Free | D-glucopyranuronamide | Linear | L | Pyr=pyroglutamic acid | Synthetic derived from TRH | Stimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland | 37 °C for 1-120 minutes | 200μM | ~20 | Homogenate of Caco-2 cells proteases | LC-MS | Homogenate of Caco-2 cells | in vitro | None | None | Not reported | |||
| 17498958 | 2007 | Peptide2 (Thyrotropin-releasing hormone (TRH) analogue) | 3 | 2-aminooctanoic acid | D-glucopyranuronamide | Linear | L | None | Synthetic derived from TRH | Stimulates the release TSH(thyroid-stimulating hormone) by pitutiary gland | 37 °C for 1-120 minutes | 200μM | ~20 | Homogenate of Caco-2 cells proteases | LC-MS | Homogenate of Caco-2 cells | in vitro | None | None | Not reported | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 3.2mg/kg | 8.15 ±1.97 ( alpha or distribution half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 6.4mg/kg | 9.69 ±1.5 ( alpha or distribution half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 12.8mg/kg | 8.56 ±2.01 ( alpha or distribution half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 3.2mg/kg | 24.74 ±8.30 ( beta or elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 6.4mg/kg | 27.38 ±11.52 ( beta or elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 12.8mg/kg | 30.49 ±10.24 ( beta or elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 3.2mg/kg | 1.45 ±0.53(gamma or termination elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 6.4mg/kg | 1.30 ±0.27 (gamma or termination elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 12.8mg/kg | 1.24 ±0.44 (gamma or termination elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 17532097 | 2007 | N/OFQ (Nociceptin/Orphanin FQ peptide receptor) | 17 | Free | Free | Linear | L | None | Derived from the prepronociceptin protein | NOP-Receptor ligands | 37 °C for 240 min | 6 μg/μl | 3.2 ±1.8 | Mouse brain homogenate proteases | RP-HPLC | Mouse brain homogenate | in vitro | None | None | Hypotensive and bradycardic effects evoked by N/OFQ after i.v. administration in rats, was lasting (about 10 min) | |||
| 17532097 | 2007 | UFP-112 (Nociceptin/Orphanin FQ receptor antagonist) | 17 | Free | Amidation | Linear | L | (pF)F = p-flouro Phenylalanine; Aib= 2-Aminoisobutyric acid | Synthetic | NOP-Receptor ligands | 37 °C for 240 min | 6 μg/μl | 11.3 ±1.4 | Mouse brain homogenate proteases | RP-HPLC | Mouse brain homogenate | in vitro | 20497197 | None | Hypotensive and bradycardic effects evoked by UFP-112 after i.v. administration in rats wast lasting for (i.e. 80 min | |||
| 18697865 | 2008 | Ghrelin | 28 | Free | Free | Linear | L | n-octanoyl group at ser 3 | Secreted by stomach P/D1-type cells | Stimulates apetite and GH secretion | Blood collected after 20 minutes to 2200 h after i/v injection of peptide | 1 µg/kg i/v injected | 21 ±3.0 | Human plasma proteases | Competitive Radioimmunoassay | Human plasma | in vivo | 15788704 | None | Not reported | |||
| 18697865 | 2008 | Ghrelin | 28 | Free | Free | Linear | L | n-octanoyl group at ser 3 | Secreted by stomach P/D1-type cells | Stimulates apetite and GH secretion | Blood collected after 20 minutes to 2200 h after i/v injection of peptide | 3 µg/kg i/v injected | 45 | Human plasma proteases | Competitive Radioimmunoassay | Human plasma | in vivo | 15788704 | None | Not reported | |||
| 18972837 | 2008 | sCT (Salmon calcitonin) | 32 | Free | Free | Cyclic (C1-C7) | L | None | Hormone secreted by the parafollicular cells of thethyroid gland | Calcitropic Hormone, reduce blood calcium | 5-360minutes | 10 µM | 13.18 | Rat kidney homogenates proteases | LC-ESI-MS | Rat kidney homogenates | in vitro | None | None | Not reported | |||
| 18972837 | 2008 | sCT (Salmon calcitonin) | 32 | Free | Free | Cyclic (C1-C7) | L | None | Hormone secreted by the parafollicular cells of thethyroid gland | Calcitropic Hormone, reduce blood calcium | 5-360minutes | 10 µM | 43.07 | Rat kidney homogenates proteases | LC-ESI-MS | Rat Liver homogenates | in vitro | None | None | Not reported | |||
| 19770015 | 2009 | VrAPI (Aspartic protease inhibitor in seeds of V. radiata) | 15 | Free | Free | Linear | L | None | From plant Vigna radiata | Protease inhibitor | pH 2-10, Temp 20-100 °C | 2mg -5mg at pH 3 and temperature 100 | ~30 | None | Bradford assay | Buffer | in vitro | None | None | Total (aspartic protease) activity 2516 U | |||
| 21185160 | 2011 | O-1(Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 25 ±4 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-16 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 15th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 58 ±2 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-17 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 55 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 22186872 | 2011 | Angiotensin I | 10 | Free | Free | Linear | L | None | Derived from angiotensinogen | Precursor of angiotensin-II | Room Temperature | 1mg/mL | 1 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Bradykinin | 9 | Free | Free | Linear | L | None | Endogenous peptide of kinin family | Vasodilator, Inflammatory mediator | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | β-Endorphin | 31 | Free | Free | Linear | L | None | Endogenous opioid neuropeptide in neurons of both the central and peripheral nervous system. | Agonist of the opioid receptors | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | [Leu5]Enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid neuropeptide in neurons of both the central and peripheral nervous system. | Neurotransmitter | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Substance P | 11 | Free | Amidation | Linear | L | None | Member of the tachykinin neuropeptide family. | Neurotransmitter | Room Temperature | 1mg/mL | 10 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Somatostatin | 14 | Free | Free | Cyclic (C3-C14) | L | None | Neuropeptide secreted by Hypothalamus | Inhibits insulin and glucagon secretion. | Room Temperature | 1mg/mL | 10 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22263969 | 2012 | ANP-Fc (Atrial natriuretic peptide- Fc) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation. | Natriuretic and vasodilator | 4-72 hours | 0.5mg/kg of protein | 2 to 5 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | GLP-1(7 €“36)NH2 [Glucagon-like peptide-1] | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulate blood glucose | Blood sample collected after 32-60 minutes after the infusion of peptide | 20pmol/kg | 4.8 ±0.8 | Pig kidneys proteases | Radioactivity measurement | Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | Ex-4 (Exendin-4) | 39 | Free | Free | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | Blood sample collected after 50-130 minutes after the infusion of peptide | 10 pmol/kg | 32.8 ±4.1 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | Ex(1 €“30) or Exendin(1 €“30) | 30 | Free | Free | Linear | L | None | Synthetic derived from Exendin 4 | GLP-1 receptor agonist | Blood sample collected after 42-130 minutes after the infusion of peptide | 20 pmol/kg | 28.4 ±1.7 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | GLP-1Arg34(7 €“36), Ex(31 €“39) or [GLP-Ex] | 39 | Free | Free | Linear | L | None | Synthetic | GLP-1 receptor agonist | Blood sample collected after 42-130 minutes after the infusion of peptide | 20 pmol/kg | 19.5 ±3.3 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23813302 | 2013 | TRV027 | 8 | Sar=Sarcosine | Free | Linear | Mix | D-Ala at 8th position | Synthetic β-arrestin-biased agonist | Beta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitment | Not mentioned | 0.01 - 20 μg/kg/min dose | <2 (intial half life) | Human plasma proteases | LC/MS/MS | Human plasma | in vivo | None | None | Not reported | |||
| 23813302 | 2013 | TRV027 | 8 | Sar=Sarcosine | Free | Linear | Mix | D-Ala at 8th position | Synthetic β-arrestin-biased agonist | Beta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitment | Not mentioned | 0.01 - 20 μg/kg/min dose | ~ 10 (Terminal half life) | Human plasma proteases | LC/MS/MS | Human plasma | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 2-120 minutes | 20μg/Kg | 0.05 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 3-120 minutes | 50μg/Kg | 0.54 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(7-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 4-120 minutes | 50μg/Kg | 2.1 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 25025626 | 2014 | Vasotab TY | 76 | Free | Free | Linear | L | None | Salivary glands of the horsefly ofTabanus yao | Vasodialator and anti-thrombic | 1-480 minutes | 5mg/kg | >1 | Mouse plasma proteases | ELISA | Kunming Mouse plasma (Dose i/v injected) | in vivo | None | None | At the dosages of 5,10, and 20 nmol/kg, vasotab TY inhibited thrombus formation by47.2, 72.2, and 86.1%, respectively. | |||
| 25025626 | 2014 | Vasotab TY | 76 | Free | Free | Linear | L | None | Salivary glands of the horsefly ofTabanus yao | Vasodialator and anti-thrombic | 1-480 minutes | 5mg/kg | 50 | Mouse lungs proteases | ELISA | Kunming Mouse lungs (Dose i/v injected) | in vivo | None | None | At the dosages of 5,10, and 20 nmol/kg, vasotab TY inhibited thrombus formation by47.2, 72.2, and 86.1%, respectively. | |||
| 25039358 | 2014 | Gly8-GLP-1(7-36)(Glucagon Like protein-1) | 30 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 37 °C for 2-72 hours | 1000ng/ml | 0.6 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 8.3 ± 0.4 pM in HEK-293 cells | |||
| 25243635 | 2014 | GLP-1(Glucagon Like protein-1) | 31 | Free | Free | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 5-90 hours | 500μg | <2 | DPP IV | ELISA | DPP IV | in vitro | None | None | The insulin levels were increased dramatically to 806.74 ± 30.60 pmol/L within 15 min after GLP-1 administration | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 37 C, 48 Hours | 10 µM | 4.18 | Fxa(Facor Xa) and DPP-IV | HPLC-ESI/MS/MS | Protein Sample +HAS + Fxa +DPP IV | in vitro | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | ~ 5 | db/db mice plasma proteases | LC-MS/MS | db/db Mice plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | ~ 5 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 26197931 | 2015 | PYY(3-34) [Peptide YY] | 34 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Blood sample collected after 15minutes of the infusion of peptide | 100 pmol/kg | 3.6 ±0.5 | Pig blood proteases | Radioimmunoassay | Female pigs blood | in vivo | None | None | Porcine PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.9nmol/L | |||
| 26197931 | 2015 | PYY(1-36) [Peptide YY] | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Blood sample collected after 15minutes of the infusion of peptide | 100 pmol/kg | 7.3 ±0.8 | Pig blood proteases | Radioimmunoassay | Female pigs blood | in vivo | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 1 ±0.3 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26308095 | 2015 | Exenatide | 39 | Free | Amidation | Linear | L | None | Saliva of Gila monster | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 30 | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26325323 | 2015 | Endogenous LHRH | 10 | Free | Amidation | Linear | L | Pyro-Glutamate at 1st position | Hypothalamus | Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH) | Blood sample collected after0.5-24 hours after the injection of peptide | 2.5mg/Kg | 4-8min | Human plasma proteases | LC/MS | Human plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 26337231 | 2015 | P16 [TNF α (75 €“94)] | 20 | Free | Free | Linear | L | None | Tumor necrosis factor-derived (TNF) | Tumor growth inhibitor and anti-angiogenic | Blood sample collected after0.5-24 hours after the injection of peptide | 5mg/kg | 0.096 ±0.008 | BALB/c mice plasma proteases | LC/MS | BALB/c mice plasma (Dose i/v injected) | in vivo | None | None | Growth inhibition effect of RMP16 was observed in DU145 cells (IC50 = 17.20 ± 1.95 nM, Tumor inhibition rates of P16-treated mice was 21.81% | |||
| 26400022 | 2015 | Hirulog-1 | 20 | Free | Free | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 20-25 | Human plasma proteases | HPLC, MS-MS | Human plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 20.50 ± 0.62nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.77 ± 0.09nM | |||
| 26400022 | 2015 | Hirulog-1 | 20 | Free | Free | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 15 ±1.3 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 20.50 ± 0.62nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.77 ± 0.09nM | |||
| 26400022 | 2015 | Peptide 1 (Hirudin mimetic peptide) | 22 | Free | Amidation | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 13+-2.6 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 13.40 ± 0.46 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 5.80 ± 0.55nM | |||
| 18632826 | 2008 | 99m Tc-Duramycin | 19 | Free | Free | Linear | L | Succinimidyl 6-hydrazinonicotinate acetone hydrazone (HYNIC) derivatized, HYNIC conjugated at either at Cys -1 or Amine group Of Lys-2 | Phosphatidylethanolamine binding probe and employed in In Vivo Imaging of Acute Cardiac Cell Death | Molecular probe for imaging PtdE | Blood sample collected at 1-60 minutes | 2.3nmol | <4 | Rat blood proteases | HPLC radiodetection (radio-HPLC) | Healthy Sprague €“Dawley rats blood | in vivo | None | None | Binding of 99mTc-duramycin to apoptotic cells was elevated by a factor of 32 ± 6 | |||
| 21459096 | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Derived from parotid gland | Vasorelaxing | 37 °C for 0-125 minutes | Not mentioned | 1.3 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 21459096 | 2011 | BNP(B-type natriuretic peptide) | 32 | Free | Free | Cyclic (C10-C26) | L | None | Brain natriuretic peptide | Cardiac fibrosis Inhibitor | 37 °C for 0-125 minutes | Not mentioned | 8 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 21459096 | 2011 | CNP(C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | Secreted from vascular endothelium | Vasodialator | 37 °C for 0-125 minutes | Not mentioned | 4.3 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | 19395584 | None | Not reported | |||
| 21459096 | 2011 | CD-NP (C-terminal tail of DNP) | 37 | Free | Free | Cyclic (C6-C22) | L | None | Chimeric peptide derived from CNP and DNP | Natriuretic and aldosterone suppressor | 37 °C for 0-125 minutes | Not mentioned | 17-22.9 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 19344673 | 2009 | Mouse [D-Leu-4]OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Blood collected after 5-120 minutes after peptide delivery | 1mg/200ul | 30 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intraperitoneal route of delivery) | in vivo | 11495687 | None | Not reported | |||
| 19344673 | 2009 | Mouse [D-Leu-4]OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Blood collected after 5-120 minutes after peptide delivery | 1mg/200ul | 35 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Subcutaneous Route of delivery) | in vivo | 11495687 | None | Not reported | |||
| 19344673 | 2009 | Mouse [D-Leu-4]OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Blood collected after 5-120 minutes after peptide delivery | 1mg/200ul | 42 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intra-muscular route of delivery) | in vivo | 11495687 | None | Not reported | |||
| 19344673 | 2009 | Mouse [D-Leu-4]OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Blood collected after 5-120 minutes after peptide delivery | 1mg/200ul | 41.1 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intranasal route of delivery) | in vivo | 11495687 | None | Not reported | |||
| 19157421 | 2009 | Glypromate | 3 | Free | Free | Linear | L | None | N-terminal cleavage product of human insulin-like growth factor-1 (IGF-1) in the brain | Neuroprotective | Blood collected after 0.5-12 hours after peptide delivery | 3 -10 mg/kg/h dose | 5 | Rat plasma proteases | LC-MS | Sprague-Dawley rats plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 19157421 | 2009 | NNZ-2566 (Glycyl-L-2-methylprolyl-L- glutamic acid) | 3 | Free | Free | Linear | L | Methylation of alpha-C of Pro | Glypromate analogue | Neuroprotective | Blood collected after 0.5-12 hours after peptide delivery | 3 -10 mg/kg/h dose | 49 | Rat blood proteases | LC-MS | Sprague-Dawley rats brain (Dose i/v injected) | in vivo | None | None | NNZ-2566-treated animals(i/v) exhibited an average infarct area of 79.8 ±10.4 mm2 (3 mg/kg/h, pb0.01) and 21.3 ±7.5 mm2 (10 mg/kg/h) as compare to ET-1 induced an infarct area of 153.1 ±20.1 mm2 (mean ±s.e.m) in saline-treated rat; Total injury size was 22.2 ±5.7 mm2 following 30 mg/kg (76% protection; Dunnett's multiple comparison test) and only 4.6 ±2.3 mm2 following 60 mg/kg (95% protection; Dunnett's multiple comparison test). | |||
| 24139844 | 2013 | Conjuagte 3(conjugates of 4-aminocyclophosphamide (4-NH2-CPA)) | 5 | Bn-glutarylation | Amidated CPA | Linear | L | None | Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA) | Anti-cancer | Not mentioned | Not mentioned | 55 | PSA(Prostate-specific antigen ) | HPLC | Conjuagte 3+PSA(Prostate-specific antigen) | in vitro | None | None | pEC50-8.19 ±1.0minutes, Emax 9.44 ±0.3 nmol/well | |||
| 24874704 | 2014 | AM(adrenomedullin) | 52 | Free | Amidation | Cyclic (Ringed structure formed by C16-C21) | L | None | Isolated from Human pheochromocytoma | Vasodilator and cardiovascular protection | Not mentioned | 3nmol/kg Dose | 15.2 ±1.9 min (2nd plasma half life) | Rat plasma proteases | ELISA | Male Wistar rats plasma | in vivo | http://www.genscript.com/peptide/RP11288-Adrenomed | None | Native human AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.59 ± 0.90 and9.30 ± 0.26 nmol/well | |||
| 24874704 | 2014 | PEGylated AM | 52 | Pegylation | Amidation | Cyclic (Ringed structure formed by C16-C21) | L | None | Isolated from Human pheochromocytoma | Vasodilator and cardiovascular protection | Not mentioned | 3nmol/kg Dose | 4.87 ±0.68(1st plasma half life) | Rat plasma proteases | ELISA | Male Wistar rats plasma | in vivo | http://www.genscript.com/peptide/RP11288-Adrenomed | None | PEGylated AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.519 ± 0.10 and9.44 ± 0.30 nmol/well | |||
| 25453979 | 2014 | (D-Leu-4)OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio | 34 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum(Subcutaneous Route of delivery) | in vivo | None | None | Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM | |||
| 25453979 | 2014 | (D-Leu-4)OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio | 49 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intraperitoneal route of delivery) | in vivo | None | None | Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM | |||
| 25453979 | 2014 | (D-Leu-4)OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio | 36 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intra-muscular route of delivery) | in vivo | None | None | Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM | |||
| 25453979 | 2014 | (D-Leu-4)OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio | 20 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Oral route of delivery) | in vivo | None | None | Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM | |||
| 25453979 | 2014 | (D-Leu-4)OB3 | 7 | Free | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio | 41 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intranasal route of delivery) | in vivo | None | None | Stimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS | |||
| 24462899 | 2014 | APTEDB-DTX (Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate) | 27 | Free | Free | Linear | L | Modified Gly at 16th postion i.e. propargylglycine and peptide conjugated with drug DTX at this position | Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate | Drug(anticancer agent i.e. DTX) Delivery vehicle | Not mentioned | 5 mg DTX/kg Dose | 0.491 | Mice serum proteases | HPLC | C57BL6 mice Serum | in vivo | None | None | Stimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS | |||
| 5092290 | 2014 | LL-37 (Antimicrobial Peptide) | 37 | Free | Free | Linear | L | None | Human epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein) | Antimicrobial | 15-720 minutes hour | 3 µM | ~1 | Cathepsin | Proteolysis assay, (confirmed by Western blotting) | Western Blotting | in vitro | 16716248 | None | Not reported | |||
| 1319455 | 1992 | hCRH(Human Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 30.5 ±3.3 | Human plasma proteases | IRM(Immunoradiometric assays) | Human plasma | in vivo | 12379493 | None | 22.4 ± 8.1 ng/hour (ACTH response) | |||
| 1319455 | 1992 | hCRH(Human Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 46.5 ±7.2 | Sheep plasma proteases | IRM(Immunoradiometric assays) | Human plasma | in vivo | 12379493 | None | 46.5 ± 6.4 ng/hour (ACTH response) | |||
| 1319455 | 1992 | oCRH(Ovine Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 42.8 ±6.4 | Human plasma proteases | IRM(Immunoradiometric assays) | Sheep plasma | in vivo | 6603620 | None | 39.9 ± 11.7 ng/hour (ACTH response) | |||
| 1319455 | 1992 | oCRH(Ovine Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 39.8 ±10.1 | Sheep plasma proteases | IRM(Immunoradiometric assays) | Sheep plasma | in vivo | 6603620 | None | 40.2 ± 8.4 ng/hour (ACTH response) | |||
| 1387608 | 1992 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Blood collected 1-60 minutes after peptide infused | 2μg/min | 12.5 (Terminal half life) | Human plasma proteases | IRM(Immunoradiometric assays) | Young Human plasma (average age 23.3) (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 1387608 | 1992 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Blood collected 1-60 minutes after peptide infused | 2μg/min | 9.6 (Terminal half life) | Human plasma proteases | IRM(Immunoradiometric assays) | Older Human plasma(average age 75.3) (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 1646465 | 1991 | rANP(99-126) (Recombinant atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | Not mentioned | 114 ±38.6 | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma | in vivo | None | None | Not reported | |||
| 1646465 | 1991 | iso-rANP(1-45) (Recombinant atrial natriuretic peptide) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | 1 x 106 cpm | 130 ±13 | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 1646465 | 1991 | iso-rANP(1-45) (Recombinant atrial natriuretic peptide) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | 1x 106 cpm | 164.3 ±9.0(β- t1/2) | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 1649728 | 1991 | VIP(Vasoactive intestinal peptide) | 28 | Free | Amidation | Linear | L | None | Peptide hormone secreted by Intestine | Stimulates the secretion of electrolytes and water | Sample collected at 40-50 minutes | 10pmol min-1 kg -1 peptide infused | 1.27 ±0.20 | Rabbit plasma proteases | Radioimmunoassay | New Zealand White rabbits plasma(have normal sodium diet i.e. 29.35 k 4.02 pmol/l) | in vivo | None | None | Not reported | |||
| 1723638 | 1991 | Galanin(1-16) | 16 | Free | Free | Linear | L | None | High affinity synthetic agonist | Neuroendocrine activities, stimulates growth hormone secretion | 37 °C | 2 μM | 28 | Hypothalamic membrane protaeses | HPLC | Hypothalamic membranes of Male Sprague-Dawley rats | in vitro | None | None | Not reported | |||
| 1730807 | 1992 | GHRP (Growth Hormone releasing peptide) | 6 | Free | Amidation | Linear | Mix | None | Growth Hormone releasing peptide | Release growth hormone | Not mentioned | 100μg/kg | 20 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | None | None | GH response elicited by 300 μg/kg on oral administeration of peptide | |||
| 1763193 | 1991 | Peptide T (Dala1-peptide T-NH2) | 8 | Free | Amidation | Linear | Mix | None | Synthetic derived from the external envelope protein of HIV IIIB | HIV-entry inhibitor | Not mentioned | Intravenous test dose of 0.033 mg/Kg of peptide T | 30-60 | AIDS patient plasma proteases | Radioimmunoassay , HPLC | AIDS patient plasma | in vivo | None | None | Not reported | |||
| 1826667 | 1991 | GRF(1-29)-NH2 (Growth hormone-releasing factor (GRF- Growth regulating factor)) | 29 | Free | Amidation | Linear | L | None | Growth regulating factor (GRF) | Release growth hormone | Not mentioned | 100 µg/ml | 0.25 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [Ala15]GRF(1-29)-NH2 | 29 | Free | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | 0.3 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [DesNH2-Tyr1,Ala15]GRF(1-29)-NH2 | 29 | Chlorpheniramine M | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | 1 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [DesNH2-Tyr1,D-Ala2,Ala15]GRF(1-29)-NH2 | 29 | Chlorpheniramine M | Amidation | Linear | Mix | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | 1 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 45 ±5 | Normal Human plasma proteases | Radioimmunoassay and HPLC | Normal Human plasma | in vitro | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 10.4 ±1.1 | Pancreatitis patients blood proteases | Radioimmunoassay and HPLC | Pancreatitis patient plasma | in vitro | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 11.1 ±1 | Pancreatitis patients plasma proteases | Radioimmunoassay and HPLC | Pancreatitis patient blood | in vitro | None | None | Not reported | |||
| 2162275 | 1990 | PHM (Peptide histidine methionine) | 27 | Free | Amidation | Linear | L | None | Peptide derived from Prepro-VIP | Vasodilator | Not mentioned | 5 pmol min-1 kg-1 | 6.5 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | It increase heart rate | |||
| 2162275 | 1990 | PHV (Peptide histidine valine) | 42 | Free | Free | Linear | L | None | Peptide derived from Prepro-VIP | Vasodilator | Not mentioned | 5 pmol min-1 kg-1 | 37.5 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | It increases heart rate but not significantly | |||
| 2896343 | 1988 | GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | L | None | Growth regulating factor | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 6.2 ±0.7 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 100% | |||
| 2896343 | 1988 | [D-Ala2]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 6.6 ±0.4 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 5146% | |||
| 2896343 | 1988 | [D-Asp3]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 5.9 ±0.8 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 670% | |||
| 2896343 | 1988 | lD-Asn8]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 6.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 221% | |||
| 2896343 | 1988 | [D-Tyr10]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 4.7 ±0.8 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 230% | |||
| 2896343 | 1988 | Ac-[D-Tyr1,D-AIa2]GRF(1-29)-NH2 (Growth regulating factor) | 29 | Acetylation | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 7.4 ±0.5 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 2817% | |||
| 2940625 | 1986 | [D-Trp6]-LHRH (Luteinizing hormone-releasing hormone) | 10 | Free | Amidation | Linear | Mix | Pyr=Pyro-glutamic acid | LHRH (Luteinizing hormone-releasing hormone) derivative | Release Luteinizing hormone | Blood collected 1-240 minutes after peptide infused | 100 µg/ml | >10 (alpha t1/2) | Dog plasma proteases | HPLC | Two male Beagle dogs plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 2953516 | 1987 | rANP (Recombinant Atrial natriuretic peptide ) | 26 | Free | Free | Cyclic (C5-C21) | L | None | Atrial natriuretic factor | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 0.2-2 hours after peptide injection | 1 μg/min dose | 4.5 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | ANP induced dose-related effects on systemic and renal hemodynamic, as well as electrolyte excretion | |||
| 2966345 | 1988 | rANF(Asn1-Arg98) [Rat atrial natriuretic factor] | 98 | Free | Free | Linear | L | Radioiodinated peptide at Tyr-4 | Rat ANF derivative [Rat atrial natriuretic factor] | Natriuretic, diuretic and vasorelaxant peptide | Not mentioned | 10 X106 CPM | 54.8 ±3.9(2nd component) | Rat plasma proteases | Radioimmunoassay | Male Sprague-Dawley rats plasma | in vivo | http://www.uniprot.org/uniprot/P01161 | None | Not reported | |||
| 2966345 | 1988 | rANF(Asn1-Arg98) [Rat atrial natriuretic factor] | 98 | Free | Free | Linear | L | Radioiodinated peptide at Tyr-4 | Rat ANF derivative [Rat atrial natriuretic factor] | Natriuretic, diuretic and vasorelaxant peptide | Not mentioned | 10 X106 CPM | 2.5 ±0.3(1st compent) | Rat plasma proteases | Radioimmunoassay | Male Sprague-Dawley rats plasma | in vivo | http://www.uniprot.org/uniprot/P01162 | None | Not reported | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 10 µg/kg peptide injected to rhesus monkey | 4.0 ±1.2 (t1/2fast) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1035 ± 226 %, cortisol increased by 123 ± 34% on 10 µg/kg dose | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 100 µg/kg peptide injected to rhesus monkey | 1.5 ±0.5 (t1/2fast) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1858 ± 452 %, cortisol increased by 231 ± 28% on 10 µg/kg dose | |||
| 2988919 | 1985 | oCRF(Ovine corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 1 µg/kg peptide injected to rhesus monkey | 3.6 ±1.1 (t1/2 fast) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 161 ± 40 %, cortisol increased by 78 ± 22 % on 10 µg/kg dose | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 10 µg/kg peptide injected to rhesus monkey | 29.0 ±2.0(t1/2 slow) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1858 ± 452 %, cortisol increased by 123 ± 28% on 10 µg/kg dose | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 100 µg/kg peptide injected to rhesus monkey | 32.7 ±10.1 (t1/2 slow) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1858 ± 452 %, cortisol increased by 231 ± 28% on 10 µg/kg dose | |||
| 2988919 | 1985 | oCRF(Ovine corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 1 µg/kg peptide injected to rhesus monkey | 44.3 +/= 6.7 (t1/2 slow) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 161 ± 40 %, cortisol increased by 78 ± 22 % on 10 µg/kg dose | |||
| 3147901 | 1988 | Oxyntomodulin | 37 | Free | Free | Linear | L | None | Synthetic derived from proglucagon, identified in extracts from porcine small intestinal mucosa | GLP-1-GCGR (glucagon) agonist | Blood samples collected at 1-5 hourss after peptide injection | 100- 400ng/kg/h | 12 ±1 | Human plasma proteases | Radioimmunoassay | Human plasma (Dose i/v injected) | in vivo | http://www.glucagon.com/oxyntomodulin.html | None | The acid secretion increased during the first 90 rnin of pentagastrin infusion from 1 - 2 meq H+/15 rnin to a plateau of 5-6 meq H+/15 min | |||
| 3215483 | 1988 | MET-enkephalin (Methionine-enkephalin) | 5 | Free | Free | Linear | L | None | Enkephalin | Neurotransmitter | 37 °C for 1-180 minutes | 300pg (pooled platelet-poor plasma) | 12.8 | Human plasma proteases | TLC (Thin-layer chromatography) | Human plasma | in vitro | None | None | Not reported | |||
| 3215483 | 1988 | LEU-enkephalin (Leucine-enkephalin) | 5 | Free | Free | Linear | L | None | Enkephalin | Neurotransmitter | 37 °C for 1-180 minutes | 300pg (pooled platelet-poor plasma) | 7 | Human plasma proteases | TLC (Thin-layer chromatography) | Human plasma | in vitro | None | None | Not reported | |||
| 3261772 | 1988 | hCGRP(Human Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Blood collected-10 to 90 minutes after peptide infusion | 5pmol/kg | 3.6 ±0.3 (Half life of 1st phase) | Sheep plasma proteases | Radioimmunoassay, RP-HPLC | Merino-Corriedale cross ewes (sheep) plasma | in vivo | None | None | Not reported | |||
| 3261772 | 1988 | hCGRP(Human Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Blood collected-10 to 90 minutes after peptide infusion | 5pmol/kg | 13.6 ±1.0(Half life of 1st phase) | Sheep plasma proteases | Radioimmunoassay, RP-HPLC | Merino-Corriedale cross ewes (sheep) plasma | in vivo | None | None | Not reported | |||
| 3379352 | 1988 | Reduced IGF-1(Free form) (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | Labelled with 125I, Disulphide bond is reduced | Bovine IGF-1 | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 0.8 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 3379352 | 1988 | S-CM IGF-1 (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | S-CM=S-carboxymethylated | Bovine IGF-1 | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 0.8-0.9 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 3601235 | 1987 | Porcine NPY (Neuropeptide Y) | 36 | Free | Amidation | Linear | L | None | Neuropeptide | Acts as a neurotransmitter | Blood collected 1 to 90 minutes after peptide infusion | 06-10nM/kg | ~ 20 (20-28) | Dog plasma proteases | Radioimmunoassay | Six mongrel dogs plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3492729 | 1986 | MET-enkephalin (Methionine-enkephalin) | 5 | Free | Free | Linear | L | None | Enkephalin | Neurotransmitter | Blood collected 5-60 minutes after peptide infused | 1-20mM | <2 | Proteases from rhesus monkey plasma | RP-HPLC | Rhesus monkey plasma | in vitro | None | None | Not reported | |||
| 3768731 | 1986 | DSIP (Delta sleep inducing peptide) | 9 | Free | Free | Linear | L | None | Neuropeptide secreted from hypothamus | Stress reliever, stimulates LH, somatostatin | Blood collected 2-60 minutes after peptide injected | 0.1mg/Kg | 7.24 ±0.77 | Proteases from dog plasma | Radioimmunoassay | Mongrel dog plasma(Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3768731 | 1986 | des-Trp-DSIP | 8 | Free | Free | Linear | L | None | DSIP analogue | Anticarcinogenic | Blood collected 2-60 minutes after peptide injected | 0.1mg/Kg | 7.55 ±0.52 | Proteases from dog plasma | Radioimmunoassay | Mongrel dog plasma(Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3768731 | 1986 | D-Ala3-DSIP | 9 | Free | Free | Linear | Mix | None | DSIP analogue | Anticarcinogenic | Blood collected 2-60 minutes after peptide injected | 0.1mg/Kg | 8.19 ±0.30 | Proteases from dog plasma | Radioimmunoassay | Mongrel dog plasma(Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3768731 | 1986 | D-Ala4-DSIP | 9 | Free | Free | Linear | Mix | None | DSIP analogue | Anticarcinogenic | Blood collected 2-60 minutes after peptide injected | 0.1mg/Kg | 12.9 ±0.83 | Proteases from dog plasma | Radioimmunoassay | Mongrel dog plasma(Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3768731 | 1986 | D-Ala4-DSIP-NH2 | 9 | Free | Amidation | Linear | Mix | None | DSIP analogue | Anticarcinogenic | Blood collected 2-60 minutes after peptide injected | 0.1mg/Kg | 10.2 ±0.69 | Proteases from dog plasma | Radioimmunoassay | Mongrel dog plasma(Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3924685 | 1985 | hGRF-1(1-40) (Human growth regulating factor) | 40 | Free | Amidation | Linear | L | None | Human growth regulating factor | Release growth hormone | Blood collected 60-240 minutes after peptide injection | 5 µg/200ul | 57.3 ±1.5 (beta or elimination half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 3924685 | 1985 | hGRF-1(1-40) (Human growth regulating factor) | 40 | Free | Amidation | Linear | L | None | Human growth regulating factor | Release growth hormone | Blood collected 60-240 minutes after peptide injection | 5 µg/200ul | 3.2 ±0.2 (alpha or distribution half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 4.95 ±1.04(short half life or initial decay) | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 32.4 ±5(long half life) | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 4.55 ±1.23 (short half life or initial decay) | Proteases from Human(obese) plasma | Radioimmunoassay | Human(obese) plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 32.4 ±5(long half life) | Proteases from Human(obese) plasma | Radioimmunoassay | Human(obese) plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1651738 | 1991 | alpha-ANP (alpha-atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | alpha-atrial natriuretic peptide | Natriuretic and vasodilator | Blood collected 30-60 minutes during and 5-20 minutes after peptide injection | 0.005 - 0.05 µg/kg/min in 25 mL normal saline infused over 1 h | 4.3 ±0.6 | Proteases from Human plasma(younger, 20-39 years old) | Radioimmunoassay | Human plasma(younger, 20-39 years old) | in vivo | None | None | Natriuresis (145 ±36 ν 142 ± 28 µMol/min) and urinary cGMP excretion (40.9 ± 6.7 nmol/h) | |||
| 1651738 | 1991 | alpha-ANP (alpha-atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | alpha-atrial natriuretic peptide | Natriuretic and vasodilator | Blood collected 30-60 minutes during and 5-20 minutes after peptide injection | 0.005 - 0.05 µg/kg/min in 25 mL normal saline infused over 1 h | 7.8 ±0.6 | Proteases from Human plasma(older, 65-83 years old) | Radioimmunoassay | Human plasma(older, 65-83 years old) | in vivo | None | None | Natriuresis 142 ± 28 µMol/min and urinary cGMP excretion 35.3 ± 4.1 | |||
| 1777964 | 1991 | CLAP(Prpcolipase activation peptide) | 5 | Free | Free | Linear | L | None | Derived from colipase | Procolipase activation peptide | Room Temperature(25C) | 500nM/L | 5 | Proteases from Human serum | ELISA | Human Serum | in vitro | None | None | Not reported | |||
| 1831249 | 1991 | ANP(99-126) (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Blood collected 2-20 minutes after peptide infused | 5pmol/kg | 4.8 ±0.8 | Proteases from Human plasma (Chronic renal diseases) | Radioimmunoassay | Human plasma (Chronic renal diseases) | in vivo | None | None | GFR and ERPF increased by a mean value of 23% and 27% respectively | |||
| 1882091 | 1991 | GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | L | pGlu= Pyro-glutamate | Hormone secreted by Hypothalamus | Stimulates the release of the gonadotropins from the pituitary. | 37 °C | 40mg/ml | 10.5 | Proteases from Rat ovary tissues | Radioimmunoassay | Rat ovary tissues | in vitro | 1631133 | None | Not reported | |||
| 1882091 | 1991 | GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | L | pGlu= Pyro-glutamate | Hormone secreted by Hypothalamus | Stimulates the release of the gonadotropins from the pituitary. | 37 °C | 40mg/ml | 45 | Proteases from Rat Lung tissues | Radioimmunoassay | Rat lung tissues | in vitro | 1631133 | None | Not reported | |||
| 1882091 | 1991 | GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | L | pGlu= Pyro-glutamate | Hormone secreted by Hypothalamus | Stimulates the release of the gonadotropins from the pituitary. | Blood collected 30-300 minutes after peptide injection | 24 µg/kg | 2.66 (t1/2 alpha) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | 1631133 | None | Not reported | |||
| 1882091 | 1991 | GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | L | pGlu= Pyro-glutamate | Hormone secreted by Hypothalamus | Stimulates the release of the gonadotropins from the pituitary. | Blood collected 30-300 minutes after peptide injection | 24 µg/kg | 12.16 (t1/2 beta) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | 1631133 | None | Not reported | |||
| 1882091 | 1991 | D-Phe-6-GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | Mix | None | GnRH derivative | Stimulates the release of the gonadotropins from the pituitary. | Blood collected 30-300 minutes after peptide injection | 24 µg/kg | 14.53 | Rat plasma proteases | Radioimmunoassay | (Dose i/m injected)Rat plasma | in vivo | 1631133 | None | Not reported | |||
| 1882091 | 1991 | D-Trp3-D-Phe-6-GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | Mix | None | GnRH derivative | Stimulates the release of the gonadotropins from the pituitary. | Blood collected 30-300 minutes after peptide injection | 24 µg/kg | 25.8 (t1/2 beta) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | 1631133 | None | Not reported | |||
| 1882091 | 1991 | D-Trp3-D-Phe-6-GnRH (Gonadotropin releasing hormone) | 10 | Free | Amidation | Linear | Mix | None | GnRH derivative | Stimulates the release of the gonadotropins from the pituitary. | Blood collected 30-300 minutes after peptide injection | 24 µg/kg | 36.4 | Rat plasma proteases | Radioimmunoassay | (Dose i/m injected)Rat plasma | in vivo | 1631133 | None | Not reported | |||
| 2156886 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 2 pmol/kg peptide infused | 3.1 | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide infused | 1.23 ±0.35 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide+ captoril(ACE inhibitor) infused | 6.99 ±0.34 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide+phosphoramidon, a specific E-24.11 inhibitor infused | 11.8 ±0.49 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide+phosphoramidon, a specific E-24.11 inhibitor +captoril(ACE inhibitor infused | 14.3 ±0.48 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide | 4.6 ±0.1 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide+ captoril(ACE inhibitor | 8.3 ±0.3 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide+phosphoramidon, a specific E-24.11 inhibitor infuse | 5.6 ±0.2 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide+phosphoramidon, a specific E-24.11 inhibitor +captoril(ACE inhibitor infused | 9.9 ±0.4 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2454805 | 1988 | [125I]B-chain mutant IGF-1 | 71 | Free | Free | Linear | L | None | Human Recombinant peptide | Stmulates glycogen synthesis | Blood collected 10 minutes to 6 hours after peptide injection | 2 µCi peptide injected to rhesus monkey | 27.5 | Proteases from Rat serum | Radioimmunoassay | Rat Serum | in vivo | None | None | Stimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm | |||
| 2454805 | 1988 | [125I] [Gln3,Ala4,Tyr15,Leu16]IGF-1 | 70 | Free | Free | Linear | L | None | Human Recombinant peptide | Stmulates glycogen synthesis | Blood collected 10 minutes to 6 hours after peptide injection | 3 µCi peptide injected to rhesus monkey | 26.9 | Proteases from Rat serum | Radioimmunoassay | Rat Serum | in vivo | None | None | Stimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm | |||
| 2498387 | 1989 | Buserelin | 9 | Free | Ethylamide | Linear | Mix | D-Ser(tBu) at 6th position, Pglu=pyr- Glutamate | Analogue of LHRH (Luteinizing hormone-releasing hormone) | Stimulates release of LH, FSH and estradiol | Blood collected 0-6 hours after peptide injection | 500 µg/kg | 11.2 (elimination t1/2 after 10-60 min of i/v injection) | Proteases from serum of women with endometriosis | Radioimmunoassay, HPLC | (Dose i/v injected)Serum of women with endometriosis | in vivo | None | None | Serum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values | |||
| 2498387 | 1989 | Buserelin | 9 | Free | Ethylamide | Linear | Mix | D-Ser(tBu) at 6th position | Analogue of LHRH (Luteinizing hormone-releasing hormone) | Stimulates release of LH, FSH and estradiol | Blood collected 0-6 hours after peptide injection | 500 µg/kg | 50.4 (elimination t1/2 after 60-120 mins of i/v injection) | Proteases from serum of women with endometriosis | Radioimmunoassay, HPLC | (Dose i/v injected)Serum of women with endometriosis | in vivo | None | None | Serum LH, FSH, and estradiol concentrations increased acutely up to 10-fold above basal values | |||
| 2521208 | 1989 | VP (Vasopressin) | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Anti-diuretic hormone secreted by pitutiary gland | Anti-diuretic and regulates retention of water | Not mentioned | Exogenously administered | 5.4(lower phase) | Proteases from Rabbit plasma | Radioimmunoassay | Rabbit plasma | in vivo | None | None | Not mentioned | |||
| 2521208 | 1989 | VP (Vasopressin) | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Anti-diuretic hormone secreted by pitutiary gland | Anti-diuretic and regulates retention of water | Not mentioned | Endogenously administered | 1.3 | Proteases from Rabbit plasma | Radioimmunoassay | Rabbit plasma | in vivo | None | None | Not mentioned | |||
| 2521208 | 1989 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic | Natriuretic and vasodilator | Not mentioned | Exogenously administered | 1.2 | Proteases from Rabbit plasma | Radioimmunoassay | Rabbit plasma | in vivo | None | None | Not mentioned | |||
| 2521208 | 1989 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic | Natriuretic and vasodilator | Not mentioned | Endoogenously administered | 3.2 | Proteases from Rabbit plasma | Radioimmunoassay | Rabbit plasma | in vivo | None | None | Not mentioned | |||
| 2866222 | 1985 | hGRF-1(1-29) (Human growth hormone-releasing factor) | 29 | Free | Amidation | Linear | L | None | Human growth hormone-releasing factor | Stimulates growth hormone release | Blood collected 2-60 minutes after peptide injection | 10 µg/200μ1 0.9% NaCl/0.5% Human Serum albumin, | 1.9 ±0.2 (alpha half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 2866222 | 1985 | hGRF-1(1-29) (Human growth hormone-releasing factor) | 29 | Free | Amidation | Linear | L | None | Human growth hormone-releasing factor | Stimulates growth hormone release | Blood collected 2-60 minutes after peptide injection | 10 µg/200μ1 0.9% NaCl/0.5% Human Serum albumin, | 10.4 ±0.2 (beta or elimination half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 2868381 | 1986 | Somatostatin | 14 | Free | Free | Cyclic (C3-C14) | L | None | Growth hormone €“inhibiting hormone (GHIH) | Inhibitor of Growth hormone secretion | Blood sample collected after 10 minutes in 5 minutes interval, followed by 30 minutes thricely at 1 | 250 µg peptide infused | 1.2-3.6 | Proteases from plasma of healthy Human | Radioimmunoassay | Human plasma | in vivo | None | None | Not reported | |||
| 2868381 | 1986 | Somatostatin | 14 | Free | Free | Cyclic (C3-C14) | L | None | Growth hormone €“inhibiting hormone (GHIH) | Inhibitor of Growth hormone secretion | Blood sample collected after 10 minutes in 5 minutes interval, followed by 30 minutes thricely at 1 | 250 µg peptide infused | 1.4-4.1 | Proteases from plasma of Human patient (cirrhotic subjects) | Radioimmunoassay | Plasma of Human patient (cirrhotic subjects) | in vivo | None | None | Not reported | |||
| 3108068 | 1987 | IGF-1 (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | None | Purified from bovine colostrum | Mediates growth and development | Blood collected 12hours after peptide injection | 6 - 10 µg/Kg | <15 | Proteases from chicken plasma | Radioimmunoassay | (Dose i/v injected)Chicken plasma | in vivo | None | None | GH concentrations subsequent to TRH injection were significantly depressed45.1 and 48.2% in IGF-l-treated as compared with control chicks; and GRF-stimulated GH secretion was significantly decreased by IGF-I administration in (41.3%) | |||
| 1664804 | 1991 | Rat BNP-45 ( Brain natriuretic peptide-45) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Isolated from rat heart and shown to be a circulating form of rat BNP | Cardiac Natriuretic Peptide | Blood samples collected at 0.5-10 minutes post peptide injection | 2 µg/150ul saline | 6.95 (t 1/2 beta or 2nd phase t1/2) | Proteases from Mice (WKY)plasma | Radioimmunoassay | (Dose i/v injected)Mice (WKY) plasma | in vivo | None | None | Urinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.2 | |||
| 1664804 | 1991 | Rat alpha-ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic and vasodilator | Blood samples collected at 0.5-10 minutes post peptide injection | 2 µg/150ul saline | 4.03 (t 1/2 beta or 2nd phase t1/2) | Proteases from Mice (WKY)plasma | Radioimmunoassay | (Dose i/v injected)Mice (WKY) plasma | in vivo | None | None | Urinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.4 | |||
| 2524034 | 1989 | [Leu5]Enkephalin | 18 | Free | Free | Linear | L | None | Somatostatin | Inhibitor of Growth hormone secretion | Not mentioned | Peptide 0.04 w/v in 154mM KCl | 33 ±7 | Proteases from rat rectal proteases | HPLC | Rat rectal lumen | in vitro | None | None | Not mentioned | |||
| 2524034 | 1989 | [3H-Lys9]DE-gamma-E | 18 | Free | Free | Linear | L | None | Neuroleptic peptide | Neuroregulator | Not mentioned | 6 µg or 200uCi | 1.2 ±0.6 | Proteases from rat blood | HPLC | Rat blood | in vivo | None | None | Not mentioned | |||
| 2556215 | 1989 | Angiotensin I (AI) | 10 | Free | Free | Linear | L | None | Derived from angiotensin | Precusor of angiotensin- II (AII) | 37 °C | 100 - 2000 ng/ml | 0.6 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (20%) | in vitro | None | None | Not mentioned | |||
| 2714145 | 1989 | GLP-1(72-107) (Glucagon-like peptide-1) | 36 | Free | Amidation | Linear | L | None | Glucagon-like peptide-1 derivative | Regulates glycemic index, inhibits gastric acid secretion | Not mentioned | 14.4ng/kg peptide infused from 45 min as priming dose, followed by 100 - 400 ng/kg/h dose for 45 m | 17.2 ±2 | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | 200pmol/L and 600pmol/L cause 16% and 23% Inhibition of pentagastrin-stimulated acid secretion respectively | |||
| 2714145 | 1989 | Truncated GLP-1(78-107) | 31 | Free | Amidation | Linear | L | None | Glucagon-like peptide-1 derivative | Regulates glycemic index, inhibits gastric acid secretion | Not mentioned | 4.8 -14.4ng/kg peptide infused from 45 min as priming dose, followed by 12.5 - 50 ng/kg/h dose for | 11.4 ±2.1 | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | 200pmol/L of peptide causes 36% Inhibition of pentagastrin-stimulated acid secretion respectively | |||
| 8147781 | 1994 | CGRP(Calcitonin gene related peptide) | 37 | Free | Free | Linear | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | 37 °C for 5-60 minutes | 60 µL of 1 nmol/L CGRP | 4.3 ±0.2 | Proteases from sheep plasma | Radioimmunoassay | Sheep plasma before nephrectomy | in vitro | None | None | Not reported | |||
| 8147781 | 1994 | CGRP(Calcitonin gene related peptide) | 37 | Free | Free | Linear | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | 37 °C for 5-60 minutes | 60 µL of 1 nmol/L CGRP | 7.6 ±0.8 | Proteases from sheep plasma | Radioimmunoassay | Sheep plasma after 2 days nephrectomy | in vitro | None | None | Not reported | |||
| 8147781 | 1994 | CGRP(Calcitonin gene related peptide) | 37 | Free | Free | Linear | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | 37 °C for 5-60 minutes | 60 µL of 1 nmol/L CGRP | 7.3 ±0.4 | Proteases from sheep plasma | Radioimmunoassay | Sheep plasma after 5 days nephrectomy | in vitro | None | None | Not reported | |||
| 8217216 | 1993 | AcSDKP (Acetyl-SDKP) | 4 | Acetylation | Free | Linear | L | None | Isolated from fetal calf bone marrow | Natural hemoregulatory | 37 °C for 24 hours | 4 X lO-7M, 10 µCi | 0.75 | Proteases from Human serum | HPLC | Human serum | in vitro | None | None | Not reported | |||
| 8217216 | 1993 | AcSDKP (Acetyl-SDKP) | 4 | Acetylation | Free | Linear | L | None | Isolated from fetal calf bone marrow | Natural hemoregulatory | 37 °C for 24 hours | 4 X lO-7M, 10 µCi | 0.5 | Proteases from Horse serum | HPLC | Horse serum | in vitro | None | None | Not reported | |||
| 8218482 | 1993 | YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer) | 5 | Free | Free | Linear | L | Peptide covalently attached to Isocyanate containing polyurethane prepolymer | Synthetic RGD containing peptide | Cell attachment property | Not mentioned | Not mentioned | 0.5 (Half life of 1st phase) | Proteases from mouse bood | HPLC | Mouse blood | in vivo | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 1 (DYN A analogue) | 11 | Free | Amidation | Linear | L | None | Human placenta Dynorphin A derivative | Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates. | 37 °C | 100 µM | 42 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 3 (DYN A analogue) | 11 | Free | Amidation | Linear | L | None | Human placenta Dynorphin A derivative | Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates. | 37 °C | 100 µM | 43 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 9234336 | 1994 | 131I-VIP (Vasoactive intestinal peptide) | 28 | Free | Amidation | Linear | L | Iodinated at Tyr | Neuropeptide | Anti-inflammatory neuropeptide | Organs are collected at 2-60 minutes after administration of drug (by killing organism) | 250 µg (6MBq in 0.2mL) | 2.3 ±0.8 (elimination half life) | Proteases from rat lung tissues | HPLC | (Dose i/v injected)Rat lung tissues | in vivo | None | None | Not reported | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 1.05 ±0.04 (1st phase elimination life) | Proteases from SHR rat plasma | Radioimmunoassay | Rat(SHR) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 1.19 ±0.09 (1st phase elimination life) | Proteases from WKY rat plasma | Radioimmunoassay | Rat(WKY) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 18.1 ±1.4 (2nd phase elimination life) | Proteases from SHR rat plasma | Radioimmunoassay | Rat(SHR) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 16.3 ±1.2 (2nd phase elimination life) | Proteases from WKY rat plasma | Radioimmunoassay | Rat(WKY) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8395230 | 1993 | Bradykinin | 9 | Free | Free | Linear | L | None | Endogenous peptide of kinin family | Vasodilator, Inflammatory mediator | 37 °C for 15-60 minutes | 10 µg/L of peptide | 29 ±1 | Neutral endopeptides in Human umbilical vein endothelial cells | Radioimmunoassay | Human umbilical vein endithelial cells | in vitro | None | None | Not reported | |||
| 8395230 | 1993 | Bradykinin | 9 | Free | Free | Linear | L | None | Endogenous peptide of kinin family | Vasodilator, Inflammatory mediator | 37 °C for 15-60 minutes | 10 µg/L of peptide | 46 ±2 | Neutral endopeptides in Human umbilical vein endothelial cells | Radioimmunoassay | Human umbilical vein endithelial cells+ phosphoramidon | in vitro | None | None | Not reported | |||
| 8388403 | 1993 | ile 12-ANP (Atrial natriuretic peptide) | 26 | Free | Free | Cyclic (C5-C21) | L | None | Infusions of atrial natriuretic peptide | Natriuretic and vasodilator | Blood sample collected after 15-240 minutes after peptide administration | 1.5pmol/Kg/min dose of peptide | 4.1 ±0.4 | Proteases from Human plasma | Radioimmunoassay | Human plasma(elder men) | in vivo | None | None | It increases the cGMP approx 3 fold | |||
| 2945560 | 1986 | hANP (Human Atrial Natriuretic Peptide) | 28 | Free | Amidation | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Not mentioned | 98.3 ± 44.6pg/ml | 5.65 | Proteases from Human plasma | Radioimmunoassay | Human plasma(bolus injection) | in vivo | None | None | Not reported | |||
| 18424366 | 2008 | GLP(7-34) (Glucagon like peptide) | 28 | Acetylation | Amidation | Linear | L | None | GLP-1 (Glucagon like peptide-1) analogue | Antihyperglycemic or incretin effect (Stimulate Insulin release in glucose dependent manner) | 37C for 2 hours | 200 µg/ml | ~34 | DPP IV | MALDI-TOF-MS | Peptide in 0.01 M Na2HPO4 buffer | in vitro | None | None | In the DPP-IV-free rat pancreatic beta cell line RINm5F GLP-1-(7-34)-amide elevated cAMP production with an EC50 of about 40 nM | |||
| 1911217 | 1991 | CGRP (Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Not mentioned | 300-600pmol | 9.00 (plasma half-life) | Proteases from Human plasma | Not mentioned | Human Plasma | in vivo | None | None | Not reported | |||
| 2991517 | 1985 | Compound 16 (Ketomethylene pentapeptide analogue) | 4 | Cbc=Cyclobutanecarboxylic acid | Free | Linear | L | Proline ring is tritiated | Pentapeptide analogue of the ketomethylene-containing angiotensin converting enzyme (ACE) inhibitor | Angiotensin converting enzyme (ACE) inhibitor and anti-hypertensive | Not mentioned | 2mg | 24.4 | Proteases from rat blood | Liquid scintillation spectrometer | (Dose i/v injected) Rat blood | in vivo | None | None | Potent ACE-inhibitor with I50 =7.0nM | |||
| 2991517 | 1985 | Compound 1 (Ketomethylene pentapeptide analogue) | 1 | 5(S)-benzamido-4-oxo-6-phenylhexanoyl | Free | Linear | L | Proline ring is tritiated | Pentapeptide analogue of the ketomethylene-containing angiotensin converting enzyme (ACE) inhibitor | Angiotensin converting enzyme (ACE) inhibitor and anti-hypertensive | Not mentioned | 2mg | 11.6 | Proteases from rat blood | Liquid scintillation spectrometer | (Dose i/v injected) Rat blood | in vivo | None | None | Potent ACE-inhibitor with I50 =70nM | |||
| 16197609 | 2005 | PCK3145 (Prostate secretory protein 94 derived peptide) | 15 | Free | Free | Linear | L | None | Prostate secretory protein 94 (PSP94) derivative | Anti cancer | Not mentioned | 5-80mg/m2 | Mean Elimination half life: 0.35-1.45 (Mean Elimination half life) | Proteases from Human plasma | Not mentioned | Human plamsa | in vivo | http://www.drugbank.ca/drugs/DB04985 | None | Not reported | |||
| 20158487 | 2010 | PEG10kDa-[(123)I]-CCK-10 | 10 | Free | Amidation | Linear | L | SO3H Group at Tyr-4, Coupled to PEG(10KDa), PEG=Polyethylene glycol, CCK-10=Cholecystokinin | Peptide Hormone produced by small intestine | Stimulates the digestion of fat and protein | Not mentioned | Not available | 15 | Rat blood proteases | HPLC | Rat blood | in vivo | None | None | Not reported | |||
| 20221650 | 2010 | R1(NH2GR11) (An arginine-rich cell permeable peptide) | 15 | Cu-DOTA (DOTA=1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid) | Free | Linear | L | Cu-labelled | Derived from prostate cancer cell lines, an arginine-rich cell permeable peptide | Cell permeable peptide | Not mentioned | Not available | 10.7 | Proteases from mouse blood | Fluorescence Imaging | Mouse blood | in vivo | None | None | In PC3, LNCaP, PZ-HPV-7, DU145 and DU145, FITC-NHGR11 displayed much higher uptake efficiency | |||
| 20221650 | 2010 | R1(NH2GR11) (An arginine-rich cell permeable peptide) | 15 | Cu-DOTA (DOTA=1,4,7,10- tetraazacyclododecane-1,4,7,10-tetraacetic acid) | Free | Linear | L | Cu-labelled | Derived from prostate cancer cell lines, an arginine-rich cell permeable peptide | Cell permeable peptide | Not mentioned | Not available | 17.2 (Elimination half life) | Proteases from mouse blood | Fluorescence Imaging | Mouse blood | in vivo | None | None | In PC3, LNCaP, PZ-HPV-7, DU145 and DU145, FITC-NHGR11 displayed much higher uptake efficiency | |||
| 2624887 | 1989 | CC-2 (Corpora cardiaca) | 8 | Free | Amidation | Linear | L | pyr-Glu= Pyro-Glutamic acid | Hypertrehalosaemic hormone in cockroaches | Activate fat body glycogen phosphorylase and increase haemolymph trehalose | 2 hours | 1-2pmol | 13.2 | Proteases from Haemolymph of american cockroach | Not mentioned | Haemolymph of american cockroach | in vivo | None | None | Increase in carbohydrates in haemolymph; simulates activation of glycogen phosphorylase and induction of trehalose synthesis | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 4 IU rhGH/m2 BSA | 18 | Proteases from Human serum | Radioimmunoassay | (Intravenous route of injection) human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 4 IU rhGH/m2 BSA | 2.59 ±1.32 | Proteases from Human serum | Radioimmunoassay | (Subcutaneous route of injection) human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 10 IU rhGH/m2 BSA | 4.29 ±1.89 | Proteases from Human serum | Radioimmunoassay | (Subcutaneous route of injection) human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 1490668 | 1992 | rhGH(Recombinant DNA derived human growth hormone) | 191 | Free | Free | Linear | L | None | Recombinant DNA derived human growth hormone | Promotes growth and development | Not mentioned | 4 IU rhGH/m2 BSA | 6.06 ±2.64 | Proteases from Human serum | Radioimmunoassay | (Intramuscular route of injection)human serum | in vivo | None | None | In a GH-deficient child, hGH serum levels between 10 and 20 ng/ml were demonstrated for a period of 8 h after s.c. administration of 0.07 IU rhGH/kg body weight. | |||
| 6361234 | 1983 | Amphibian bombesin | 14 | Free | Amidation | Linear | L | Pyr=Pyro-glutamine | Skin of the frog Bombina bombina | Insulinotropic agent | Not reported | 5 pmol/kg . min for 30 min and a volume of 1 ml/min. | 3 | Calf blood proteases | Radioimmunoassay | Arterial blood sample of pedigree jersey calves | in vivo | 18185064 | None | Not mentioned | |||
| 6361234 | 1983 | Porcine gastrin releasing peptide | 27 | Free | Amidation | Linear | L | None | Gastrin releasing peptide | Stimulates the release of Gastrin | Not reported | 5 pmol/kg . min for 30 min and a volume of 1 ml/min. | 3 | Calf blood proteases | Radioimmunoassay | Arterial blood sample of pedigree jersey calves | in vivo | 18185064 | None | Not mentioned | |||
| 10377427 | 1999 | ANP ( Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Cardiac atria | cardiovascular homeostasis | Blood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide | 0.2 µci/mouse of [125I]ANP | 1.44 ±0.05 | Npr3+/+ mice blood proteases | Radioimmunoassay | Npr3+/+ mice blood sample | in vivo | 6230082 | None | Blood pressure=118.7 ±1.9 mmHg | |||
| 10377427 | 2000 | ANP ( Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Cardiac atria | cardiovascular homeostasis | Blood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide | 0.2 µci/mouse of [125I]ANP | 2.4 ±0.08 | Npr3-/- mice blood proteases | Radioimmunoassay | Npr3-/- mice blood sample | in vivo | 6230082 | None | Blood pressure=110.4 ±2.3 mmHg | |||
| 2939312 | 1986 | α-hANP (Alpha human atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Human atrial extracts | Natriuretic and hypotensive actions | Venous samples were drawn at 1 mln intervals for 10 mlns after injectlon and then at 15 and 30 mlns. | 100 µg | 2.5 | Human blood proteases | Radioimmunoassay | Intravenous bolus injection of 100μg alpha human atrial natriuretic factor in human | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 100μg/kg | 8.4 ±4(t1/2α) | Diestrous female rats blood proteases | Radioimmunoassay | Intravenous injection in diestrous female rats | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 100μg/kg | 33.2 ±6.8(t1/2β) | Diestrous female rats blood proteases | Radioimmunoassay | Intravenous injection in diestrous female rats | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 10 µg | 32(t1/2β) | Pregnant female rats blood proteases | Radioimmunoassay | Subcutaneous injection in pregnant rats | in vivo | 3083092 | None | Not mentioned | |||
| 12083977 | 2002 | GnRH (Gonadotropin-releasing hormone) | 10 | PyroGlu=Pyroglutamic acid | Free | Linear | L | pGlu=pyroglutamic acid | Hypothalamic neurons | Regulating the synthesis and secretion of the gonadotropins luteinising hormone (LH) and follicle-stimulating hormone (FSH). | Not mentioned | Not mentioned | less than 15 | Human plasma proteases | Radioimmunoassay | Human blood | in vivo | None | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.17 ±0.05 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Breast fed healthy infants(0-1years)serum sample | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.48 ±0.007 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Formula fed healthy infants(0-1years)serum sample | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.26 ±0.06 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of healthy infant boys(0-1 years) | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.51 ±0.08 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of healthy infant girls(0-1 years) | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.37 ±0.05 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of children(0-1 years) | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 3.10 ±0.05 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of adults | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 19023544 | 2008 | TP5 (Thymopentin) | 5 | Free | Free | Linear | L | None | Synthetic peptide of thymic hormone | Immunomodulator | Not mentioned | Not mentioned | 5.6 ±0.7 | Rabbit plasma proteases | HPLC | heparinized rabbit plasma | in vitro | http://www.drugbank.ca/drugs/DB00112 | None | IL2 concentration in mouse serum:0.65pg/ml,macrophage clearance index(K value)=0.0132 ±0.0008,phagocytic index(α value=3.43 ±0.29. | |||
| 20382695 | 2010 | hGLP-1[7-36] (Human glucagon like peptide-1) | 30 | Free | Amidation | Linear | L | None | Incretin released by intestinal L cells | Metabolism regulation | 1 hour | 40 nm(1μg/μl upto 500μl) | 50 | Rat blood proteases | HPLC | Rat blood plasma | in vitro | http://www.drugbank.ca/drugs/DB00113 | None | cAMP stimulation,EC50=0.08nM | |||
| 21036718 | 2010 | 177Lu-AMBA | 9 | 177Lu,DO3A-CH2CO-G-(4-aminobenzoyl) | Amidation | Linear | L | None | Synthetic Bombesin like peptide | Clinical trials for use as systemic radiotherapy for hormone refractory prostate cancer (HRPC) patients. | Not mentioned | 10μg/mouse | 0.52 ±0.05(t1/2α) | Mice plasma proteases | Radio-HPLC | Intravenous injection in PC-3M-luc-C6 tumour-bearing mice | in vivo | http://www.drugbank.ca/drugs/DB00138 | None | In vitro stability =24.3 ±21.9% after 48 hours | |||
| 21986100 | 2011 | DALCE [(D-Ala2, Leu5, Cys6)-enkephalin] | 6 | Free | Free | Linear | Mix | None | Enkephalin derative | Treatment of ischemia | Not mentioned | 1mg/Kg | 9.1 ±2.4 | Rats plasma proteases | LC-MS | Intravenous injection in male Sprague €“Dawley rats | in vivo | http://www.drugbank.ca/drugs/DB00142 | None | Not mentioned | |||
| 21986100 | 2011 | DADLE [(D-Ala2, Leu5)-enkephalin] | 5 | Free | Free | Linear | Mix | None | Opoid peptide | Neuromodulator | Not mentioned | 1mg/Kg(200-250μl) | 4.6 | Rats plasma proteases | HPLC with tandem LC/MS/MS | Rat plasma | in vivo | http://www.drugbank.ca/drugs/DB00143 | None | Not mentioned | |||
| 21986100 | 2011 | CMD-Cys-DALCE | 6 | Free | Thiolated carboxymethyl dextran(CMD) cysteine conjugated via disulfide bond | Linear | Mix | None | Enkephalin derative | Treatment of ischemia | Not mentioned | 4.5 mg/kg corresponding to 1 mg/kg of DALCE | 56 ±6.0 | Rats plasma proteases | LC-MS | Intravenous injection in male Sprague €“Dawley rats | in vivo | http://www.drugbank.ca/drugs/DB00144 | None | Not mentioned | |||
| 22770564 | 2012 | HR2 (wild type) [HR2 regions of the HIV-1 envelope glycoprotein gp41] | 41 | Free | Free | Linear | L | None | HR2 regions of the HIV-1 envelope glycoprotein gp41 | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 37.2 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00145 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=1.5 ± 0.1nM | |||
| 22770564 | 2012 | N-terminus of HR2 | 42 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.6 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00146 | None | Not mentioned | |||
| 22770564 | 2012 | N-terminus-PEG750 of HR2 | 42 | Pegylation-PEG750 | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 40 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00147 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=7.2 ± 0.7nM | |||
| 22770564 | 2012 | R4C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 37.4 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00149 | None | Not mentioned | |||
| 22770564 | 2012 | R4C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 4th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 44.1 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00150 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.1 ± 1.1nM | |||
| 22770564 | 2012 | S11C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.9 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00152 | None | Not mentioned | |||
| 22770564 | 2012 | S11C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 11th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 50.2 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00153 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.4 ± 0.8nM | |||
| 22770564 | 2012 | S15C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 39.9 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00155 | None | Not mentioned | |||
| 22770564 | 2012 | S15C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 15th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 53.7 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00156 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.1 ± 1.0nM | |||
| 22770564 | 2012 | E18C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.4 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00158 | None | Not mentioned | |||
| 22770564 | 2012 | E18C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 18th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 50.3 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00159 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.5 ± 1.0nM | |||
| 22770564 | 2012 | N22C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.9 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00161 | None | Not mentioned | |||
| 22770564 | 2012 | N22C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 22nd position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 51.8 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00162 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.2 ± 0.9nM | |||
| 22770564 | 2012 | Q29C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.6 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00164 | None | Not mentioned | |||
| 22770564 | 2012 | Q29C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 29th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 58.1 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00165 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.2 ± 0.8nM | |||
| 22770564 | 2012 | C terminus derivative of HR2 | 42 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 39 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00167 | None | Not mentioned | |||
| 22770564 | 2012 | S20C derivative of HR2 | 41 | Free | Pegylation (PEG2000) | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.6 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00170 | None | Not mentioned | |||
| 22770564 | 2012 | S20C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 20th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 42 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00171 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)>400 | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 6 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 100 μg/kg of the body weight | 0.14 ±0.03(t1/2α) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00173 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 8 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 200 μg/kg of the body weight | 0.15 ±0.06(t1/2α) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00175 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 10 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 400 μg/kg of the body weight | 0.09 ±0.01(t1/2α) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00177 | None | Not mentioned | |||
| 23196806 | 2012 | TAMRA-TAT [5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT] | 11 | 5-(and-6)-carboxytetramethylrhodamine(TAMRA) | Free | Linear | L | None | HIV | Cell penetrating peptide | Not mentioned | 60 μg/g | 6.7 | Modified simulated intestinal fluid with pancreatic enzymes | HPLC with fluorescence detection | Modified simulated intestinal fluid | in vitro | http://www.drugbank.ca/drugs/DB00179 | None | Fluorescence intensity (intestinal delivery)=4.0×105 in Duodenum, 6.0×105 in Jejunum, 4.0×105 in Ileum, 1×105 in Colon | |||
| 23196806 | 2012 | TAMRA-TAT microemulsion | 11 | 5-(and-6)-carboxytetramethylrhodamine(TAMRA) | Free | Linear | L | None | HIV | Cell penetrating peptide | Not mentioned | Microemulsion composition: Miglyol 812/Capmul MCM/Tween 80/TAMRA-TAT solution at the weight ratio of | 19.4 | Modified simulated intestinal fluid with pancreatic enzymes | HPLC with fluorescence detection | Modified simulated intestinal fluid | in vitro | http://www.drugbank.ca/drugs/DB00180 | None | Fluorescence I ntensity (intestinal delivery)< 1.0×105 in Duodenum, Jejunum, Ileum, Colon | |||
| 1213660 | 1975 | Procine Proinsulin | 84 | Free | Free | Cyclic (C7-C70,C19-C83,C69-C74) | L | None | Proinsulin | Not mentioned | Not reported | 5-8.6 µg/kg were injected. | 8.2 ±0.3 | Porcine blood proteases | Radioimmunoassay | Porcine blood | in vivo | http://www.drugbank.ca/drugs/DB00186 | None | Not reported | |||
| 1213660 | 1975 | Procine C-Peptide | 34 | Free | Free | Linear | L | None | Proinsulin | Not mentioned | Not reported | 5-8.6 µg/kg were injected. | 9.9 ±0.5 | Porcine blood proteases | Radioimmunoassay | Porcine blood | in vivo | http://www.drugbank.ca/drugs/DB00187 | None | Not reported | |||
| 7787827 | 1994 | 125I-β-NGF | 120 | Free | Free | Cyclic (3 disulphide bonds between C15-C80, C58-C108, C68-C110) | L | None | β-nerve growth factor | Nerve growth promoting peptide | Blood samples (250 µl) were obtained from the catheterized carotid artery 15, 30, 45 and 60 min afte | 800 000 cpm of 125I-7S-NGF or 125I-β-NGF (diluted in 200 µl of saline) | 36.3 + 2.20 | Rats blood proteases | Column chromatography | Intravenouly injected in adult male Wistar rats | in vivo | http://www.drugbank.ca/drugs/DB00188 | None | Not reported | |||
| 7962302 | 1994 | GHRH | 29 | Free | Amidation | Linear | L | None | Synthetic | Growth hormone-releasing hormone (GHRH) stimulates growth hormone (GH) gene transcription, synthesis, and secretion of growth hormone via growth hormone-releasing hormone receptor (GHRH-R) | Blood samples were obtained at 5 min intervals for measurement of serum GH concentrations and at the | Intravenous dose of 1 µg/kg followed by a 15 min infusion of saline in human subjects. | 18.5 ±0.8 | Human blood proteases | Immunoradiometric assay (IRMA) | Human blood | in vivo | http://www.drugbank.ca/drugs/DB00189 | None | Not reported | |||
| 7899230 | 1994 | Leucine enkephalin | 5 | Free | Free | Linear | L | None | Leucine enkephalin | Opioid peptide | Not reported | 0.63 mg/ml | 40 | Sheep nasal wash fluid proteases | HPLC | Sheep nasal wash fluid | in vitro | http://www.drugbank.ca/drugs/DB00190 | None | Not reported | |||
| 7899230 | 1994 | Leucine enkephalin | 5 | Free | Free | Linear | L | None | Leucine enkephalin | Opioid peptide | Not reported | 20 µg/ml | 12 | Sheep nasal mucosal proteases | HPLC | Sheep nasal mucosal tissue homogenate | in vitro | http://www.drugbank.ca/drugs/DB00191 | None | Not reported | |||
| 7899230 | 1994 | des-tyrosine leucine enkephalin | 4 | Free | Free | Linear | L | None | des-tyrosine leucine enkephalin | Opioid peptide | Not reported | 0.63 mg/ml | 13 | Sheep nasal wash fluid proteases | HPLC | Sheep nasal wash fluid | in vitro | http://www.drugbank.ca/drugs/DB00192 | None | Not reported | |||
| 7899230 | 1994 | des-tyrosine leucine enkephalin | 4 | Free | Free | Linear | L | None | des-tyrosine leucine enkephalin | Opioid peptide | Not reported | 20 µg/ml | 7 | Sheep nasal mucosal proteases | HPLC | Sheep nasal mucosal tissue homogenate | in vitro | http://www.drugbank.ca/drugs/DB00193 | None | Not reported | |||
| 8100840 | 1993 | Somatostatin (SOM) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Synthetic | Growth hormone inhibiting hormone (GHIH) | Not reported | Not reported | <5 | Rats blood proteases | Not mentioned | Rats plasma | in vivo | http://www.drugbank.ca/drugs/DB00194 | None | Not reported | |||
| 8100840 | 1993 | Neuropeptide Y | 36 | Free | Amidation | Linear | L | None | Neuropeptide | Stimulation of the right cardiac sympathetic nerve | Not reported | Not reported | 21 | Dogs blood proteases | Not mentioned | Dogs plasma | in vivo | http://www.drugbank.ca/drugs/DB00195 | None | Not reported | |||
| 8082705 | 1994 | Facteur thymique serique (FTS) | 9 | Free | Free | Linear | L | None | Thymic peptide hormone | Suppressed hyperglycemia | Not reported | Not reported | 2 to 3 | Rats blood proteases | Radioimmunoassay | Intravenouly injected in male Wistar rats | in vivo | http://www.drugbank.ca/drugs/DB00196 | None | Plasma glucose in FTS-treated group=15.7 ± 1.8 (mmol/l)while in control Plasma glucose=28.3 ±2.1 ( µmol/l) | |||
| 8035644 | 1994 | Adrenomedullin (ADM) | 52 | Free | Free | Linear | L | None | Synthetic | Hormone in circulation control | Not reported | Intraarterial doses of 0.01-0.3 nmol | 55 to 80 | Cat blood proteases | HPLC | Hind limb vascular bed of the cat | in vivo | http://www.drugbank.ca/drugs/DB00197 | None | Not reported | |||
| 8035644 | 1994 | ADM 15-22 | 8 | Free | Free | Linear | L | None | Carboxy terminal 15-52 fragment of adrenomedullin | An inhibitor of the cellular actions of adrenomedullin | Not reported | Intraarterial doses of 0.01-0.3 nmol | 55 to 80 | Cat blood proteases | HPLC | Hind limb vascular bed of the cat | in vivo | http://www.drugbank.ca/drugs/DB00198 | None | Not reported | |||
| 17204551 | 2007 | Rat Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 0 - 60 minutes | 10 μg | 22 ±2 | Protease from rat plasma | Radioimmunoassay | Intravenous injection of peptide into Sprague Dawley rats | in vivo | None | None | Co-administration of obestatin with ghrelin inhibited food intake. | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 19 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 53 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + P8340 protease inhibitor cocktail | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 39 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + EDTA | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 20.5 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + Soybean trypsin inhibitor | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 20.5 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + APMSF | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 24 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + 1,10-Phenanthrolin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 20 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + Captopril | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 17 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + Chymostatin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 27 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 38.5 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + Soybean trypsin inhibitor | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 16 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate+ APMSF | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 28 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + 1,10-Phenanthrolin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 28 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + Captopril | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 29.5 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate+ Chymostatin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.4 | 90 μg | 42.2 [40.5, 44.0] | Proteases from mouse plasma | HPLC, LC-UV/MS | Mouse plasma | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.5 | 90 μg | 12.6 [11.4, 14.1] | Proteases from Mouse liver homogenate | HPLC, LC-UV/MS | Mouse liver homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.6 | 90 μg | 30.0 [27.8, 32.6] | Proteases from Mouse stomach homogenate | HPLC, LC-UV/MS | Mouse stomach homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.10 | 90 μg | 13.3 [12.7, 14.0] | Proteases from mouse liver homogenate | HPLC, LC-UV/MS | Mouse liver homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.11 | 90 μg | 28.0 [25.8, 30.5] | Proteases from mouse liver homogenate+protease inhibitor cocktai | HPLC, LC-UV/MS | Mouse liver homogenate with protease inhibitor cocktail | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mono-iodinated human obestatin | 23 | Free | Amidation | Linear | L | Iodination at tyr16 | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.12 | 90 μg | 15.1 [9.1, 45.0] | Proteases from Mouse liver homogenate | HPLC, LC-UV/MS | Mouse liver homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 2.1 (α half life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 10.0 (β half life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 3.6 (α half-life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 8353280 | 1993 | Interleukin-3 (IL-3) | 140 | Free | Free | Cyclic (C17-C80,C79-C140) | L | Glycosylation at 84thand 112th position | IL3 is produced by activated T lymphocytes, activated mast cells, and eosinophils and neutrophils | Hematopoietic growth factor | Not mentioned | 1,000 biologic units | 30.8 (β half life) | Balb/c mice blood proteases | ELISA | Injected intravenously in Balb/c mice blood | in vivo | http://www.uniprot.org/uniprot/P01586 | None | Mice treated with IL3 had megakaryocyte frequency=0.9 ±0.21 per high-power field while saline control had 1.4 ±0.33 per high-power field | |||
| 19115392 | 2009 | Interleukin-1 Receptor Antagonist (IL-1ra) | 152 | Free | Free | Cyclic(66-116) | L | Glycosylation at 84th position | Interleukin-1 Receptor Antagonist | The natural specific receptor antagonist (IL-1ra) binds to IL-1RI but does not initiate signaling as it does not engage the IL1R accessory protein and therefore acts as a receptor antagonist. | Not mentioned | Not mentioned | 6 to 15 | Rats blood proteases | Not mentioned | Rat blood | in vivo | http://www.uniprot.org/uniprot/P25086 | None | Significant depression of LTP in the group of animals that received intracerebroventricular injection of Aβ-peptide (1 €“40) compared with control animals injected with vehicle. | |||
| 38789061 | 2024 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 0.5 ± 0.1 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38737283 | 2024 | ABD035-immunoGN | N.A. | P1h3 | His-tag | Linear | L | Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N | Synthetic | Antitumor | Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min | 0.1 μmol/kg | 35.22 | BALB/c mice serum protease | ELISA | BALB/c mice serum | In Vivo | None | None | Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation | |||
| 38737283 | 2024 | immunoGN | N.A. | P1h3 | His-tag | Linear | L | Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N | Synthetic | Antitumor | Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min | 0.1 μmol/kg | 4.599 | BALB/c mice serum protease | ELISA | BALB/c mice serum | In Vivo | None | None | Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation | |||
| 38737283 | 2024 | dAb7h8-immunoGN | N.A. | P1h3 | His-tag | Linear | L | Humanized anti-HER2 scFv P1h3, albumin-binding peptides (ABD035 or dAb7h8), cathepsin B-cleavable peptide B2, endosome-disruptive peptide E5C3 fusion protein, GN= Gasdermin-N | Synthetic | Antitumor | Blood samples were promptly collected at 5, 10, 30, 60, 360, and 720 min | 0.1 μmol/kg | 31.25 | BALB/c mice serum protease | ELISA | BALB/c mice serum | In Vivo | None | None | Cytotoxicity of ABD035-immunoGN in N87 cells reached as high as 62 %, compared to 38 % for immunotBid after 24 h of incubation | |||
| 38613996 | 2024 | PepH3 | 7 | Free | Amidation | Linear | L | None | Synthetic | Anticancer | At different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C | 1 mM | 21.00 ± 2.91 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | IC50 > 100.0 for TNBC MDA-MB-231 Monolayer | |||
| 38493673 | 2024 | Peptide ALW | 12 | Free | Free | Linear | L | None | Synthetic | Alleviating Lupus Nephritis | N.A. | 12.5 mg/kg | 0.315 (Elimination Half Life) | Cd1 mice plasma protease | N.A. | CD1 mice plasma | In Vivo | None | None | KD(M) = 1.99*10-4 (Binding affinity of peptides to anti-dsDNA IgG3) | |||
| 38312052 | 2024 | Maraciclatide (99mTc) | 7 | Acetylation | Free | Cyclic(Ac-Cys8 Bond, Cys2-Cys6 Disulfide Bond) | L | Radiolabelled with technetium, X= Unknown Structure | synthetic | Novel Diagnostic Imaging Agent For A Range Of Pathological Conditions | Blood and plasma samples were collected at 10 min, 30 min, 1 h, 2 h, 4 h, 8 h, 24 h, 48 h, 72 h, and 7 days post-administration | The data acquired from all participants who received 99mTc-maraciclatide within the expected clinical range (15, 75 µg, 150) were pooled | 1 (Terminal Elimination Half Life) | Human Plasma Protease | Gamma counter | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/73050806 | None | N.A. | |||
| 38104907 | 2024 | [Al18F]NODA-MPAA-HTA | 8 | Conjugating 18F nuclide with a modified KE108 peptide, MPAA modification at N terminal | The amino group of KE108 peptide conjugated with the carboxyl group of NODA | Cyclic(d-Dab2-Phe8) | Mix | D-Tryp amino acid substituition, d-Dab = Diaminobutyric acid | 18F-radiolabeled somatostatin analogue | Used for PET imaging of Neuroendocrine tumors (NETs) | Blood samples were collected from the retroorbital plexus into capillary at 5, 10, 15, 30,60 and 120 min | N.A. | 37.63 ± 13.05 (Elimination Half Life) | BALB/c mice blood protease | Gamma counter | BALB/c mice blood sample | In Vivo | None | None | Affinity of [Al18F]NODA-MPAA-HTA (Kd = 8.77 ± 1.14 nM, n = 4) | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 0.1 mg/kg | 3.49 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 1 mg/kg | 3.34 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 10 mg/kg | 7.64 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 0.1 mg/kg | 18.8 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 1 mg/kg | 10 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 10 mg/kg | 10.2 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 8.4 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.33 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.66 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 14 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.11 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 14 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 7 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 8 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.67 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.85 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.8 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.16 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.31 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.04 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.68 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.83 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 6.59 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.66 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.01 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 5.7(Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.05 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.13 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.09 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.41 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 6 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.9 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 100μg/kg | 1.15 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 150 μg/kg | 1.15 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 50 μg/kg | 1.38 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 100μg/kg | 2.18 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 140 μg/kg | 1.94 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 200 μg/kg | 1.94 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 250 μg/kg | 1.88 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| 38863646 | 2024 | (89Zr, Mn)-WPMNs | N.A. | Free | Free | Linear | L | Mn and 89Zr labeling, MNPs modified with WL12-SH | WL12 derivative | Targets PD-L1 | Blood samples were collected from orbital vein at 1, 3, 5, 10, 15, 20, 30, 45 min and 1, 1.5, 2, 3, 4, 14, 24, 48, 72, 96 h | 0.5 mg/ml | 0.1234 (Fast) (Metabolic Half Life) | KM mouse blood protease | Radioactivity assay using γ-counter | KM mouse blood | In Vivo | None | None | N.A. | |||
| 38027063 | 2023 | ScFv9 | 304 | Free | Free | Linear | L | Biotinylation | The scFv9 sequence is derived from an antibody fragment to target amyloid beta (Aβ) | Treatment of AD and Parkinson disease | Plasma was collected at 0, 2, 4, 8, and 24 h after injection | 250 μg | 0.74 | TgCRND8 mice plasma protease | Direct ELISA | TgCRND8 mice plasma | In Vivo | None | None | N.A. | |||
| 37880318 | 2023 | L3 | 15 | Free | Amidation | Linear | L | None | Derived from calcitermin | Antimicrobial | 37 °C | 0.0001 M | 20 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 189 ± 23 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation) | |||
| 37880318 | 2023 | Wild-type Calcitermin (WT) | 15 | Free | Free | Linear | L | None | C-terminal cleavage fragment of calgranulin C | Antimicrobial | 37 °C | 0.0001 M | 18 ± 3 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 28 ± 15 for 0.032 mg/mL peptide concentration (0.1 mL of microbial suspension after 24 hours of incubation at 37°C) (Effect of peptide derivatives on Candida albicans (ATCC 10231) proliferation) | |||
| 37875481 | 2023 | IL-15-Cy7 | N.A. | Free | Free | Linear | L | Cy7 | Derived from Interleukin-15 | Antitumor | The blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h) | N.A. | 0.69 | Mice blood protease | Fluorescence spectrophotometry | Mice blood | In Vivo | None | None | Not mentioned | |||
| 37397495 | 2023 | Peptide | 9 | Free | Free | Linear | L | Removing an Asp residue | Isolated from Merluccius productus fish protein hydrolysate | Inhibits BACE-1 | Blood was taken after 0, 5, and 30 min and 2, 6, and 24 h after injectio | 4 mg/kg | 0.69 | Mouse plasma protease | Mass spectrometry | Mouse plasma | In Vivo | None | None | Ki(µM)= 0.0940 BACE-1 activity with peptide which has reduced activity due to inhibition by peptide | |||
| 37390979 | 2023 | BI-3434 | 33 | Free | Amidation | Linear | L | Lys33 conjuagted with HLE (fatty acid based half life extension group),Substituting Ser with 2-aminoisobutyric acid (Aib) at position 2 | Lipidated secretin analog | Secretin receptor agonist | N.A. | 30 nmol/kg | <15 | Male NMRI mice plasma protease | Mass spectrometry | Male NMRI mice plasma (Non fasted) | In Vivo | None | None | EC50 =15.5 pM for BI-3434 | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 54.6 | Beagle dogs plasma protease | Triple Quadrupole Mass spectrometry | Beagle dogs plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 52.7 | Cynomolgus monkeys plasma protease | Triple Quadrupole Mass spectrometry | Cynomolgus monkeys plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 5.68 | CD-1 mouse plasma protease | Triple Quadrupole Mass spectrometry | CD-1 mouse plasma | In Vitro | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | 2.72 | Intestinal fluid protease | Triple Quadrupole Mass spectrometry | Simulated Intestinal Fluid (SIF) at pH = 5.5 | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 32.5 | CD-1 mouse Liver Microsomes protease | LC-MS/MS | CD-1 mouse Liver Microsomes | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 27.7 | SD rats Liver Microsome Protease | LC-MS/MS | SD rats Liver Microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 33 | Beagle dogs Liver Microsome Protease | LC-MS/MS | Beagle dogs Liver Microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 21.8 | Cynomolgus monkeys Liver Microsome Protease | LC-MS/MS | Cynomolgus monkeys Liver microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15,30, 60, 90, and 120 minutes), samples were removed for analysis | 2 μM (0.5 mg protein/mL of each species pooled together) | 20.3 | Human Liver Microsome protease | LC-MS/MS | Human Liver Microsome | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | <15 | CD-1 mouse Hepatocytes Lysate Protease | LC-MS/MS | CD-1 mouse Hepatocytes Lysate | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.81 | SD rats Hepatocytes Lysates protease | LC-MS/MS | SD rats hepatocytes Lysates | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 10.7 | Beagle dogs Hepatocytes Lysates protease | LC-MS/MS | Beagle dogs Hepatocytes Lysates | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 12.1 | Cynomolgus monkeys Hepatocytes Lysates protease | LC-MS/MS | Cynomolgus monkeys Hepatocytes Lysates | In Vitro | None | None | N.A. | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.28 | Human Hepatocytes Lysates protease | LC-MS/MS | Human Hepatocytes | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.28 | Human Hepatocytes Lysates protease | LC-MS/MS | Human Hepatocytes Lysates | In Vitro | None | None | Enzyme Activity = 3.18 at 2 microMolar of HM1010 (Cytochrome P450 (CYP2B6) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | At the assay points (time zero, 15, 30, 60,120, and 180 minutes), samples were removed for analysis | 2 μM (0.5 million cells/mL, of each species pooled together) | 5.28 | Human Hepatocytes Lysates protease | LC-MS/MS | Human Hepatocytes Lysates | In Vitro | None | None | Enzyme Activity = 2.06 at 2 microMolar of HM1010 (Cytochrome P450 (CYP3A4) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37094132 | 2023 | SNIO–CBP | 16 | Single nanometer iron oxide and PEG conjugation at N terminal | Amidation | Cyclic (C5-C14 Disulfide Bond) | L | None | SINO-CBP product | Used in detection of Liver Fibrosis | N.A. | 2 nmol/g animal | 5.7 ± 1.9 (Elimination Half Life) | Mice blood protease | Dynamic T1-weighted MRI | Mice blood | In Vivo | None | None | Kd = 18.4 µM (Binding affinity of SNIO–CBP toward human type I collagen) | |||
| 37073494 | 2023 | Carmo‐HrTH‐I | 10 | pGlu = Pyroglutamate | Amidation | Linear | L | C‐mannosylated tryptophan residue at position 8 | Derived from the corpora cardiaca (CC) of the Indian stick insect Carausius morosus | Hypertrehalosemia In Ligated Stick Insects | 0, 2‐, 5‐, 10‐and 30 min at Room temp | 100 pmol | 5 | C.Morosus hemolymph protease | HPLC | C.Morosus hemolymph | In Vitro | None | None | [Lipid]T0 min(µg/µL) = 9.32 ± 1.59 for Natural Carmo‐HrTH‐I (10 pmol) (Biological activity of a crude methanolic extract of corpora cardiaca (CC) from the natural hypertrehalosemic hormones (HrTHs) extracted from the CC of the Indian stick insect(Carausius morosus) in an in vivo bioassay withL. migratoria) | |||
| 37047588 | 2023 | B7-33 | 27 | Free | Free | Linear | L | None | Derived as a single-chain peptidomimetic of the B-chain of H2 relaxin | Treatment of Acute Cardiac Failure | A total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min) | 400 µg/mL | 6 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | HEK-7BP Binding B.S.A. Free Eu-H2 pKi = 7.28 ± 0.11 | |||
| 37047588 | 2023 | AcK(PalmGlu)-PEG12-B7-33 | 27 | Ac modifed Lysine in Palmitic fatty acid linked with B7-33 using PEG linker | Free | Linear | L | None | B7-33 analog | Treatment of Acute Cardiac Failure | A total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min) | 400 µg/mL | 60 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | HEK-7BP Binding B.S.A. Free Eu-H2 pKi =7.52 ± 0.13 | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1.5 mg/kg | 0.306 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 4.5 mg/kg | 0.344 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 13.5 mg/kg | 0.547 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.805 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.248 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.46 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.437 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.341 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.391 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.665 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 1 mg/kg | 0.668 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.655 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.648 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.615 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 75 mg/kg | 0.62 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 5 mg/kg | 0.888 | Monkeys Plasma Protease | LC-MS/MS | Monkeys plasma | In Vivo | None | None | N.A. | |||
| 36982773 | 2023 | CEND-1 | 9 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | iRGD cyclic peptide | Antitumor | Blood samples were collected for pharmacokinetic evaluations pre-dose and at 1, 5, 10, 15 and 30 min, and 1, 2 and 6 h post-dose in rats, dogs and monkeys, and 3, 10, 30 and 90 min, and 4 and 8 h post-dose in mice | 50 mg/kg | 0.956 | Monkeys Plasma Protease | LC-MS/MS | Monkeys plasma | In Vivo | None | None | N.A. | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | (Onc72 in 19% MHB2 medium) MIC = 12.5 μmol L−1 (29 mg L−1) on E.coli BW25113 | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | (Onc72 in 25% mouse serum ) MIC = 25 μmol L−1 (58 mg L−1) on E.coli BW25113 | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | Onc72 Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 43 | CD-1 mice plasma protease | LC-MS | CD-1 mice plasma | In Vivo | None | None | Onc72: Non-toxic to human HepG2 and HEK293 cell lines at 50 μmol L−1 | |||
| 36509220 | 2023 | KM8 | 18 | Free | Amidation | Linear | L | None | Analogue of Mastoparan | Antitumor | N.A. | N.A. | 30 | Mouse plasma protease | Plasma stability assay | Mouse plasma | In Vivo | None | None | N.A. | |||
| 36410792 | 2023 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Small Bowel Hypertrophic Effect | Blood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912 | 670 nmol/kg | 0.6 ± 0.1 | SD rats serum protease | GLP-2 ELISA | SD rats serum | In Vivo | None | None | EC50 = 0.12 ± 0.056 nM for teduglutide peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP) | |||
| N.A. | 2023 | SEQ ID NO 1 | 28 | Free | Free | Linear | L | None | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 0.2 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 0.83 | |||
| 37329900 | 2023 | KAN-101 | N.A. | N.A. | N.A. | N.A. | N.A. | Liver-targeting glycosylation signature conjugated to a deaminated gliadin peptide | N.A. | Liver-Targeted Immune Tolerance Therapy | N.A. | 0·15 mg/kg, 0·3 mg/kg, 0·6 mg/kg, 1·2 mg/kg, 1·5 mg/kg | 3·72 to 31·72 | Human protease | N.A. | Human | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration | 20 μg/kg | 15.2 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 18.5 | SD rats plasma protease | LC-MS/MS | SD rats plasma dosed with BPC once a day for seven consecutive days | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration | 20 μg/kg | 7.87 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 17.1 | SD rats plasma protease | LC-MS/MS | SD rats plasma dosed with BPC once a day for seven consecutive days | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration | 500 μg/kg | 29.7 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 6 μg/kg | 5.27 ± 2.25 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 30 μg/kg | 19.6 ± 3.72 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma with repeated dose of 30 μg/kg for seven consecutive days | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 6 μg/kg | 20.0 ± 5.53 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 30 μg/kg | 25.5 ± 7.08 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration | 150 μg/kg | 29.3 ± 5.06 | Beagle Dogs Plasma Protease | LC-MS/MS | beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | https://pmc.ncbi.nlm.nih.gov/articles/PMC7994712/ | None | IC50(nM) = 1.7 (relative affinities of CST for the different Somatostatin receptor SSTR1) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.09 (relative affinities of CST for the different Somatostatin receptor SSTR2) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.3 (relative affinities of CST for the different Somatostatin receptor SSTR3) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.2 (relative affinities of CST for the different Somatostatin receptor SSTR4) | |||
| 36559278 | 2022 | Native CST | 14 | Free | Free | Cyclic (C2-C13 Disulfide Linkage) | L | None | Neuropeptide | Antiinflammatory | 37 °C | 6 mg/mL | 2 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 0.3 (relative affinities of CST for the different Somatostatin receptor SSTR1) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 47.3 (relative affinities of A5 for the different Somatostatin receptor SSTR1) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 35 (relative affinities of A5 for the different Somatostatin receptor SSTR2) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 5.1 (relative affinities of A5 for the different Somatostatin receptor SSTR3) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 4.1 (relative affinities of A5 for the different Somatostatin receptor SSTR4) | |||
| 36559278 | 2022 | CST analogue 5 | 14 | N-octanoyl | Free | Cyclic (C2-C13 Disulfide Linkage) | Mix | w=D-Trp,Mesityl | CST analogue | Antiinflammatory | 37 °C | 6 mg/mL | 21 | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | IC50(nM) = 1.12 (relative affinities of A5 for the different Somatostatin receptor SSTR1) | |||
| 36557850 | 2022 | Leuprolide | 9 | pGlu = Pyroglutamate | NHEt (Ethylamine) | Linear | Mix | d-Leucine6 substituitions | Synthetic | Anticancer (Treatment of Advanced Prostate Cancer) | Blood sample of approximately 0.3 mL was collected via femoral artery cannulation at various time points (0, 1, 3, 5, 10, 20, 30, 60, 90, 120, 180, 240, 360, 480, and 600 min) | 0.1 mg/kg | 38.2 ± 4.3 (Terminal Elimination Half Life) | Male SD Rats Plasma Protease | UPLC-MS/MS | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 | 12 | Free | Free | Linear | L | Cysteine was introduced at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 1.7 | Human plasma protease | Flow cytometry-based functional assay and mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 | 12 | Free | Free | Linear | L | Cysteine was introduced at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 7 | Human plasma protease | Antibody-competition assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 | 12 | Free | Free | Linear | L | Cysteine was introduced in the sequence of both peptides at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 9 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 | 12 | Free | Free | Linear | L | Cysteine was introduced in the sequence of both peptides at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 6 | Human plasma protease | Functional stability assay | Human plasma after GuHCl + DTT treatment | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 | 12 | Free | Free | Linear | L | Cysteine was introduced at position 10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 5 | Human plasma protease | Mass spectrometry | Human plasma after GuHCl + DTT treatment | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (C10S) | 12 | Free | Free | Linear | L | Cys10 replaced by Ser10 | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 4 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys10 residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 5 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (C10S) | 12 | Free | Free | Linear | L | Cys replaced by Ser | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 4 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 7 µM | 3 | Human plasma protease | Mass spectrometry | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 6 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | WSC02 (C10S) | 12 | Free | Free | Linear | L | Cys replaced by Ser | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 7 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (Cdm) | 12 | Free | Free | Linear | L | Carbamidomethylation of Cys residue = Cdm | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 3 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36499357 | 2022 | JM#21 (C10S) | 12 | Free | Free | Linear | L | Cys replaced by Ser | Synthetic | Anticancer, Antiinflammatory | Five microliter aliquots were separated after 0, 5, 10, 20, 30, 45, 60, 90, and 120 min | 20 µM | 4 | Human plasma protease | Functional stability assay | Human plasma | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 1 (aka P5779) | 4 | Free | Amidation | Linear | L | None | Synthetic | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.0 ± 0.1 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 68.5 nM | |||
| 36443291 | 2022 | Entry 4 (Azapeptide 53) | 4 | Free | Aza-glutamic acid (azaE4) modification at position 4 (E4) | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.6 ± 0.11 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 396.8 nM | |||
| 36443291 | 2022 | Entry 6 (Azapeptide 55) | 4 | Aza-Phe at postion 1 | Amidation, Q amino acid subtituition at place of E at C terminal | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 24.4 ± 1.6 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 159.3 nM | |||
| 36443291 | 2022 | Entry 9 (Azapeptide 58) | 4 | Free | Amidation, Aza-glutamine (azaQ4) | Linear | L | None | P5779 analogues | Inhibitor of Hmgb1/Md-2/Tlr4 Complex Formation | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.9 ± 0.20 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | HMGb1:MD-2 inhibition (IC50) = 422.9 nM | |||
| 36443291 | 2022 | Entry 1 (Bradykinin) | 9 | Free | Free | Linear | L | None | Derived from kininogen | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 5.29 ± 0.5 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 44.4 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 2 (azaR1-BK) | 9 | Modified at position 1 with an aza-amino acid (aza-arginine) | Free | Linear | L | None | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.46 ± 0.05 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 3(azaP2-BK) | 9 | Free | Free | Linear | L | Modified at position 2 with an aza-amino acid (aza-proline) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 5.40 ± 1.1 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 61.1 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 4 (azaP3-BK) | 9 | Free | Free | Linear | L | Modified at position 3 with an aza-amino acid (aza-proline) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.63 ± 0.25 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 5 (azaG4-BK) | 9 | Free | Free | Linear | L | Modified at position 4 with an aza-amino acid (aza-glycine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 4.33 ± 1.3 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 6 (azaF5-BK) | 9 | Free | Free | Linear | L | Modified at position 5 with an aza-amino acid (aza-phenylalanine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 14.7 ± 1.6 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 7 (azaP7-BK) | 9 | Free | Free | Linear | L | Modified at position 7 with an aza-amino acid (aza-proline) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 2.38 ± 0.03 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 8 (azaF8-BK) | 9 | Free | Free | Linear | L | Modified at position 8 with an aza-amino acid (aza-phenylalanine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 39.3 ± 2.5 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 99.6 (PEG2 induction in Fibroblasts) | |||
| 36443291 | 2022 | Entry 9 (azaR9-BK) | 9 | Free | Free | Linear | L | Modified at position 9 with an aza-amino acid (aza-arginine) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 42.6 ± 0.8 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | N.A. | |||
| 36443291 | 2022 | Entry 10 ([azaP2, azaF8]-BK) | 9 | Free | Free | Linear | L | Modified at both positions 2 and 8 with aza-amino acids (aza-proline and aza-phenylalanine, respectively) | Aza-bradykinin analogues | Effects on Pain, Inflammation, Edema/Vasodilation and Blood Pressure | Aliquots (200 μL) were taken at each time point (0, 5, 10, 15, 20, 30, 60 and 120 minutes) | 0.1 mg/ml | 29.2 ± 3.8 | C57Bl/6 J mouse serum protease | LC-MS/MS | C57BL/6 J male mouse serum | In Vitro | None | None | EC50(nM) = 80.6 (PEG2 induction in Fibroblasts) | |||
| 36380917 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | 37 °C | 0.3 nmol | 10.2 ± 0.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | PDB id: 5VAI | None | BGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | 37 °C | 6 nmol | 55.7 ± 12.1 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | PDB id: 5VAI | None | BGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glc-GLP-1-1 | 31 | Free | Free | Linear | L | Glucosylation at Asn15 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 30.2 ± 2.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-3 | 31 | Free | Free | Linear | L | Glucosylation at Asn26 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 46.1 ± 3.5 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-5 | 31 | Free | Free | Linear | L | Glucosylation at Asn34 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 32.5 ± 1.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn15 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 49.1 ± 5.7 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 24.44 ± 2.37 (In vivo glucose stabilizing capability) | |||
| 36135098 | 2022 | GNRs-AAP1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 0.29 (T1/2 a) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 0.18 (T1/2 a) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36135098 | 2022 | GNRs-AAP1-2-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 0.2 (T1/2 a) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | N.A. | 1 mg/kg | 1 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse) | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | N.A. | 1 mg/kg | 0.9 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 36101452 | 2022 | AM | 52 | Free | Amidation | Cyclic (C16-C21 Disulfide Bond) | L | None | Isolated from Human pheochromocytoma | Vasodilator and Cardiovascular Protection | Blood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration | 50 nmol/kg | 32.3 | Wistar rats plasma protease | ELISA (measure mAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | AM | 52 | Free | Amidation | Cyclic (C16-C21 Disulfide Bond) | L | None | Isolated from Human pheochromocytoma | Vasodilator and Cardiovascular Protection | Blood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration | 50 nmol/kg | 27.5 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36034808 | 2022 | uPAR | 335 | Free | Free | Linear | L | None | Derived from PLAUR gene | Plays role in thrombosis | N.A. | N.A. | 48.2 ± 2.3 | BEAS-2B cells lysate protease | Densitometry analysis using NIH Image J | BEAS-2B cells lysate with UK treatment +H/R (Hypoxia/Reoxygenation) + Cycloheximide | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-Palm-3PRGD2 | 2 | Lys1 linked with (palmitoyl-Glu-OH) | Glu3 linked with (PEG4-c(RGDfK))2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between | Synthetic | Antitumor | N.A. | 0.74 MBq | 4.49 (T1/2a) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | Synthetic | Antitumor | N.A. | 0.74 MBq | 1.94 (T1/2a) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | Synthetic | Antitumor | N.A. | 0.74 MBq | 11.81 (T1/2Β) | KM mice blood protease | Gamma counter | KM mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | Synthetic | Antitumor | N.A. | 0.74 MBq | 14.54 (Slow) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-Palm-3PRGD2 | 2 | Lys1 linked with (palmitoyl-Glu-OH) | Glu3 linked with (PEG4-c(RGDfK))2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4, Lys1 and Glu2 linked with PEG4 in between | synthetic | Antitumor | N.A. | 0.74 MBq | 2.08 (Fast) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35890224 | 2022 | 177Lu-3PRGD2 | 1 | PEG4 | Glu linked with [PEG4-c(RGDfK)]2 | Cyclic (3PRGD2) | Mix | 177Lu radiolabeling at PEG4 | synthetic | Antitumor | N.A. | 0.74 MBq | 1.06 (Fast) | C57Bl/6 mice blood protease | Gamma counter | C57BL/6 mice blood sample | In Vivo | None | None | N.A. | |||
| 35807500 | 2022 | TIPP | 5 | Free | Free | Linear | L | None | From calf thymus extracts | Treatment of Asthma | At 0.5, 1, 2, 5, 10, 15, 20, and 40 min post administration (eight mice at each time points), blood samples were taken from an inner canthus | 50 mg/kg | 5.99 ± 1.82 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | TIPP inhibits degranulation and inflammation in RBL-2H3 cells and pretreatment with 200 microgram/mL of TIPP for 20 minutes reduces the level of biomarkers of allergic response and inflammation i.e β-hexosaminidase, Histamine, IL-4 | |||
| 35779189 | 2022 | NX210 | 12 | Free | Free | Linear | L | None | Derived from the subcommissural organ (SCO)-spondin | Treatment of Neurodegenerative Diseases | Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion | 2.5 mg/kg | 13.3 | Human plasma protease | HPLC–MS/MS | Human plasma | In Vivo | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3965545/ | None | N.A. | |||
| 35779189 | 2022 | NX210 | 12 | Free | Free | Linear | L | None | Derived from the subcommissural organ (SCO)-spondin | Treatment of Neurodegenerative Diseases | Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion | 5 mg/kg | 6.19 | Human plasma protease | HPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 35779189 | 2022 | NX210 | 12 | Free | Free | Linear | L | None | Derived from the subcommissural organ (SCO)-spondin | Treatment of Neurodegenerative Diseases | Blood PK samples (4 mL) for the analysis of NX210 via its metabolite NX210c were collected prior to dosing, immediately after bolus injection or termination of the infusion and at 5, 10, 15, 20, 25, 30, 70, 120, and 180 min after bolus injection or termination of infusion | 10 mg/kg | 20 | Human plasma protease | HPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.04 mmol/kg | 0.3 (Elimination Half Life) | Male SD rats plasma protease | ICP-MS | Male SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.04 mmol/kg | 0.28 (Elimination Half Life) | Female SD rats plasma protease | ICP-MS | Female SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.04 mmol/kg | 0.57(Elimination Half Life) | (P) SD rats plasma protease | ICP-MS | (P) SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.1 mmol/kg | 0.31 (Elimination Half Life) | Male SD rats plasma protease | ICP-MS | Male SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.1 mmol/kg | 0.32 (Elimination Half Life) | Female SD rats plasma protease | ICP-MS | Female SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.1 mmol/kg | 0.65 (Elimination Half Life) | (P) SD rats plasma protease | ICP-MS | (P) SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.2 mmol/kg | 0.3 (Elimination Half Life) | Male SD rats plasma protease | ICP-MS | Male SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.2 mmol/kg | 0.32 (Elimination Half Life) | Female SD rats plasma protease | ICP-MS | Female SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from jugular veins at predose and at 2, 5, 10, 15, 30, and 45 minutes and 1, 2, 3, and 4 hours after dosing from group 1 to 3 | 0.2 mmol/kg | 0.22 (Elimination Half Life) | (P) SD rats plasma protease | ICP-MS | (P) SD rats plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.04 mmol/kg | 0.76 (Elimination Half Life) | Male dogs plasma protease | ICP-MS | Male dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.04 mmol/kg | 0.74 (Elimination Half Life) | Female dogs plasma protease | ICP-MS | Female dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.04 mmol/kg | 0.8 (Elimination Half Life) | (P) dogs plasma protease | ICP-MS | (P) dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.1 mmol/kg | 0.7 (Elimination Half Life) | Male dogs plasma protease | ICP-MS | Male dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.1 mmol/kg | 0.67 (Elimination Half Life) | Female dogs plasma protease | ICP-MS | Female dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.1 mmol/kg | 0.33 (Elimination Half Life) | (P) dogs plasma protease | ICP-MS | (P) dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.2 mmol/kg | 0.69 (Elimination Half Life) | Male dogs plasma protease | ICP-MS | Male dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.2 mmol/kg | 0.63 (Elimination Half Life) | Female dogs plasma protease | ICP-MS | Female dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35703463 | 2022 | MT218 | 7 | Free | ZD2 conjugated to a clinical contrast agent gadoteridol Gd(HP-DO3A) using N3 linker | Linear | L | None | ZD2 analog | Cancer targeting contrast agent | Blood samples were collected from fore limb veins at predose and at 5, 10, 15, 30, and 45 minutes and 1, 1.5, 2, 3, 4, and 6 hours after dosing from group 1 to 3. | 0.2 mmol/kg | 0.048 (Elimination Half Life) | (P) dogs plasma protease | ICP-MS | (P) dogs plasma | In Vivo | None | None | MT218 did not inhibit the enzyme activities of CYP1A2, CYP2B6, CYP2C9, CYP2C19, CYP2D6, or CYP3A4 at concentrations up to 100 μM | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 15.3 μg/kg | 0.498 ± 0.0100 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35414877 | 2022 | Native GIP | 153 | Free | Free | Linear | L | None | Glucagon | Glucose dependent insulinotropic | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | 45 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | N.A. | |||
| 35414877 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | 35 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | PDB id: 5VAI | None | N.A. | |||
| 35359494 | 2022 | CSP1 | 17 | Free | Free | Linear | L | None | Competence stimulating peptide | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 30 | Trypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 10 for CSP1 against ComD1 receptor, EC50(nM) = 530 for CSP1 against ComD2 receptor | |||
| 35359494 | 2022 | CSP1 | 17 | Free | Free | Linear | L | None | Competence stimulating peptide | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 1 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 10 for CSP1 against ComD1 receptor, EC50(nM) = 530 for CSP1 against ComD2 receptor | |||
| 35180646 | 2022 | NPY1–36 | 36 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 4.66 ± 0.70 | Human plasma protease | LC-MS/MS | Human plasma after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY1–36 | 36 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 4.78 ± 1.07 | Human plasma protease | LC-MS/MS | Human plasma with 5 mg saxagliptin after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY3–36 | 34 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 26.9 ± 6.2 | Human plasma protease | LC-MS/MS | Human plasma after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY3–36 | 34 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 25.5 ± 6.2 | Human plasma protease | LC-MS/MS | Human plasma with 5 mg saxagliptin after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35174698 | 2022 | GFP-Ec | 250 | GFP | Ec (E.coli) SsrA tag sequences conjugation | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 6 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Mf | 266 | GFP | Mf (M.fluorum) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 56 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Ec | 250 | GFP | Ec (E.coli) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 14 | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35150805 | 2022 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 1200 nmol/kg | 0.137 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.42nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35113575 | 2022 | TT1-IP peptide | 27 | Free | Amidation | Cyclic (C-C Disulfide Bond) | L | Conjugation of TT1 and IP proteins which is linked by Ahx | TT1 and IP fusion protein | Antitumor (Effect on TPP-IPs on Cll xenograft models) | plasma collected at 10, 20, 30, 45, 60, 120 and 360 min | 5 mg/kg | 28 (Terminal Half Life) | BALB/c mice plasma protease | HPLC-MS | Balb/c mice plasma | In Vivo | None | None | The average survival for TT1-IP and LinTT1-IP treated groups was 19 days (the survival range for TT1-IP group was 17-23 days and for LinTT1-IP group was 13-25 days) and for the control group 16 days (range of 14-20 days) | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 1 mg | 0.25 ± 0.02 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 4 mg | 0.36 ± 0.04 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 10 mg | 0.45 ± 0.05 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 20 mg | 0.55 ± 0.07 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 30 mg | 0.70 ± 0.08 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 45 mg | 0.73 ± 0.05 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 60 mg | 0.78 ± 0.06 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34910492 | 2022 | 68Ga-DOTA-SETSKSF | 7 | 68Ga labelled | Free | Cyclic | L | None | Synthetic | Used For Positron Emission Tomography imaging of PD-L1 expression in tumors | N.A. | N.A. | 14.48 ± 3.26 | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 15 µg/kg | 24.4 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 30 µg/kg | 27 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at day 1 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 21 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at week 26 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 26.6 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at week 52, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 27.9 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34217775 | 2022 | FE 992326 | 30 | Free | Amidation | Linear | L | None | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min | 0.3 mg/kg | 6.5 ± 1.8 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992325 | 10 | D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Agp | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min | 0.3 mg/kg | 21 ± 2 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min | 0.2 mg/kg | 25 ± 8 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992326 | 30 | Free | Amidation | Linear | L | None | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min | 1 mg/kg | 11 ± 8.4 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992325 | 10 | D-val at position 1 | Amidation, 3-Pal modification at C terminal | Cyclic (C3-C10 disulfide bond) | Mix | Agp | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min | 1 mg/kg | 48 ± 11 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 50 ± 5, Human(%Plasma Protein Binding) = 46 ± 4 for FE 992325 | |||
| 34217775 | 2022 | FE 205030 | 10 | Oxazole-2-carbonyl, D-val at position 1 | Amidation | Cyclic (C3-C10 disulfide bond) | Mix | Phe linked with (2-Cbm),3Pal, Orn linked with iPr | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 40, 60, 90, 120, 180, 240, 300 min | 0.6 mg/kg | 23 ± 2 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 18.5 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 20 μg/kg | 7.87 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 100 μg/kg | 17.1 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected from rats in groups one to four at the corresponding time points before (0 h) and within 6 h after BPC157 administration. Blood samples were collected from rats in group five before the last three doses and within 6 h after the last dose | 500 μg/kg | 29.7 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 6 μg/kg | 5.27 ± 2.25 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 30 μg/kg | 19.6 ± 3.72 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 6 μg/kg | 20.0 ± 5.53 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 30 μg/kg | 25.5 ± 7.08 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| 36588717 | 2022 | BPC157 | 15 | Free | Free | Linear | L | None | Isolated from human gastric juice | Therapeutic Agent For Severe Trauma And Stress Damage And Can Promote The Healing Of Wounds, Ligament Injuries, Tendon Injuries, And Fractures | Blood samples were collected at the corresponding time points before (0 h) and within 6 h of a single administration. Blood samples were collected from dogs administered multiple doses at corresponding time points before the first dosing (0 h), within 6 h after dosing, before the last three doses, and at corresponding time points after the last dosing | 150 μg/kg | 29.3 ± 5.06 | Beagle dogs plasma protease | LC-MS/MS | Beagle dogs plasma | In Vivo | None | None | N.A. | |||
| N.A. | 2022 | 12kD-PEG-e9-XPLGLAG-r9-k(cy5) | 25 | 12 KDa PEG | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 6 nmol | 20 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Example 12 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modification, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 46 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13 | |||
| N.A. | 2022 | Example 4 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A14E, A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B27E, B28E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 24 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 28.6 | |||
| N.A. | 2022 | Example 10 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modification, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 28 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3 | |||
| N.A. | 2022 | Example 11 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E, B28E modificatino, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 28 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13.6 | |||
| N.A. | 2022 | Example 12 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 25 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13 | |||
| N.A. | 2022 | PA2 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG) modifications | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 24 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | PA3 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B28D modifications | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 26 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 33 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 58 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 85.1 | |||
| N.A. | 2022 | Example 41 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 57 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 42 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 41 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | PA1 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG) modification | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 41 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| 35177945 | 2022 | pE13F | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 7.2 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.56 ± 0.07 | |||
| 35177945 | 2022 | K17F | 17 | Free | Free | Linear | L | None | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 4.6 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.06 ± 0.01 | |||
| 35177945 | 2022 | P92 | 16 | Lys1 acetylation | Free | Linear | Mix | D-Arg = r, D-Gln = q, D-Leu = l, D-ala = a, Proline side chain linked with (4Br-Phe) at C terminus | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 24 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | Ki(nM) = 0.09 ± 0.02 | |||
| 35259149 | 2022 | TP5 | 5 | Free | Free | Linear | L | None | Synthetic | Treatment Of Patients With Immunodeficiency Diseases, Such As Rheumatoid Arthritis, Cancers, Hepatitis B Virus Infection, And Acquired Immunodeficiency Syndrome (Aids) | One hundred microliter plasma samples were collected at the following time intervals: 0.5, 5, 10, 20, 30, and 45 min and 1, 2, 3, 4, 6, 8,and 10 h after peptide administration. | 1 mg/kg | 0.022 ± 0.004 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | The cytotoxicity of TP5-MA was evaluated in mice spleen lymphocytes. Cytotoxicity was not detected after treatment with different concentrations of TP5-MA and TP5 | |||
| 35807558 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Treatment Of Type 2 Diabetes | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 46 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/, PDB id: 5VAI | None | N.A. | |||
| 35059568 | 2021 | JPE-1375 | 7 | Hoo = L-hydroorotic acid | Amidation | Linear | Mix | hle5 = D-homoleucine, Pff6 = Phe(4-F), Orn = Ornithine,Replaces the C-terminal Arg of PMX53 with a hydrophobic amino acid | Peptidomimetic C5a receptor antagonists | C5Ar1 Antagonists | Serial blood samples were collected at 10, 15, 30, 45, and 60 min, and at 2, 4, 6, and 24 h via a tail vein | 1 mg/kg | 0.13 (Elimination Half Life) | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | None | The inhibition of TNF levels also presented a similar median effective concentration (EC50) for PMX53 (5.9 μM) | |||
| 35056979 | 2021 | Al-ProD | 4 | Maleimide | DOX | Linear | L | None | Albumin-binding maleimide and cathepsin B-cleavable peptide conjugate | Antitumor | blood samples were collected from mice at pre-determined times (0, 3 h, 6 h, 9 h, 12 h, 24 h, 48 h, 72 h, 96 h, 120 h, and 144 h) | 3 mg/kg | 3.1 | BALB/C nude mice plasma protease | Fluorescence assay | BALB/c nude mice plasma | In Vivo | None | None | The IC50 value of HSA-bound Al-ProD in MDA-MB231 breast cancer cells is 7.33 µM, On day 20, the tumor volume in the Al-ProD-treated group was 347.42 ± 25.9 mm³, significantly smaller than the free DOX group (580.25 ± 139.92 mm³) and saline group (1810.98 ± 544.56 mm³) | |||
| 34707178 | 2021 | PYY3-36 analogues 44 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 0.5 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34661390 | 2021 | VVGS peptide | 15 | Free | Free | Linear | L | None | Synthetic | Targets tropoelastin | Aliquots (6 μL) taken after 0, 35, and 120 min | 0.6 mM which is diluted in water at a final concentration of 0.06 mM when aliquoting | 45 | Pooled serum protease from human male AB plasma | RP-HPLC | 50% pooled serum from human male AB plasma | In Vitro | None | None | KD (μM) = 41 ± 12 ( Interaction between Immobilized Human Recombinant Tropoelastin and Gd4TESMA) | |||
| 34630378 | 2021 | VP1 vaccine | 284 | Free | Free | Linear | L | None | Synthetic | Treatment of Coxsackievirus B3 (Cvb3)-Induced Viral Myocarditis | 1h at RT | 0.25 μg/μL | <15 | Murine serum protease | ELISA | Murine serum | In Vivo | None | None | ABD-VP1 increased the 28-day survival rate from about 40% (VP1) to 73% | |||
| 34575581 | 2021 | C5a receptor 1 antagonist (PMX205) | 5 | HC = Hydrocinnamate, O1: ornithine | Free | Cyclic | Mix | D-Cha3: cyclohexylalanine | Lipophilic analogue of PMX53 | Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury | Blood samples were collected at 0.04, 0.25, 0.5, 0.75, 1, 1.5, 1, 4, 6, and 24 h for both groups and then 48, 72, 96, and 120 h | 1 mg/kg | 0.84 (Terminal Elmination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | IC50 = 31 nM for PMX205 | |||
| 34575581 | 2021 | C5a receptor 1 antagonist (PMX205) | 5 | HC = Hydrocinnamate, O1: ornithine | Free | Cyclic | Mix | D-Cha3: cyclohexylalanine | Lipophilic analogue of PMX53 | Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury | Samples (n = 4) were quenched at regular intervals of 5 min, 10 min, 15 min, 30 min and 60 min | 1 µg/ml | 0.17 (Elimination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | IC50 = 31 nM for PMX205 | |||
| 34575581 | 2021 | C5a receptor 1 antagonist (PMX205) | 5 | HC = Hydrocinnamate, O1: ornithine | Free | Cyclic | Mix | D-Cha3: cyclohexylalanine | Lipophilic analogue of PMX53 | Treatment of Inflammatory Bowel Disease, Amyotrophic Lateral Sclerosis, Allergic Asthma, And Spinal Cord Injury | Blood sample was collected at 2.5, 5, 10, 15, 30, 45, 60, and 90 min | 1 μg/mL | 0.33 (Elimination Half Life) | Mice spinal cord homogenate protease | LC-MS/MS | Mice spinal cord homogenate | In Vivo | None | None | IC50 = 31 nM for PMX205 | |||
| 34455010 | 2021 | ELA-32 | 32 | pGlu = Pyroglutamate | Free | Cyclic (Cys-Cys Disulfide Bond) | L | None | Derived from Zebrafish | Anticancer, Treatment of Cardiovascular Disease | Blood sample were withdrawn at time points: 0, 2, 5, 10, 15, 30, 60, 120, 240 min | 5 μg/mL | 47.2 ± 5.7 | Human plasma protease | LC–MS/MS | Human plasma | In Vitro | None | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 0.89 | Human plasma protease | N.A. | Human pediatrics plasma (in Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1 | Human plasma protease | N.A. | Human pediatrics plasma (in non - Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34393794 | 2021 | LIT01-196 | 17 | Fluorocarbon chain (CF3(CF2)7(CH2)2C(O)) to the N-terminal part of K17F | Free | Linear | L | None | Apelin-17 Analog | Treatment of Hypertension | N.A. | 900 nmol/kg | 28 | Rats plasma protease | RIA | Rats plasma | In Vivo | Pubchem CID Apelin: 56841713 | None | IC50 = 0.56 ± 0.04 nmol/l for LIT01-196 | |||
| 34206631 | 2021 | Leu-ENK | 5 | Free | Free | Linear | L | None | Opioid peptide | Analgesic | Aliquot (95 µL) was taken at 0, 5, 15, 60, and 300 min | 315 µmol/L | 25 | Mice plasma protease | UPLC | Mice dipotassium ethylenediaminetetraacetic acid containing pooled plasma | In Vitro | None | None | N.A. | |||
| 34201398 | 2021 | optP7 | 9 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | For 0, 0.5, 1, 3, 6, and 24 h at 37 °C | 100 μM | 13 | Human serum protease | UPLC-MS | Human serum | In Vitro | None | None | MIC(µM) = 3 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 0.8 for E.coli in growth media MH,MIC(µM) = 1.5 for K. pneumoniae in growth media MH,MIC(µM) = 1.5 for A. baumannii in growth media MH,MIC(µM) = 0.8 for VRE in growth media MH,MIC(µM) = 6 for MRSA in growth media MH | |||
| 34201398 | 2021 | c-optP7 | 15 | Free | Free | Cyclic(Cys1-Cys15) | L | All Alanine replaced by β-alanine | Synthetic | Antimicrobial | For 0, 0.5, 1, 3, 6, and 24 h at 37 °C | 100 μM | 9 | Human serum protease | UPLC-MS | Human serum | In Vitro | None | None | MIC(µM) = 142 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 71 for E.coli in growth media MH,MIC(µM) > 142 for K. pneumoniae in growth media MH,MIC(µM) = ND for A. baumannii in growth media MH,MIC(µM) > 142 for VRE in growth media MH,MIC(µM) = 142 for MRSA in growth media MH | |||
| 34163352 | 2021 | OPT | 20 | Free | Free | Linear | L | None | Derived from the QKHPD-containing region of NCX1 | Binds To Pser68-Plm | Aliquots of 50 μl were collected at different time points (0–48 h) | 300 μM | 0.86 | Human serum protease | Mass spectrometry | Human serum | In Vitro | None | None | N.A. | |||
| 34122400 | 2021 | TP5 | 5 | Free | Free | Linear | L | None | derived from thymopoietin | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 3.2 ± 0.5 | Human serum protease | HPLC | Human serum | In Vitro | None | None | The cytotoxicity of CbTP was lower than that of parental peptide CATH2 | |||
| 36133017 | 2021 | CKP-NLP | 30 | Free | Free | Linear | L | AF488 labeled , Lys1 fatty acid conjugation (Palm) | Synthetic | Platform for potential delivery of peptide like drug candidates | 37 °C | N.A. | 1 | N.A. | SEC | N.A. | In Vitro | None | None | N.A. | |||
| 34048741 | 2021 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Salivary gland of the lizard Heloderma suspectum | Antidiabetes | Blood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h | 0.07 mg/kg | 0.32 ± 0.04 | Male SD rats plasma protease | ELISA | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 33940058 | 2021 | OPBP-1 | 12 | Free | Free | Linear | D | Substituition of A with Y at position 10 | Derived from H12 | Anticancer | Co-incubation of OPBP-1 with 10% human serum for 0 h, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, 32 h and 48 h. | 8 mg/kg | 0.33 ± 0.01 | Male SD rats plasma protease | RP-HPLC | Male SD rats plasma | In Vivo | None | None | After 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models. | |||
| 33825469 | 2021 | Native Ex4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 0.72 ± 0.07 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33813091 | 2021 | FITC-TPP1 | 21 | FITC labelled | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding | 4 mg/kg | <10 (Blood Clearance Half Life) | Mice blood plasma protease | Fluorescence spectrometry | Mice blood plasma | In Vivo | None | None | N.A. | |||
| 33791863 | 2021 | 125I-Ang1–7 | 7 | Free | Free | Linear | L | 125I labeled | Synthetic | Role in Renal and Cardiovascular Homeostasis | Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration | 4.5 mM | 0.6 | Rats plasma protease | Radioactivity assay | Rats plasma | In Vivo | None | None | Ang1–7 exhibited 4.2±0.1%, 3.7±0.6%, 4.4±0.2%, and 2.6±0.4% binding capacity in D.D. water, PBS 50 mM, PBS10mM, and acetate bufer, respectively | |||
| 33656323 | 2021 | IL-2 | 132 | Free | Free | Cyclic (C57-C104 Disulfide Bond) | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.041 ± 0.006 (T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.613 ± 0.063(T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 control | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.035 ± 0.014(T1/2a ) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | IL-2 | 132 | Free | Free | Cyclic (C57-C104 Disulfide Bond) | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 10 min and 2, 6, 12, 20, and 36 h for group I and 1, 4, 8, 16, 24, and 48 h for group II by retro-orbital bleeding, . Serum samples were collected at 0, 2, 5, 20, 30, and 45 min for group I and 10 min and 1, 2, 4, 6, and 8 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.273 ± 0.040(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33656323 | 2021 | B6 control | 146 | Free | Lys146 contains Fatty acid moiety which introduces 8-amino-3,6-dioxaoctanoic acid (AEEA) and glutamic acid | Cyclic (C57-C104 Disulfide Bond) In IL-2 | L | None | Synthetic | Anticancer, Autoimmune diseases treatment | Serum samples were collected at 0, 5, and 30 min and 2, 6, and 12 h for group I and 2, 10, and 60 min and 4, 8, and 24 h for group II by retro-orbital bleeding | 0.6 mg/kg | 0.196 ± 0.114(T1/2b) | Mouse plasma protease | Sandwich ELISA | Mouse plasma | In Vivo | pdb id: 5LQB and https://pubs.acs.org/doi/suppl/10.1021/acs.bioconjchem.1c00062/suppl_file/bc1c00062_si_001.pdf | None | KD (M) = (1.952 ± 0.130) × 10−8 for IL-2 | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 1 mg | 0.26 ± 0.02 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 4 mg | 0.36 ± 0.04 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 10 mg | 0.45 ± 0.05 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 20 mg | 0.55 ± 0.07 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 30 mg | 0.70 ± 0.08 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 45 mg | 0.73 ± 0.05 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 60 mg | 0.78 ± 0.06 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607165 | 2021 | JMV438 | 6 | Both Arg residues in positions 1 and 2 were replaced by two Lys | Free | Linear | L | None | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 1.57 ± 0.27 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 4.00 ± 0.35 for hNTS1 | |||
| 33607165 | 2021 | JMV449 | 6 | Free | Free | Linear | L | Arg8-Arg9 was replaced by a reduced amine bond (Ψ[CH2NH]) between Lys8-Lys9 | Derived from NT | Analgesic without hypothermia | Plasma collected at 0, 1, 2, 5, 10, 30 and 60 min | 0.156 mM | 8.37 ± 2.02 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | (Binding) Ki (nM) = 2.02 ± 0.80 for hNTS1 | |||
| 33387593 | 2021 | Wild-type (IFN) | 165 | Free | Free | Linear | L | None | Human derived | Antiviral, Antiproliferative | Blood samples were taken at different times post-injection | 100000 U | 0.9 ± 0.1 (T1/2 Elimination) | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | PDB id: 1ITF | None | Antiviral SBA (IU/ng) = 201 ± 9 in wild-type IFN, Antiproliferative SBA (IU/ng) = 240 ± 50 | |||
| 33245951 | 2021 | GIP(1–42) | 42 | Free | Free | Linear | L | None | Secreted by entero-endocrine K cells located in the proximal intestine | Insulinotrophic Effect | Blood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min and then co-incubation with Val-Pyr | 25 nmol/kg | 5 ± 0.6 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type= | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 4.01 ± 1.19 | Human male blood protease | Two site ELISA | Human male blood sample | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 3.94 ± 1.10 | Human female blood protease | Two site ELISA | Human female blood sample | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 3.96 ± 1.12 | Human blood protease (All) | Two site ELISA | Human blood sample (All) | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33129837 | 2021 | OM19r-8 | 19 | Free | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Blood samples were collected in 1.5 mL capacity disposable tubes at 0.125, 0.25, 0.5, 0.75, 1, 5, 10, 15, 30, 45, 60 and 75min | 1 mg/ml | 1.632 ± 0.34 (Elimination Half Life) | Wistar rats blood protease | N.A. | Wistar rats blood sample | In Vivo | None | None | MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin | |||
| 33129837 | 2021 | mPEG5- OM19r-8 | 19 | mPEG5 | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Blood samples were collected in 1.5 mL capacity disposable tubes at 0.125, 0.25, 0.5, 0.75, 1, 5, 10, 15, 30, 45, 60 and 75min | 1 mg/ml | 28.09 ± 2.81 (Elimination Half Life) | Wistar rats blood protease | N.A. | Wistar rats blood sample | In Vivo | None | None | MIC(μM) = 1 for OM19r -8 in E. coli ATCC25922, OM19r-8 and 250 mPEG5-OM19r-8 showed no cytotoxicity at the concentration up to 32 µM, hemolytic activity of OM19r-8 and mPEG5-OM19r-8 was < 10% at the determined concentration (1-128 μM), which was obviously superior to the control peptide melittin | |||
| 32078672 | 2020 | rFVIII | 654 | Free | Free | Linear | L | None | Synthetic | Role In Clotting | N.A. | 150 IU/kg | 0.23 | DKO mice plasma protease | chromogenic activity assays | DKO mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 33203916 | 2020 | Native TRAIL | 168 | Free | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h | 0.01 mg/mL | 3.4 ± 1.1 | BALB/c wild type mice plasma protease | Western blotting | BALB/c wild type mice plasma | In Vivo | PDB id: 1D0G | None | KD (M) = (6.02 ± 1.99) × 10–8 (Binding kinetics of TRAIL-ATNC and TRAIL against TRAIL receptor DR5.) | |||
| 33203916 | 2020 | TRAIL-ATNC | 168 | Free | TRAIL joined with ATNC using flexible linkers consisting of small amino acids (GSGGGSG) that could form a bridge between the C-terminal of TRAIL and the triple helix | Linear | L | None | Synthetic | Anticancer | Blood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h | 1 mg/mL | 56.1 ± 5.8 | BALB/c wild type mice plasma protease | Western blotting | BALB/c wild type mice plasma | In Vivo | PDB id: 1D0G | None | KD (M) = (2.56 ± 2.58) × 10–10 (Binding kinetics of TRAIL-ATNC and TRAIL against TRAIL receptor DR5.) | |||
| 33203916 | 2020 | TRAIL-ATNCIL4rP | 168 | Free | TRAIL joined with ATNC using flexible linkers consisting of small amino acids (GSGGGSG) that could form a bridge between the C-terminal of TRAIL and the triple helix followed by (MMP2) cleavage site (GPLGLAG) then IL4rP (CRKRLDRNC) | Linear | L | None | Synthetic | Anticancer | Blood samples (25–30 μL) were collected at 5, 15, 30, 60, 180, 360, 720 min, and 24 h | 1 mg/mL | 53.6 ± 5.8 | BALB/c wild type mice plasma protease | Western blotting | BALB/c wild type mice plasma | In Vivo | PDB id: 1D0G | None | IC50 value of 0.48 nM for TRAIL-ATNCIL4rP | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.3 | Simulated intestinal fluid protease | HPLC | Simulated intestinal fluid | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.6 | 50% W/V liver homogenate protease | HPLC | 50% w/v liver homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.95 | 50% W/V liver homogenate protease | HPLC | 50% w/v liver homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.15 | 50% V/V mouse plasma protease | HPLC | 50% v/v mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.11 | 50% V/V Mouse Plasma Protease | HPLC | 50% v/v Mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.87 | 50% V/V Mouse Plasma Protease | HPLC | 50% v/v Mouse plasma | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Lau-PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.36 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.2 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Human Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.16 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32888078 | 2020 | Mouse Myr-PTEN-PDZ | 8 | N-myristoyl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 0.25 | 50% W/V Brain Homogenate Protease | HPLC | 50% w/v Brain Homogenate | In Vitro | None | None | N.A. | |||
| 32858124 | 2020 | Cmpd# 3 | 16 | Acetylation | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.1 mg/kg | 0.362 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 1.95 ± 1.16 | |||
| 32812282 | 2020 | α-MSH | 14 | Free | Free | Linear | L | None | Deriving from the pro-opimelanocortin (POMC) | Stimulates The Production And Release Of Melanin By Melanocytes | 4 ◦C for 15 min | 40 μM | 7.4 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | N.A. | |||
| 32808659 | 2020 | ELA-21 | 21 | Free | Free | Linear | L | None | produced endogenously in the body | Anti-Heart Failure Activity | Blood was collected at time points of 0, 3, 10, 30 and 90 mins, and 4.5, 12 and 24 h | 100 mg/kg | ∼13 | Mice plasma protease | Western blotting | Mice plasma | In Vivo | https://sci-hub.se/10.1016/j.ijcard.2019.04.089 | None | EC50 = 0.6 nM (cAMP supression) | |||
| 32803073 | 2020 | WT-Rb | 168 | Free | Free | Linear | L | Biotinylation | Synthetic | Antitumor | Blood was collected in predetermined time points postinjection (n = 5; 0.05, 0.5, 1, 2, 4, 6, 12 and 24 h | 10 mg/kg | 20 (Initial Half-Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB ID: 4J4L | None | The tumor size remained around 200 mm3 until 27 days when Pal-Rb was administered (p < 0.01), whereas tumor continued to grow over 600 mm3 when WT-Rb and PBS were injected. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 68.5 ± 12.0 µg/kg | 16.8±5.66 (Terminal Half Life) | (IP) corn oil treated rats plasma protease | ELISA | Corn oil treated rat plasma | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 64.5 ± 13.2 µg/kg | 24.5±0.05 (Terminal Half Life) | Untreated rats plasma protease | ELISA | untreated rats plasma | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 68.5 ± 12.0 µg/kg | 47.9 ± 20.9 (Terminal Half Life) | (IP) corn oil treated rats CSF protease | ELISA | Corn oil treated rat CSF | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32736262 | 2020 | EX | 39 | Free | Amidation | Linear | L | None | Produced by the salivary glands of Gila monster | Antiobesity | Blood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio | 50 nmol/kg | 0.69 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 76 nmol/g | 46.2 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = Gemcitabine) | In Vivo | None | None | N.A. | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 76 nmol/g | 3.7 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = Prodrug) | In Vivo | None | None | N.A. | |||
| 32603666 | 2020 | V-Gem | 1 | Free | Gemicitabine | Linear | L | None | Derived from Gemcitabine | Anticancer | 2, 5, 15, 30, 45, 60, 90, 120, 180, 240, 300, and 360 min | 228 nmol/g | 39.1 | Mice blood plasma protease | LC-MS/MS | Mice blood plasma (analyte = Gemcitabine) | In Vivo | None | None | N.A. | |||
| 32582624 | 2020 | NT(8-13) | 6 | Free | Free | Linear | L | None | Derived from NT | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 1.0 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 1.5 ± 0.03 for hNTS1 | |||
| 32582624 | 2020 | Entry 1 | 6 | KK amino acid substiuitions | Free | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 1.6 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 4.0 ± 0.4 for hNTS1 | |||
| 32582624 | 2020 | Entry 2 | 6 | Kψ[CH2NH]K substiuition at position 1 | Free | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 8.4 ± 2.0 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 2.0 ± 0.8 for hNTS1 | |||
| 32582624 | 2020 | Entry 3 | 5 | KK amino acid substiuitions | TMSAla conjugation | Linear | L | None | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 1.6 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 0.018 ± 0.004 for hNTS1 | |||
| 32582624 | 2020 | Entry 5 | 6 | KK amino acid substiuitions | Free | Linear | L | Sip amino acid substiution | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 4.5 ± 0.8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 14 ± 11 for hNTS1 | |||
| 32582624 | 2020 | Entry 7 | 5 | Kψ[CH2NH]K substiuition | TMSAla conjugation | Linear | L | Sip amino acid substiution, TMSAla substuition | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 3.5 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 55 ± 5 for hNTS1 | |||
| 32582624 | 2020 | Entry 9 | 6 | KK amino acid substiuitions | Free | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 2.9 ± 0.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 7 600 ± 1 000 for hNTS1 | |||
| 32582624 | 2020 | Entry 11 | 5 | KK amino acid substiuitions | TMSAla-OH conjugation | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 2.8 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 710 ± 100 for hNTS1 | |||
| 32582624 | 2020 | Entry 13 | 5 | KK amino acid substiuitions | TMSAla-OH conjugation | Linear | Mix | Substiution of Y amino acid with d-W | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 10 ± 2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 3 600 ± 600 for hNTS1 | |||
| 32582624 | 2020 | Entry 15 | 6 | KK amino acid substiuitions | Free | Linear | L | Substiution of Y, I amino acid with Dmt, Tle | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 4.6 ± 0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 57 ± 6 for hNTS1 | |||
| 32512181 | 2020 | [3H]-THF | 8 | Free | Free | Linear | L | 3H labeling at proline5 residue | Isolated from calf thymus | Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment) | Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min | 93 nmol/mL | 3.7 ± 0.2 | Rats blood protease | N.A. | Rats blood sample | In Vitro | None | None | N.A. | |||
| 32512181 | 2020 | [3H]-THF | 8 | Free | Free | Linear | L | 3H labeling at proline5 residue | Isolated from calf thymus | Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment) | Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min | 93 nmol/mL | 5.6 ± 0.2 | Mouse blood protease | N.A. | Mouse blood sample | In Vitro | None | None | N.A. | |||
| 32512181 | 2020 | [3H]-THF | 8 | Free | Free | Linear | L | 3H labeling at proline5 residue | Isolated from calf thymus | Antiviral, Anticancer (As an adjunct to chemotherapy in cancer treatment) | Samples were taken for analysis after 0, 1, 2, 5, 10, 15, 20, 30, 45 and 60 min | 93 nmol/mL | 5.2 ± 0.4 | Human blood protease | N.A. | Human blood sample | In Vitro | None | None | N.A. | |||
| 32506501 | 2020 | des-Ac-a-MSH | 14 | Free | Amidation | Linear | L | None | Derived from POMC | Antiinflammatory, Antipyretic | 37 °C | 2 µM | 0.21 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 1.667E-09 for MC1R-des-Ac-a-MSH | |||
| 32506501 | 2020 | gamma2-MSH | 12 | Free | Amidation | Linear | L | None | Derived from POMC | Antiobesity | 37 °C | 2 µM | 0.028 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 7.749E-10 for MC1R-g2-MSH | |||
| 32404523 | 2020 | C34 | 34 | Free | Free | Linear | L | None | Derived from the gp41 CHR | Therapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys | Blood samples (300 μl) were collected from the tail vein before administration and at different intervals after injection (3, 6, 9, 20, 23, 29, 48, 72, and 96 h) | 1.7 μmol/kg | 0.6 | Rats plasma protease | HIV inhibition assay | Rats plasma | In Vivo | None | None | [EC50] = 18.51 nM for PEG40-NC (antiviral activity) | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(23,30) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifications include (S-octenyl alanine) and (Bis-pentenyl glycine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 30 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | GLP-1 | 30 | Free | Free | Linear | L | None | Unstapled GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | <10 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | GLP-1 | 30 | Free | Free | Linear | L | None | Unstapled GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 14 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32332143 | 2020 | 68Ga‐NeoBOMB1 | 7 | 68Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1 | NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminal | Linear | L | None | Synthetic | DOTA‐coupled GRPR‐antagonist | 2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i | 50 µg | 27.3 | Human plasma protease | RP-HPLC | Human plasma | In Vivo | None | None | N.A. | |||
| 32332143 | 2020 | 68Ga‐NeoBOMB1 | 7 | 68Ga-DOTA-(p-aminomethylaniline)-(diglycolic acid), D-Phe at position 1 | NH-CH[CH2-CH(CH3)2]2 chemical group attached at C terminal | Linear | L | None | Synthetic | DOTA‐coupled GRPR‐antagonist | 2, 5, 10, 30 and 45 min and at 1, 2 and 3 h p.i | 50 µg | 35 | Human blood protease | RP-HPLC | Human blood sample | In Vivo | None | None | N.A. | |||
| 32243137 | 2020 | OXM-1 | 37 | Free | Free | Linear | Mix | Incorporation of D-ser in place of L-ser at 2nd position | Derived from proglucagon | Antiobesity, Antisteatotic | N.A. | 40 μg/kg | 6 (Terminal Half Life) | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 10 for OXM-1 (in Vitro Potency of Stapled Peptides in Human GLP-1R- and GCGR-Mediated CRE-Luc Reporter Assays) | |||
| 32133341 | 2020 | R3 B1-27 | 27 | Free | Free | Linear | L | None | Native relaxin-3 | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 3.1 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 5.91 ± 0.21 | |||
| 32133341 | 2020 | R3 B1-22R | 23 | Free | Amidation | Linear | L | None | Synthetic | Relaxin-3 antagonist | N.A. | 0.05 μg/μl | 4 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.76 ± 0.03 | |||
| 32075870 | 2020 | hGLP-2 | 33 | Free | Free | Linear | L | None | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 1 mg/kg | 6.4 ± 0.2 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.07 for hGLP-2 receptor | |||
| 32075870 | 2020 | Glepaglutide | 39 | Free | KKKKKK amino acids substiuitions at C terminal | Linear | L | G,E,T,S,L,A,A,A,A amino acid substuitions at positions 2,3,5,8,10,11,16,24,28 respectively | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 19 ± 1.9 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.03 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 16 ± 0.8 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 43 ± 4 (Elimination Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 1 mg/kg | 0.5 ± 0.1 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 5 mg/kg | 0.5 ± 0.0 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.25 mg/kg | 0.9 ± 0.1 (Terminal Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 31926774 | 2020 | Leuprolide | 10 | Free | NHEt (Ethylamine) | Linear | L | None | Synthetic | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.43 ± 0.025 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The administration of same dose of PEGylated leuprolides also results in an initial testosterone surge. In addition, the extent of the testosterone surge is almost the same for all three peptides, either PEGylated or not | |||
| 31926774 | 2020 | Leuprolide | 10 | Free | NHEt (Ethylamine) | Linear | L | None | (GnRH) agonist | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.43 ± 0.06 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The administration of same dose of PEGylated leuprolides also results in an initial testosterone surge. In addition, the extent of the testosterone surge is almost the same for all three peptides, either PEGylated or not | |||
| 31926774 | 2020 | PEG2K-LEU | 10 | Free | Free | Linear | L | PEGylation at His2 | Derived from leuprolide | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.53 ± 0.032 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group | |||
| 31926774 | 2020 | PEG2K-LEU | 10 | Free | Free | Linear | L | PEGylation at His2 | Derived from leuprolide | Anticancer (Treatment of Advanced Prostate Cancer) | Blood samples were collected from rats orbit at predetermined time interval | 1.0 mg/kg | 0.59 ± 0.023 | SD rats serum protease | UPLC–MS/MS | SD rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC6017563/ | None | The weight of testis of the rats received unmodified leuprolide, PEG2K-LEU and PEG5K-LEU decreases to be ~57%, ~58%, and ~52% of the untreated group | |||
| 31866565 | 2020 | YSNSG peptide | 5 | Free | Free | Cyclic | L | None | Synthetic | Antitumor | Blood samples from blood vessel in the tail were taken at the following time intervals: 15, 30, 60, 90 and 120 min | 20 mg/kg | 25.8 ± 8.2 | B16F1 melanoma mice plasma protease | UPLC-MS/MS | B16F1 melanoma mice plasma | In Vivo | None | None | The relative recoveries of the microdialysis probes of YSNSG peptide in mice using the reverse dialysis method were 79.3 ± 6.6% in the region 1 of the tumor and 79.1 ± 7.4% in the region 2 of the tumor | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | N.A. | N.A. | 13.9 ± 3.6 | Human blood plasma protease | 2-site immunoassay | Human blood plasma | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | N.A. | N.A. | 17.0 ± 6.8 | Human blood plasma protease | 2-site immunoassay | Human blood plasma after Sitagliptin | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | GH levels were obtained every 10 minutes from 8 PM until 8 AM | N.A. | 13.9 | Human blood plasma protease | 2-site immunoassay | Human blood plasma | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31529097 | 2020 | GH | 191 | Free | Free | Linear | L | None | Produced by the somatotroph cells in the anterior pituitary gland | Involved in the regulation of growth and metabolism | GH levels were obtained every 10 minutes from 8 PM until 8 AM | N.A. | 14.5 | Human blood plasma protease | 2-site immunoassay | Human blood plasma after 1month of Sitagliptin | In Vivo | pdb id: 1HWG | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 43 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 9.9 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 52 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 12 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 32 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 8.3 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 38 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 13 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 | 12 | Acetylation | Free | Linear | L | Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 0.9 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 13.8 | |||
| 31774631 | 2019 | BAY55-9837 | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 0.31 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31632382 | 2019 | Api137 | 18 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O: L-ornithine at position 2 | Apidaecin analog | Antimicrobial | N.A. | 20 mg/kg | < 30 | Mice plasma protease | RP-HPLC | Mice plasma | In Vivo | None | None | N.A. | |||
| 31443263 | 2019 | TP5 | 5 | Free | Free | Linear | L | None | Arg32–Tyr36 fragment derived from thymopoietin | Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions) | 37 °C | N.A. | 1.32 ± 0.24 | Rats plasma proteaes | HPLC | 10 μg/mL rats plasma | In Vitro | None | None | Among the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL | |||
| 31277465 | 2019 | Dox-peptide conjugate 13 | 14 | DOX | Free | Cyclic (Lys6-Glu14 bond) | L | C6 fatty acid linked between | Synthetic | Anticancer | Several aliquots (55 µL) were removed at 2, 5, 10, 15, 30, 60, 90, and 120 min | 125 µM | 11.8 | Human serum protease | HPLC | 25% human serum | In Vitro | None | None | Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25–35% as compared to Dox which reduced cell proliferation in the range of 20–34% for all selected four cell lines | |||
| 31276085 | 2019 | S-RWRWR peptide | 12 | Acetylation | Amidation | Linear | Mix | R amino acid substituition at 1,4, 11, FAM denotes 5,6-carboxyfluorescein conjugated with Orn,p=D-Proline11,O=Ornithine7 | scrambled version of the RWRWR peptide | Cell penetrating peptide | 37°C | 2 mg/ml | 30 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 31276085 | 2019 | III-67B | 12 | FAM denotes 5,6-carboxyfluorescein | Amidation | Linear | L | None | Synthetic | Cell penetrating peptide | 37°C | 2 mg/ml | 9.5 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 31235532 | 2019 | CNP-39 | 39 | Proline substituition (amino acid 1) | Free | Cyclic (1 Disulfide Bond) | L | Glycine (amino acid 2) modifcation | CNP derivative | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Samples from animals treated with the daily CNP-39 molecule were also obtained after the 1st and the 26th dose: at pre-dose, 0.08, 0.25, 0.5, 1, 2, and 4 hours postdose | 20 μg/kg per day for 26 weeks | 0.35 | Cynomolgus monkeys plasma protease | competitive radioimmunoassay | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31194563 | 2019 | Fasudil in CAR-liposome | 9 | Conjugation of amino groups of the lipids of liposomes with CAR peptide at N terminal Cys | Amidation | Linear | L | None | Synthetic | Treatment of Pulmonary Arterial Hypertension | N.A. | 3 mg/kg | 0.7 ± 0.3 | Sham rats plasma protease | LC–MS/MS | Sham rats plasma | In Vivo | None | None | N.A. | |||
| 31156041 | 2019 | AD-114-Im7-FH | 118 | Free | lm7-FH fusion | Linear | L | None | Fusion protein of AD-114 with lm7 and FH | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 3 mg/kg | 0.18 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 9.1 (Human CXCR4 affinity) | |||
| 31156041 | 2019 | AD-114-Im7-FH-SA21 | 118 | Free | lm7-FH-SA21 | Linear | L | None | Fusion protein of AD-114 with lm7 and FH, SA21 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 2 mg/kg | 0.95 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 9.2 (Human CXCR4 affinity) | |||
| 31100806 | 2019 | lysostaphin | 255 | Free | Free | Linear | L | None | Produced by Staphylococcus simulans | Anti-Staphylococcal lysin | Blood was collected by orbital bleeding at 1, 4, 7, and 24 h postadministration | 40 mg/kg | <1 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | Unconjugated lysostaphin shows a standard antibody binding response from 0.3 to 20 ng/ml. | |||
| 31100806 | 2019 | Cpl-1 | 568 | Free | Free | Linear | L | None | Lytic enzyme of a pneumococcal bacteriophage | Antimicrobial for Pneumococcal Bacteremia | Blood was collected after 5, 10, and15 min from three animals and after 30, 60, and 120 min from the other three animals | 1.6 mg | 20.5 | Mice plasma protease | Western blotting and spot densitometry | Mice serum | In Vivo | None | None | MICs of Cpl-1 = 32 μg/ml | |||
| 31100806 | 2019 | LytA | 318 | Free | Free | Linear | L | None | Derived from Streptococcus pneumoniae | Therapeutic agent in experimental peritonitis sepsis caused by highly Β-lactam resistant Streptococcus Pneumoniae | Blood samples were obtained from three animals per group, which were killed at 5, 15, 60, and 120 min | 3.1 mg/ml | 22.5 | Adult swiss mice plasma protease | N.A. | Adult swiss mice plasma | In Vivo | None | None | MICs of LytA = 16 μg/ml | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 3 mg | 0.242 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 9 mg | 0.326 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 18 mg | 0.392 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 24 mg | 0.521 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 30 mg | 0.485 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31064153 | 2019 | Lys(Har)-PA | 3 | Side chain of the Lys residue in the first position was extended by attaching additional homoarginine (Har) | Free | Linear | L | None | KPPR analogs | Peptidic inhibitor of the VEGF165/NRP-1 interaction | 100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h) | 1.1 µmol/mL | 39 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 0.2μM | |||
| 31064153 | 2019 | Dab-R | 2 | Dab (2,4-diaminobutyric acid) substiuition at 1st position | Free | Linear | L | None | KPPR analogs | Peptidic inhibitor of the VEGF165/NRP-1 interaction | 100 µL of aliquots were withdrawn at different time intervals (for 8 and 10: 0 min, 2h, 4h, 6h, 10h, 12h, 24h, 48h, 72h, 96h) | 1.1 µmol/mL | 44 | Human plasma protease | HPLC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 0.3 μM | |||
| 31038930 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration | 25 nmol/kg | 0.9 | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 7MLL | None | Exenatide presented similar GLP-1 activities with EC50 values of 1.1 | |||
| 30986342 | 2019 | T4-Cy5.5 | 7 | Free | Conjugated with Cy5.5 | Linear | L | None | Synthetic | Antitumor | N.A. | N.A. | 1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Free T4 or P-T4 slowed tumor regrowth after chemotherapy, whereas the P-T4 treatment group exhibited a better suppressive effect | |||
| 30973007 | 2019 | GBAP | 11 | Free | Free | Cyclic (Ser3-Met11 bond) | L | None | Produced by Enterococcus faecalis | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8hr, and 24 hr | 0.28 mM | <30 | Human plasma protease | HPLC | Human plasma | In Vitro | None | None | EC50 (nM) = 1.15 for GBAP | |||
| 30973007 | 2019 | GBAP 11 | 14 | Free | Free | Cyclic (Ser3-Met11 bond) | L | N-methylation at Phe7 | GBAP analogs | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8hr, and 24 hr | 0.28 mM | <30 | Human plasma protease | HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 6.3 for GBAP-[N-MeF7] | |||
| 30901967 | 2019 | HP23-E6-IDL | 32 | Free | Free | Linear | L | None | Synthetic | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides HP23-E6-IDL | 5 mg/kg | 1 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 912 ± 29 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of HP23-E6-IDL against infection by HIV-1 mutants resistant to T20) | |||
| 30900390 | 2019 | Ac-SDKP | 4 | Acetylation | Free | Linear | L | None | Synthetic | Antifibrotic effects on Hepatic Fibrosis | At 2, 4, 6, 8, 10, 18, 30, 120, 360, 480, and 540 min after the injection, 50 μL of blood was sampled from each animal through the caudal vein | 1 mg/kg | 9.65 ± 1.78 | Rats serum protease | RP-HPLC | Rats serum | In Vivo | None | None | Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro | |||
| 30900390 | 2019 | Ac-SDKP | 4 | Acetylation | Free | Linear | L | None | synthetic | Antifibrotic Effects On Hepatic Fibrosis | 9 h at 37 C | 100 μM | 6.47 ± 1.53 | Human Serum Protease | HPLC | human serum | In Vitro | None | None | Ac-SD(d)K(d)P and Ac-SDKP exhibited similar antifibrotic effects in vitro | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes | 200 pmol/kg | 4.3 ± 1.2 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes | 2000 pmol/kg | 6.9 ± 2.5 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection | 2000 pmol/kg | 53 ± 14 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30814652 | 2019 | Adnectin C | 20 | Free | Free | Linear | L | None | Derived from the tenth domain of fibronectin type III (10thFn3) | Anticancer | Blood samples were taken after 5 min, 15 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h, 12 h, 24 h, 36 h, 48 h, 72 h, and 96 h | 5 mg/kg | 49.41 | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | Kd(1/s) = 5.643E − 5 | |||
| 30794654 | 2019 | CNP(1–22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | CNP C terminal cleavage | Improved endochondral ossification and accelerated bone growth in mice | N.A. | 20 nmol/kg | 1.42 ± 0.45 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | ASB20123 | 39 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | C-type natriuretic peptide derivative | Treatment of Growth failure and Dwarfism | N.A. | 20 nmol/kg | 31.3 ± 4.8 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | CNP(1–22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | CNP C terminal cleavage | Improved Endochondral Ossification And Accelerated Bone Growth In Mice | N.A. | 50 nmol/kg | 10.0 ± 5.0 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | ASB20123 | 39 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | C-type natriuretic peptide derivative | Treatment Of Growth Failure And Dwarfism | N.A. | 50 nmol/kg | 32.1 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30756483 | 2019 | ABD–Dox | 47 | Free | Dox conjugation | Linear | L | None | Derived from streptococcal protein G | Anticancer | Blood samples were collected at 40 s, 15 and 30 min, and 2, 4, 8, 24, 48, 72, and 96 h post injection | 5 mg/kg | 29.4 ± 0.8 (Elimination Half Life) | Mice plasma protease | Flurorescence assay | Mice plasma | In Vivo | None | None | (IC50) of ABD–Dox was 6.4 × 10−6 for C26 cell | |||
| 30742145 | 2019 | Native BMP-2 | 116 | Free | Free | Linear | L | None | Synthetic | Promotes Bone repair | N.A. | 0.5 mg/kg | <30 | N.A. | Fluorescence spectrometry | Rats | In Vivo | PDB id: 1ES7 | None | n(BMP-2) did not enhance ALP expression in MSCs compared with native BMP-2 unless pretreated with IV collagenase, which significantly enhanced ALP expression and calcium deposition | |||
| 30709867 | 2019 | PNA5 | 7 | Free | Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus | Linear | L | None | Ang-(1-7) analogs | Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction | N.A. | 100 µM | 1.0 ± 0.2 | Rats serum protease | Tandem mass spectrometry (MS) | Rats serum | In Vitro | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease Brain ROS production and Inflammation in Preclinical models of HF | N.A. | 100 µM | 0.25 ± 0.05 | Rats serum protease | Tandem mass spectrometry (MS) | Rats serum | In Vitro | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | PNA5 | 7 | Free | Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus | Linear | L | None | Ang-(1-7) analogs | Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction | N.A. | 10 mg/kg | 18.2 ± 3 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease Brain ROS production and Inflammation in Preclinical models of HF | N.A. | 10 mg/kg | 20.9 ± 0.7 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | PNA5 | 7 | Free | Replaces the seventh residue (proline) with a serine, and has a glucose sugar moiety attached to the serine and is amidated on the C terminus | Linear | L | None | Ang-(1-7) analogs | Treating Vascular Cognitive Impairment and Inflammation related Memory Dysfunction | N.A. | 10 mg/kg | 26.6 ± 3.6 | CSF protease | LC-MS | CSF | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30709867 | 2019 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease Brain ROS production and Inflammation in Preclinical models of HF | N.A. | 10 mg/kg | 24.7 ± 5 | CSF protease | LC-MS | CSF | In Vivo | None | None | Potency IC50 = 0.1 μM for PNA5 (In vitro bioactivity ROS inhibition) | |||
| 30690406 | 2019 | Apelin1 | 17 | Free | Free | Linear | L | None | Native apelin 17 | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.4 | RHNEP | LC-MS | Apelin1 | In Vitro | None | None | EC50(nM) = 1.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin2 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=H | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1 | RHNEP | LC-MS | Apelin2 | In Vitro | None | None | EC50(nM) = 4.1 ± 1.0 | |||
| 30690406 | 2019 | Apelin1 | 17 | Free | Free | Linear | L | None | Native apelin 17 | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.4 | RhKLKB1 | LC-MS | Apelin1 | In Vitro | None | None | EC50(nM) = 1.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin2 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=H | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.7 | RhKLKB1 | LC-MS | Apelin2 | In Vitro | None | None | EC50(nM) = 4.1 ± 1.0 | |||
| 30690406 | 2019 | Apelin3 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=Me, Methylation at Glu8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.9 | RhKLKB1 | LC-MS | Apelin3 | In Vitro | None | None | EC50(nM) = 4.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin6 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1 | RhKLKB1 | LC-MS | Apelin6 | In Vitro | None | None | EC50(nM) = 2.6 ± 0.8 | |||
| 30690406 | 2019 | Apelin1 | 17 | Free | Free | Linear | L | None | Native apelin 17 | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.02 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 1.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin2 | 20 | R1 = NH2-Lys-Phe-Arg | Free | Linear | L | R2=H | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 0.3 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 4.1 ± 1.0 | |||
| 30606721 | 2019 | BCY-B2 | 14 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C1, C7, C14) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | Blood samples were taken from two animals per time-point, at 0.08, 0.5, 1, 2, and 4 hours post injection (p.i.), | 5.925 mg/kg | 14 (Elimination Half Life) | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vivo | None | None | KD(nM) = 25 ± 0.3 | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 13 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 16 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30543420 | 2019 | R2 | 53 | Free | Free | Linear | L | B-D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 0.3 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.025 ± 0.004 | |||
| 30543420 | 2019 | R3-02 | 53 | Free | FA-02 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 1 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.18 | |||
| 30543420 | 2019 | R3-02 | 53 | Free | FA-02 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | 1 | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.10 | |||
| 30334171 | 2019 | rhIFN-α2b | 165 | Free | Free | Linear | L | None | Synthetic | Antiviral, Antitumor, And Immunomodulatory Effects | N.A. | 500 μg/kg | 0.54 (Elimination Half Life) | Rats plasma protease | sandwich ELISA | Rats plasma | In Vivo | PDB id: 1RH2 | None | rhIFN-α2b had a high specific antiviral activity (2.5 × 108 ± 1.1 × 108IU/mg protein) | |||
| 30175919 | 2018 | Myristoylated peptide | 14 | 6FAM labelled | Additional C terminal cysteine linked to peptide using dislufide bond | Linear | L | MeAla, MeArg,Lys1 modified with Myr | Synthetic | Substrate reporter for PKB | RT | 1 µM | 12 ± 1 | N.A. | N.A. | Axenic D. discoideum K-AX3 DB or SorCM after myristoylated peptide loading | In Vitro | None | None | N.A. | |||
| 30175919 | 2018 | Electroporation peptide | 9 | 6FAM labelled | Free | Linear | L | MeAla, MeArg | Synthetic | Substrate reporter for PKB | RT | 35 µM | 53 ± 15 | N.A. | N.A. | Axenic D. discoideum K-AX3 SorCM buffer after electroporation | In Vitro | None | None | N.A. | |||
| 30175919 | 2018 | Pinocystosis peptide | 9 | 6FAM labelled | Free | Linear | L | MeAla, MeArg | Synthetic | Substrate reporter for PKB | RT | 150 µM | 19 ± 2 | N.A. | N.A. | Axenic D. discoideum K-AX3 DB after pinocytosis | In Vitro | None | None | N.A. | |||
| 30161002 | 2018 | P16 | 21 | Free | Free | Linear | L | None | TNF-a cleaved fragment | Antitumor | Orbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h) | 5 mg/kg | 0.07 | BALB/c mice plasma protease | LC-MS | BALB/c mice plasma | In Vivo | None | None | N.A. | |||
| 30161002 | 2018 | TNF-a | 158 | Free | Free | Linear | L | None | TNF-a | Antitumor | Orbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h) | 5 mg/kg | 0.43 | BALB/c mice plasma protease | LC-MS | BALB/c mice plasma | In Vivo | PDB id: 6OP0 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 0.56 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 0.9 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 1.7 (T1/2 Initial Phase) | Rats plasma protease | LC-MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 27 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris–HCl buffer (50 mM, pH 7.4) | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 47 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ala1]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 42 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM[Ala4]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 52 ± 2 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ala5]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29752565 | 2018 | Met-enkephalin | 5 | Free | Met substituition at C terminal | Linear | L | None | Synthetic | Involved in the pain modulating mechanism in the spinal cord | Incubated over 0, 30, 60, 90, 120 min at 37 °C | 0.0413 mM | 53 ± 1 | NEP (5.687 Nm) | RP-HPLC | Tris HCl buffer with 0.156 mM [Ser4]sialorphin inhibitor | In Vitro | None | None | N.A. | |||
| 29721065 | 2018 | 64Cu-DOTA-F56 | 12 | 64Cu-DOTA | Free | Linear | L | None | Synthetic | Antiangiogenic | At 10, 30, 60, and 120 min | 7.4 mBq | 0.4249 | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | F56 and F56-CM reduced the angiogenesis of zebrafish embryos in a dose-dependent way | |||
| 29685037 | 2018 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease brain ROS production and inflammation in preclinical models of HF | 15 h at 37°C | 100 µM | 13.8 ± 5.7 | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29685037 | 2018 | Ang-(1-7) | 7 | Free | Free | Linear | L | None | Ang-(1-7) | Decrease brain ROS production and inflammation in preclinical models of HF | After a 30 min incubation at 37°C | 0.1 mM | 9.2 ± 0.5 | ACE, LAP and NEP | HPLC | PBS solution containing all three hydrolytic enzymes (0.5 IU/mL), ACE, LAP and NEP | In Vitro | None | None | Ang-AA in combination with paclitaxel exerted stronger anti-tumor effects than Ang-(1-7), as indicated by reduced tumor growth, tumor weight, COX2 expression, and increased survival of the mice | |||
| 29669811 | 2018 | 125I-3E8.G4S | 278 | 125I labelled | Free | Linear | L | 125I-labeled, VH and VL joined by G4S linker | Derived from the 3E8 antibody | Optimizes biophysical properties, serum half-life and high-specificity tumor imaging | Blood samples (5 μl) were drawn from the saphenous vein by puncture, using a 30-gauge syringe needle, at 0.5, 1, 5, 24, 48, and 72 h postinjection for 3E8.G4S | 5 μCi | 0.67 | Mice blood protease | Radioiodination assay | Mice blood sample | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/instance/5995523/bin/supp_RA118.002538_136163_1_supp_109995_p6kvvq.pdf | None | KD of 3.6 nM for 3E8.G4S | |||
| 29656472 | 2018 | [K6T]P8 peptide | 10 | Free | Amidation | Linear | L | K6T modification | Synthetic | IL‐15 antagonist peptide | At t = 0, 5, 8, 10, 20,30, 45, 60, 90, and 120 minutes | 100 μM. | 5.88 ± 1.73 | Human synovial fluids protease | RP-HPLC | Human synovial fluids | In Vitro | None | None | IC50 values of 27.7 μM | |||
| 29602308 | 2018 | P4-Chlorambucil | 7 | Free | Chlorambucil | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 21.5 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Chlorambucil | 7 | Free | Chlorambucil | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 12.4 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Melphalan | 7 | Free | Melphalan | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 24.6 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Melphalan | 7 | Free | Melphalan | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 10.6 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Bendamustine | 7 | Free | Bendamustine | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 19.3 | N.A. | LC–MS/MS | Buffer pH 7.4 | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29602308 | 2018 | P4-Bendamustine | 7 | Free | Bendamustine | Linear | L | None | Protein drug conjugate | Anticancer | 37 °C | 100 μl/ ml | 15.4 | Mouse liver homogenate protease | BCA protein assay | Mouse liver homogenate | In Vitro | None | None | The efficacies of all P6-conjugates were significantly lower than those of P4–conjugates at concentrations above 10 µM | |||
| 29550018 | 2018 | DTβ4 | 88 | Free | Free | Linear | L | Dimerization using GS linker | Dimeric Tβ4 | Protects post-ischemic cardiac function | N.A. | 50 μg | 59.1 | Mouse serum protease | HPLC | Mouse serum | In Vivo | Uniprot id: P62328 | None | In scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration | |||
| 29550018 | 2018 | Tβ4 | 43 | Free | Free | Linear | L | None | Synthetic | Protects post-ischemic cardiac function | N.A. | 50 μg | 53.3 | Mouse serum protease | HPLC | Mouse serum | In Vivo | Uniprot id: P62328 | None | In scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration | |||
| 29540315 | 2018 | GUB09-123 | 33 | Free | Amidation | Linear | L | None | Synthetic | GLP-1/GLP-2 co-agonist | Blood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point) | 800nmol/kg | 0.9 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | GLP-1R, EC50 (nM) = 0.07 | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | N.A. | 24.6 (Slow Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma without NC-100717 | N.A. | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | N.A. | 1.1 (Fast Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma without NC-100717 | N.A. | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | 1 mg/kg | 26.4 (Slow Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma after administration of NC-100717 (1 mg/kg) | In Vivo | None | None | N.A. | |||
| 29531858 | 2018 | [68Ga]Ga-DOTA-RGD | 8 | CH2CO chemical group attached, DOTA conjugated with Lys1 | CCPEG | Cyclic (C2-C6 Disulfide Bond) | L | 68Ga labelling | Synthetic | PET imaging agent to visualize and quantify angiogenesis | Blood samples (0.5 ml) for radioactivity measurements (0.5 ml) were taken at 1, 3, 6, 9, 12, 15, 30, 60, 90 minutes after RGD injection | 1 mg/kg | 1.9 (Fast Phase) | NHP plasma protease | UV-HPLC and LC-ESI-MS | NHP uterus plasma after administration of NC-100717 (1 mg/kg) | In Vivo | None | None | N.A. | |||
| 29528634 | 2018 | GLP2-2G | 33 | Free | Free | Linear | L | Ala2 was substituted with Gly | GLP-2 analogue | Treatment of Short Bowel Syndrome | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 25 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.035 ± 0.003 | |||
| 29517911 | 2018 | 2d | 13 | Acetylation | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | Trp3 → Phe3, Pro4 → Aze4, Ala5 → Tyr5, Arg6 → HArg6, Leu8 → Ala(ψCH2NH)6 substituitions | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | Serial blood samples were taken from each animal via temporary indwelling tail vein cannulae at 5, 10, 20, 30, 60, 120, 180, and 240 min postdose, | 5 mg/kg | 48 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29461833 | 2018 | Pyr analogue 2 | 13 | Free | Free | Cyclic (X1-X5 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 0.8 ± 0.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 5.7 ±3.5 for 2 | |||
| 29461833 | 2018 | Pyr analogue 4 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X1-X6 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 0.7 ± 0.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 523 ±165 for 4L | |||
| 29436835 | 2018 | PIE 12-trimer | 48 | Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 0.6 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 2.1 ± 0.28 (antiviral potency) | |||
| 29436835 | 2018 | PIE 12-trimer | 48 | Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 0.8 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 2.1 ± 0.28 (antiviral potency) | |||
| 29436835 | 2018 | C16-PIE12-trimer | 48 | C16-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 0.9 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.11 ± 0.012 (antiviral potency) | |||
| 29421564 | 2018 | SP | 11 | Free | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 2 | Human serum protease | ELISA | Human serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | SP | 11 | Free | Free | Linear | L | None | Synthetic | Therapeutic Regeneration By Facilitating Mobilization Of Endogenous Stem Cells From Bone Marrow To The Injured Sites | 0 to 72 h at 37°C | 5 nmol | 1.7 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29329072 | 2018 | Compound 1 | 8 | Free | Amidation | Linear | L | None | NMU-analogs | Regulation of Feeding Behavior, the stress response and nociception | 37 °C | 112 µM | 4.3 ± 0.2 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | EC50(nM) = 38.9, IC50(nM) = 0.78 for hNMUR1 and EC50(nM) = 30.8, IC50(nM) = 1.7 for hNMUR2 | |||
| 29282303 | 2018 | SCRAP-mCherry | N.A. | DD | mCherry | N.A. | L | None | Synthetic | Affects Antigen Presentation | N.A. | N.A. | 41 ± 5 | El4 cells protease | BD cytoflex flow cytometry | EL4 cells after Shield-1 removal | N.A. | None | None | N.A. | |||
| 29122441 | 2018 | FAMP1 | 18 | FAM | Amidation | Cyclic (C10-C13 Disulfide Bond) | L | None | Synthetic | N.A. | 37 C | 10 µM | 7 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29122441 | 2018 | FAMP1 | 18 | FAM | Amidation | Cyclic (C10-C13 Disulfide Bond) | L | None | Synthetic | Increases Half Life | 37 C | 10 µM | 21 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29122441 | 2018 | FAM-P2 | 18 | FAM | Amidation | Cyclic (C10-C14 Disulfide Bond) | L | None | Synthetic | N.A. | 37 C | 10 µM | 16 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29122441 | 2018 | FAM-P2.L5 | 18 | FAM | Amidation | Cyclic (C10-C14 Disulfide Bond) | L | 1,3-bis(bromomethyl)benzene linker (L5) for stapling i, i+4 spacing | Synthetic | Increases Half Life | 37 C | 10 µM | 10 | 293T cells lysates protease | RP-HPLC-FD | 293T cells lysate | In Vitro | None | None | N.A. | |||
| 29104145 | 2018 | AS16 | 7 | Free | Free | Linear | L | None | Synthetic | Antitumor | Blood samples were taken at 0 min, 5min,30 min, 2 h, 4 h, 6 h, 8 h, 10 h and 24h from orbit | 45 mg/kg | 1 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | The activity value of AS16-Fc, as observed in vivo, is its significant inhibition of tumor growth and reduction in M2-polarized macrophages and vessel density in the MCA-205 tumor model | |||
| 29051342 | 2018 | 68Ga-NOTA-UBI | 13 | 68Ga-NOTA | Free | Linear | L | None | Synthetic | Nuclear Imaging of Infectious Diseases | Image acquisition started 30, 60 and 120 min after IV | N.A. | 29 | NHP blood protease | PET-CT imaging | NHP blood sample | In Vivo | None | None | N.A. | |||
| 28948296 | 2018 | GIP(3-30)NH2 | 27 | Free | Amidation | Linear | L | None | GIP analogue | GIP receptor antagonist | Blood samples were drawn 30, 15 and 0 min before and 20, 25, 30, 40, 50, 60, 67, 70, 75, 80, 95 and 125 min after the start of the GIP(3-30)NH2 infusion | 800 pmol/kg/min | 7.6 ± 1.4 (Elimination Half Life) | Human plasma protease | RIA | Human plasma | In Vivo | None | None | IC50 value of 87.6 nmol/l | |||
| N.A. | 2018 | Example 7 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, B3E, desB27, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 44 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 10.5 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27 modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 45 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27 modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 52 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27,modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 29 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 5 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 35 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 7.6 | |||
| N.A. | 2018 | Example 9 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, A21A, B3Q, desB27, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 30 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 16.7 | |||
| N.A. | 2018 | Example 7 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, B3E, desB27, modififcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 30 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 10.5 | |||
| N.A. | 2018 | Example 4 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B3E, desB27,modificaitons | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 31 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 9.3 | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 45 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Prior Art analogue 3 | 50 | Free | B29K(N(Eps)Tetradecanedioyl), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 50 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Example 23 | 49 | Free | B29K(N(Eps)Hexadecanedioyl-4×gGlu), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3Q, desB27, modifications | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 55 | SD rats plasma protease | ELISA | SD rats plasma with Zinc Ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 1.54 | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 1.96 ± 0.05 | Rats plasma protease | RIA | Rats plasma without NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 9.94 ± 1.40 | Rats plasma protease | RIA | Rats plasma with NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 14.9 ± 3.1 | Rats plasma protease | RIA | Rats plasma without NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 12.7 ± 1.2 | Rats plasma protease | RIA | Rats plasma with NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 10 nmol/kg | 4.34 ± 0.20 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 11 nmol/kg | 15.03 ± 4.31 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22) | 34 | Ghrelin (12-28) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 12 nmol/kg | 17.75 ± 3.99 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22) | 34 | Ghrelin (12-28) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 13 nmol/kg | 14.86 ± 2.64 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28)amide | 34 | Free | Ghrelin(12-28)amide | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 14 nmol/kg | 14.50 ± 0.85 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22)ghrelin(12-28) | 51 | Free | Ghrelin(12-28) | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 15 nmol/kg | 18.40 ± 2.05 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | Agonist activity of ghrelin(12-28)CNP(6-22)ghrelin(12-28) was also the lowest | |||
| 28899838 | 2017 | Ghrelin(28-12)CNP(6-22)ghrelin(12-28) | 51 | Reversed sequence ghrelin(28-12) fused to the N-terminal side of CNP(6-22) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 16 nmol/kg | 17.38 ± 1.00 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | Ghrelin(28-12)CNP(6-22)ghrelin(12-28) exhibited lower potency than that of ghrelin(28-12)CNP(6-22) and CNP(6-22)ghrelin(12-28) | |||
| 28800217 | 2017 | Peptide 22 | 34 | Free | Free | Linear | L | Ala5 substituition in GpTx-1 | derived from Grammostola porteri (Tarantula spider) (Lasiodora porteri) | Potently inhibits the voltage-gated sodium channels Nav1.7/Scn9A | At 0.5, 1, 1.25, 1.5,2,3, and 4 hours post-dose, 3 mice were euthanized and then blood samples were collected | 5 mg/kg | 0.605 | Mice plasma protease | LC-MS/MS | Mice serum | In Vivo | https://sci-hub.se/10.1021/jm501765v | None | IC50=0.58-10 nM for GpTx-1 | |||
| 28799326 | 2017 | GLP-1 | 31 | Free | Free | Linear | L | None | GLP-1 | Antidiabetes | Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours | 5 mg/kg | 0.03 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | PDB id: 5VAI | None | EC50 = 5.257*10-11 | |||
| 28771355 | 2017 | GLP-1 analogue 4 | 31 | Free | Free | Linear | L | K34R substituition at GLP-1, Conjugated with indomethacin via γGlu attached to the ε-amine of Lys26 of the GLP-1 analog | GLP-1 analogs | Antidiabetes | Blood sampled at eight time-points within 24 h | 5 mL/kg | 55 | Lean mice plasma protease | Luminescent Oxygen Channeling Immunoassay | Lean mice plasma | In Vivo | None | None | GLP-1R EC50 ± SEM (nM) = 0.068 ± 0.037 | |||
| 28714475 | 2017 | tagPK128 | 22 | tag | Free | Bicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit plasma kallikrein | N.A. | 0.5 mg/kg | 0.9 ± 0.2 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin | |||
| 28714475 | 2017 | tagUK18 | 24 | tag | Free | Bicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit urokinase | N.A. | 0.5 mg/kg | 1.0 ± 0.1 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 780±110 for rat albumin | |||
| 28714475 | 2017 | UK18 | 17 | Free | Free | Bicyclic(C2-C9,C9-C16 Disulfide Bond) | L | None | Synthetic | Inhibit urokinase | N.A. | 0.3 mg/kg | 0.30 ± 0.02 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) > 100,000 for rat albumin | |||
| 28714475 | 2017 | tag-3xPEG24-FXIIa inhibitor | N.A. | Tag-3xPEG24 | Amidation | Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor) | L | None | Synthetic | FXIIa Inhibitor | N.A. | 5 mg/kg | 1.0 ± 0.2 (T1/2a) | Rabbit plasma protease | RP-HPLC using fluorescence detector | Rabbit plasma | In Vivo | None | None | (EC5x) at 4.2±0.5 mM | |||
| 28714475 | 2017 | FXIIa inhibitor | N.A. | Fluorescein (F) | Amidation | Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor) | L | None | Synthetic | FXIIa Inhibitor | N.A. | 3.7 mg/kg | 0.21 ± 0.04 (T1/2b) | Rabbit plasma protease | A single quadrupole liquid chromatography mass spectrometer | Rabbit plasma | In Vivo | None | None | Ki FXIIa = 4±0.9 nM in presence of albumin | |||
| 28711730 | 2017 | rhCNTF | 187 | Free | Free | Linear | L | None | Synthetic | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 34.28 | SD rats serum protease | ELISA | SD rats serum | In Vivo | PDB id: 1CNT | None | EC50±SD = 0.48±0.12ng/ml for rhCNTF | |||
| 28605180 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 80 µg/mL | 18 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 80 µg/mL | 50 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 | |||
| 28605180 | 2017 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Substituiting Asn28 with Gln28 | Exenatide analogs | Antidiabetes | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 49 µg/mL | 17 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 11 ±3.7 | |||
| 28605180 | 2017 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Substituiting Asn28 with Gln28 | Exenatide analogs | Antidiabetes | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 49 µg/mL | 48 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 11 ±3.7 | |||
| 28464043 | 2017 | KP-10 | 10 | Free | Amidation | Linear | L | None | kisspeptin analogue | Treatment of Specific Human Reproductive Disorders | 100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min) | 1 nmol | 4 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)77047-1/fulltext | None | N.A. | |||
| 28464043 | 2017 | KP-54 | 54 | Free | Amidation | Linear | L | None | kisspeptin analogue | Treatment of Specific Human Reproductive Disorders | 100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min) | 1 nmol | 32 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)77047-1/fulltext | None | N.A. | |||
| 28457895 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 1 hour | 25 nmol/kg | ~0.35 | ICR mice retro-orbital sinus protease | Exenatide ELISA | ICR mice retro-orbital sinus | In Vivo | PDB id: 7MLL | None | both exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity | |||
| 28416744 | 2017 | cRGD-ZW800-1 | 5 | Free | ZW800-1 fluorophore | Cyclic (RGDyK) | Mix | y = D-Tyr | Synthetic | Generic tracer for Intraoperative Near-Infrared Fluorescence Imaging of Solid Tumors | Time points -5, 1, 6, 10, 20, 30, 40, 50, 60, 90, 120, and 240 min. post injection | 10 nmol | 25.3 ± 6.4 | Mice serum protease | Fluorescence assay | Mice serum | In Vivo | None | None | In vitro competition for binding cRGD-ZW800-1 (500 nM) with a 1:1 molar ratio of unlabeled cRGD (500 nM) resulted in a reduction of 32% on the HT-29 cells and 36% on the high integrin-expressing U-87 MG cells compared to cells treated without unlabeled cRGD | |||
| 28373972 | 2017 | Api88 | 18 | Gu: N,N,N',N' tetramethylguanidino | Amidation | Linear | L | O denotes L-ornithine | Apidaecin analog | Antibacterial | After 10, 20, 30, 60, or90 min animals (n = 7) | 5 mg/kg | 17.3 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | MIC = Api88 > Api137 | |||
| 28373972 | 2017 | Api88 | 18 | Gu: N,N,N',N' tetramethylguanidino | Amidation | Linear | L | O denotes L-ornithine | Apidaecin analog | Antibacterial | After 10, 20, 30, 60, or90 min animals (n = 7) | 20 mg/kg | 11.1 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | MIC = Api88 > Api137 | |||
| 28373972 | 2017 | Api137 | 18 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O denotes L-ornithine | Apidaecin analog | Antimicrobial | After 10, 20, 30, 60, or90 min animals (n = 7) | 5 mg/kg | 33.8 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | The minimum inhibitory concentration (MIC) value for Api137 against E. coli ATCC 25922 is 4 µg/mL. | |||
| 28373972 | 2017 | Api137 | 18 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O denotes L-ornithine | Apidaecin analog | Antimicrobial | After 10, 20, 30, 60, or90 min animals (n = 7) | 20 mg/kg | 16.9 | Mice plasma protease | RP-HPLC-ESI-MS | Mice plasma | In Vivo | None | None | The minimum inhibitory concentration (MIC) value for Api137 against E. coli ATCC 25922 is 4 µg/mL. | |||
| 28281868 | 2017 | eTGFBR2 | 112 | Free | Free | Linear | L | None | Synthetic | Neutralize TGF-Β1 activity | Blood samples were collected through the eyes at 5 min, 15 min, 30 min, 60 min, 120 min | 3 nmol/kg | 41.42 | Mice serum protease | Human TGF-b RII Duo Set ELISA | Mice serum | In Vivo | None | None | KD = 9.49* 10-9M of eTGFBR2 for TGF-B1 | |||
| 28209419 | 2017 | Native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | Samples were taken prior to GLP-2 administration and at 60, 90 and 180 min post injection on Day 3 of therapy or Day 42 | 2.5 μg/kg | ~45 | Human plasma protease | GLP-2 (1–33) specific radioimmunoassay | Infant human plasma | In Vivo | PDB id: 2L63 | None | N.A. | |||
| 28138743 | 2017 | CP-11 | 13 | Free | Amidation | Linear | L | None | Synthetic | Antimicrobial | A plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h) | 10 μM | 0.21 | Mouse plasma protease | LC-HRMS. | Mouse plasma | In Vitro | None | None | N.A. | |||
| 28138743 | 2017 | Omiganan | 13 | Free | Amidation | Linear | L | None | Analogue of indolicidin | Antimicrobial | A plasma aliquot was withdrawn at each time-point(0, 0.16, 0.5, 1, 2, 4 h) | 10 μM | 0.83 | Mouse plasma protease | LC-HRMS. | Mouse plasma | In Vitro | None | None | N.A. | |||
| 28097629 | 2017 | TP508 | 23 | Free | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 13.7 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG5k-TP508 | 23 | PEG5K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 11.5 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28010844 | 2017 | Octreotide | 8 | D-amino acid Phe | Free | Cyclic (C2-C7 Disulfide Linkage) | Mix | D-amino acid substituitons Trp | SST analog | Anticancer and treatment of Endocrine Diseases | The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min | 50 mg/kg | 28 | Mouse stomach tissue lysate protease | HPLC-MS | Mouse stomach tissue lysate | In Vivo | https://sci-hub.st/10.1177/106002808802201001 | None | N.A. | |||
| 28010844 | 2017 | Octreotide | 8 | D-amino acid Phe | Free | Cyclic (C2-C7 Disulfide Linkage) | Mix | D-amino acid substituitons Trp | SST analog | Anticancer and treatment of Endocrine Diseases | The mice were sacrificed at 10, 20, 40, 60, 120, 240 and 360 min | 50 mg/kg | 37.7 | Mouse intestine tissue lysate protease | MALDI-TOF-MSI and LC-MS/MS | Mouse intestine tissue lysate | In Vivo | None | None | N.A. | |||
| 27815337 | 2017 | pE13F | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 7.2 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 300 ± 182 | |||
| 27815337 | 2017 | K17F | 17 | Free | Free | Linear | L | None | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 4.6 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 15 ± 3.6 | |||
| 27815337 | 2017 | P92 | 17 | Acetylation | Pro(4-Br)Phe substituition | Linear | Mix | Aib, DLeu,DGln, ProNle, D-Arg at position 3 | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 24 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 4 ± 2.4 | |||
| 27784692 | 2017 | ELP | 815 | Free | Free | Linear | L | x = Val,Gly or Ala | Synthetic | Carrier protein | Whole-animal fluorescence images were collected at regular intervals for 24 hours | 100 mg/kg | 52.6 (T1/2,Terminal) | Rats plasma protease | whole-body fluorescence imaging | Rats plasma | In Vivo | None | None | KTP-ELP, ELP, and SynB1-ELP show no toxicity in any of the renal cell lines tested, even at concentrations up to 40 μM for 72 hours | |||
| 27689406 | 2017 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 3.2 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27689406 | 2017 | GLP-1 | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 1.2 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | PDB id: 5VAI | None | N.A. | |||
| 27689406 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Exendin-4 | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 35.1 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | PDB id: 7MLL | None | EC50 (pM) = 1.8 ± 0.8 | |||
| 27689406 | 2017 | X1 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Antiobesity | N.A. | N.A. | 3.9 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27689406 | 2017 | X2 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Antiobesity | N.A. | N.A. | 16.1 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27689406 | 2017 | X3 | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | N.A. | Antiobesity | N.A. | N.A. | 21.3 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27539157 | 2017 | Anti‐VEGF PCCs Bi‐LV | 23 | X1 = biotin-PEG3 label | lfreW = D and L -amino acids | Cyclic | Mix | Tz4 = triazole linker | Synthetic | In vivo imaging probe and an Anti‐PA peptide | Blood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min | 1 mg/kg | 7 (Elimination Half Life) | Mice plasma protease | LC‐MS/MS assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 27539157 | 2017 | Anti‐VEGF PCCs Tri‐LV | 28 | X1 = biotin-PEG3 label | eeird = D-amino acids | Cyclic | Mix | Tz4 = triazole linker | Synthetic | In vivo imaging probe and an Anti‐PA peptide | Blood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min | 1 mg/kg | 36 (Elimination Half Life) | Mice plasma protease | LC‐MS/MS assay | Mice plasma | In Vivo | None | None | IC50 = 2.6 ± 0.5 nM | |||
| N.A. | 2017 | SEQ ID NO 62 | 152 | Free | Free | Linear | L | None | Lipocalin muteins | Pcsk9-Specific Lipocalin Muteins | N.A. | N.A. | 0.99 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | US 201715445066 A | IC50(nM) = 1.36 without HSA for LDLR binding | |||
| N.A. | 2017 | SEQ ID NO 82 | 153 | Free | Free | Linear | L | None | Lipocalin muteins | Pcsk9-Specific Lipocalin Muteins | N.A. | N.A. | 0.86 | Rats plasma protease | Sandwich ELISA | Rats plasma | In Vivo | None | US 201715445066 A | IC50(nM) = 1.68 without HSA for LDLR binding | |||
| 27558296 | 2016 | Compound 1 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 0.025 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 2.6 ± 1.0 | |||
| 27558296 | 2016 | Compound 2 | 13 | pGlu = Pyroglutamate | Free | Linear | L | Nle = Norleucine at position 11 | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 0.13 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 2.0 ± 0.3 | |||
| 27558296 | 2016 | Compound 26 | 14 | pGlu = Pyroglutamate | Free | Cyclic (C2-C7 Disulfide Linkage) | L | Nle = Norleucine at position 12 | Apelin analogs | Inotropic Agent | Time points (0, 0.17, 0.5, 1, 2, 4, 6, 24 and 27 h) | 1 µg/mL | 0.1 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) > 1000 | |||
| 27558296 | 2016 | Compound 31 | 13 | Palmitic acid conjugation | Free | Linear | L | Gly9 was exchanged with Lys, TAMRA = 5,6-carboxytetramethylrhodamine at Lys9 modification at Lysine , Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid at position 12 | compound 31 analogues | Inotropic Agent | 37 C | 0.00001 M | 0.36 | Wistar rats plasma protease | HPLC | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 21.6 ± 4.5 for compound 31 | |||
| 27217590 | 2016 | OT (oxytocin) | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | None | Produced in the hypothalamus and released by the posterior pituitary gland | Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia | Time points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours | 0.1 mg/kg | 0.12 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | https://sci-hub.st/10.1016/s0079-6123(08)00417-2 | None | EC50(nM) = 0.039 (OTR agonist) | |||
| 27217590 | 2016 | OT (oxytocin) | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | None | Produced in the hypothalamus and released by the posterior pituitary gland | Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia | Time points postdose: 0.25 (OT only), 0.5, 1, 2, 4, 6, and 24 hours (6- and 24-hour sampling limited to PF1 only | 10 ml/kg | 0.5 | C57Bl/6J mice plasma protease | LC-MS/MS | C57BL/6J mice plasma | In Vivo | PDB id: 2MGO | None | EC50(nM) = 0.039 (OTR agonist) | |||
| 27166982 | 2016 | ADM analogue 3 | 39 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (C3-C8 Disulfide Linkage) | L | None | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 3.3 | Porcine liver homogenate protease | RP-HPLC | Porcine liver homogenate | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 20 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | Nα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 38 | Porcine liver homogenate protease | RP-HPLC | Porcine liver homogenate | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 10.1 ± 0.5 (Elimination Half Life) | Human blood plasma protease | RIA | Human blood plasma with 2 × 100 mg sitagliptin | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 9.4 ± 0.8 (Elimination Half Life) | Human blood plasma protease | RIA | Human blood plasma | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 14.9 ± 1.3 (Elimination Half Life) | Human blood plasma protease | RIA (total PYY assay) | Human blood plasma | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26808199 | 2016 | PYY24–36 | 13 | Free | Amidation | Linear | L | None | PYY analog | Antiobesity | An amount of 100 lL of plasma was removed from the incubations at 0, 1, 2, 4, 6,8, 12, and 24 h time-point | 1000 ng/mL | <0.5 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26774588 | 2016 | PYY3-35 | 33 | Free | Free | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 6 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-35 | 33 | Free | Free | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 39 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma with 10 mM EDTA | In Vitro | None | None | N.A. | |||
| 26752086 | 2016 | BB28 | 31 | conjugating a truncated antimicrobial peptide B28 to the N-terminus of the tumor-homing peptide bombesin | Amidation | Linear | L | Biotinylation | Synthetic | Antitumor | N.A. | 30 nmol | <5 | BALB/c mice plasma protease | ELISA | BALB/c mice plasma | In Vivo | None | None | IC50 ranges from 2.5–3.0 mM (In the absence of FBS) for BB28 | |||
| 26741458 | 2016 | Peptide 1 | 6 | Free | Free | Linear | L | None | Synthetic | Hydrogelators | Degradation was monitored after 0, 1, 2, 3, 4, 5, and 10 min | 34 μM | 3.43 ± 0.06 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26741458 | 2016 | Peptide 2 | 8 | Free | Free | Linear | L | β3-homophenylalanine (β3-hPhe) at position 3 and 6 | Synthetic | Hydrogelators | During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min. | 33 μM | 19.53 ± 0.55 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26741458 | 2016 | Peptide 3 | 8 | Free | Amidation | Linear | L | β3-homophenylalanine (β3-hPhe) at position 3 and 6 | Synthetic | Hydrogelators | During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min. | 33 μM | 40.00 ± 1.28 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26741458 | 2016 | Peptide 4 | 8 | Free | Amidation | Linear | L | β3-homophenylalanine (β3-hPhe) at position 3 and 6, substitution of Phe with Tyr at positions 4 and 7 | Synthetic | Hydrogelators | During the stability study of mixed α/β-peptides, samples were taken after 0, 5, 10, 15, 30, 60, 90, 120, 240, and 1500 min. | 33 μM | 18.71 ± 0.44 | Human blood plasma protease | HPLC | Human blood plasma | In Vitro | None | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 0.05784 | Chymotrypsin | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with Chymotrypsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26628555 | 2016 | HLDF-6-NH2 | 6 | 3H labeling at N terminal | Amidation | Linear | L | None | Isolated from the culture medium of retinoic acid-treated HL-60 cells | Neuroprotective And Nootropic Activities | N.A. | N.A. | 8 | Wistar rats blood plasma protease | N.A. | Wistar rats blood plasma | In Vivo | None | None | ChAT activity, dpm/mg of tissue = 5.61±0.40 in (βA + HLDF-6-NH2,250 µg/kg) | |||
| 26628555 | 2016 | HLDF-6-OH | 6 | 3H labeling at N terminal | Free | Linear | L | None | Isolated from the culture medium of retinoic acid-treated HL-60 cells | Neuroprotective And Nootropic Activities | N.A. | N.A. | 2 | Wistar rats blood plasma protease | N.A. | Wistar rats blood plasma | In Vivo | None | None | ChAT activity, dpm/mg of tissue = 5.29±0.34 in (βA + HLDF-6-OH,250 µg/kg) | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 20 mg | 5.9 | Human serum protease | HPLC–MS/MS | Human serum (Japanese) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 80 mg | 13.7 | Human serum protease | HPLC–MS/MS | Human serum (Japanese) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 240 mg | 23.5 | Human serum protease | HPLC–MS/MS | Human serum (Japanese) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 20 mg | 6.9 | Human serum protease | HPLC–MS/MS | Human serum ( Caucasians) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 80 mg | 14.4 | Human serum protease | HPLC–MS/MS | Human serum ( Caucasians) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 26242382 | 2016 | JNJ-54452840 | 18 | Free | Free | Cyclic (C4-C10 Disulfide Linkage And Terminal Ala1-Glu18 Linkage) | L | None | Synthetic | Treatment for Chronic Heart Failure | Blood sample collected at the following timepoints relative to the start of the infusion: predose; at 1 min (end of infusion); at 5, 7, 10, 15, 20, 30 and 45 min; and at 1, 2, 4, 8 and 24 h postdose | 240 mg | 26.1 | Human serum protease | HPLC–MS/MS | Human serum ( Caucasians) | In Vivo | Pubchem id: 86278343 | None | N.A. | |||
| 133-353-120-049-121 | 2016 | rHuEPO-Fc | 399 | Free | Free | Linear | L | Fusion with IgG Fc fragment | Human erythropoietic protein Fusion with IgG Fc fragment | Immunogenic | N.A. | 5 ug/kg | 35.24+/-5.15 | Not mentioned | ELISA | Blood | in vivo | https://lens.org/133-353-120-049-121 | US 9,375,487 B2 | N.A. |