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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 | 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 | |||
| 20844765 | 2010 | Lfc8 | 11 | Free | Free | Cyclic (head-to-tail backbone cyclization) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 110 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=3.8 μM for E.coli | |||
| 20844765 | 2010 | Lfc8 | 11 | Free | Free | Cyclic (head-to-tail backbone cyclization) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 110 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=15μM for S. Aureus | |||
| 20844765 | 2010 | Lfc8 | 11 | Free | Free | Cyclic (head-to-tail backbone cyclization) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 110 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99 ‰¤ 0.45μM for B. subtilis | |||
| 20844765 | 2010 | Lfc9 | 13 | Free | Amidation | Cyclic (C1-C13) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 110 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=1.9 μM for E.coli | |||
| 20844765 | 2010 | Lfc9 | 13 | Free | Amidation | Cyclic (C1-C13) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 110 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99 ‰¤ 0.45μM for S. Aureus | |||
| 20844765 | 2010 | Lfc9 | 13 | Free | Amidation | Cyclic (C1-C13) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 110 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99 ‰¤ 0.45μM 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 5a | 18 | Acetylation [(C6H6)-(C6H12)-(C6H6)] | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 2mg/kg | 222 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=90nM 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 | |||
| 12699744 | 2003 | Peptide 5c | 18 | Acetylation [(C6H6)(CH2)4CH3] | Amidation | Linear | L | None | Synthetic | Anticoagulant | Not reported | 2mg/kg | 79.1 | Rabbit blood proteases | ELISA | Intravenouly administered into rabbit blood | in vivo | None | None | IC50=22nM for fVIIa binding assay in presence 0f 0.1% rabbit serum albumin | |||
| 2147696 | 1990 | Synthetic peptide | 10 | Free | Free | Linear | L | None | Synthetic peptide (corresponding to amino acids 605-614 of human protein S) | Anticoagulant | Not reported | Not mentioned | 80 | Rabbit blood proteases | Spectrofluorometry | Intravenously injected in male New Zealand white rabbits and blood samples withdrawn and plasma sample prepared | in vivo | None | None | 34% of 125I protein S bound to C4b-binding protein in presence of 150 µM of peptide | |||
| 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 | |||
| 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3 µg/ml for M. Luteus ATCC 9341 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. Luteus ATCC 9342 | |||
| 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=3.12 µg/ml for M. Luteus ATCC 9344 | |||
| 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=10 µg/ml for S. Aureus ATCC 6540 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for S. Aureus ATCC 6541 | |||
| 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=9 µg/ml for S. Aureus ATCC 6543 | |||
| 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=1.56 µg/ml for S. Epidemidis ATCC 12229 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=2 µg/ml for S. Epidemidis ATCC 12228 | |||
| 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=50 µg/ml for MRSA SR 1553 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=>100 µg/ml for MRSA SR 1554 | |||
| 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=38 µg/ml for MRSA SR 1556 | |||
| 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 µg/ml for M. smegmatis ATCC 607 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for M. smegmatis ATCC 613 | |||
| 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=12.5 µg/ml for E. coli ATCC 2592 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=31 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=19 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for P. aeruginosa ATCC 9027 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=25 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 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 | KSL3 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=6.25 µg/ml for C. albicans ATCC 36232 | |||
| 10461747 | 1998 | KSL4 | 10 | Free | Free | Linear | Mix | Reduced amide bonds Ψ(CH2NH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | >81 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=31 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 | KSL6 | 10 | Free | Free | Linear | Mix | Reduced carbamate Ψ(CH2OCONH) | Synthetic | Antimicrobial | Not reported | 100 µg/mL | 67 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC=11 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 | |||
| 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 | |||
| 20587645 | 2010 | PEG20k-HM-3 | 16 | Methoxy-polyethylene glycol-Succinimidyl Carbonate (SC-mPEG, molecular weight 20 kDa, named SC-mPEG20k ) | Free | Linear | L | None | HM-3 analogue | Anti-angiogenetic | Not mentioned | Not mentioned | >132 | SD rat plasma proteases | RP-HPLC | SD rat plasma | in vitro | http://pubs.rsc.org/En/content/articlepdf/2014/tb/ | None | 44.35% inhibitory effect on mouse tumors | |||
| 20587645 | 2010 | mPEG-ALD10k-HM-3 | 16 | Methoxy-polyethylene glycolPEG-aldehyde (mPEG-ALD10k ) | Free | Linear | L | None | HM-3 analogue | Anti-angiogenetic | Not mentioned | Not mentioned | 162.08 ±36.57 | Proteases in chorioallantoic membrane of chick embryo | RP-HPLC | Chorioallantoic membrane of chick embryo | in vivo | http://pubs.rsc.org/En/content/articlepdf/2014/tb/ | None | Dramatically inhibits angiogenesis on the chorioallantoic membrane of chick embryo | |||
| 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 | |||
| 19159331 | 2009 | Peptide 1 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 2.7013 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 2 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0629 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 3 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0556 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 4 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0103 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 5 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0088 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 6 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0122 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 7 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0101 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 8 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0094 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 9 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1969 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 10 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.2897 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 11 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0485 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 12 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1557 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 13 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.089 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 14 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0469 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 15 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.2911 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 16 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1596 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 17 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0512 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 18 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0132 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 19 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0077 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 20 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0111 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 21 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0135 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 22 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0122 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 23 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0092 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 24 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.021 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 25 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0027 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 26 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0094 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 27 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0069 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 28 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0119 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 29 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1526 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 30 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 25.2445 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 31 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 40.1296 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 32 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 17.8114 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 33 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 7.122 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 34 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 13.4815 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 35 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 6.4814 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 36 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 4.3435 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 37 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.1378 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 38 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1177 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 39 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0148 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 40 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0527 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 41 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1504 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 42 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0939 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 43 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 4.1593 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 44 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 20.6999 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 45 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.2963 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 46 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.012 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 47 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0026 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 48 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0037 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 49 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0019 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 50 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0035 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 51 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0031 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 52 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0052 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 53 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1052 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 54 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 11.4998 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 55 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.466 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 56 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1016 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 57 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.3817 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 58 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1101 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 59 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0263 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 60 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0128 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 61 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0225 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 62 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0244 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 63 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0238 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 64 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0336 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 65 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0242 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 66 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0812 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 67 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1293 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 68 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0514 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 69 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0325 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 70 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0224 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 71 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0156 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 72 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.2344 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 73 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 3.3348 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 74 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.7564 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 75 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.3309 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 76 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0066 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 77 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0072 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 78 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0038 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 79 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0049 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 80 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.3384 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 81 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1866 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 82 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 4.5647 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 83 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.2013 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 84 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0195 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 85 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0264 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 86 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0165 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 87 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0087 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 88 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0051 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 89 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0054 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 90 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0039 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 91 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0053 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 92 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0131 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 93 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0329 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 94 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 7.6573 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 95 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.6468 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 96 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0033 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 97 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0047 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 98 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0063 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 99 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.131 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 100 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 2.1948 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 101 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 19.4782 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 102 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 3.8079 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 103 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.124 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 104 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.088 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 105 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.006 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 106 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0025 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 107 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0015 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 108 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.006 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 109 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0082 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 110 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1745 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 111 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0072 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 112 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0103 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 113 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0135 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 114 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0183 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 115 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0767 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 116 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0648 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 117 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 3.844 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 118 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1692 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 119 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0949 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 120 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0317 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 121 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.323 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 122 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 8.3587 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 123 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.3722 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 124 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1719 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 125 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.0014 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 126 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.5162 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 127 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0686 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 128 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0663 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 129 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0667 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 130 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0541 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 131 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0563 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 132 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.4176 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 133 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.5842 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 134 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.9286 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 135 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0399 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 136 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0072 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 137 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0037 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 138 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0008 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 139 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0017 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 140 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0044 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 141 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0088 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 142 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0056 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 143 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0367 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 144 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0093 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 145 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0124 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 146 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0294 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 147 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0787 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 148 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1194 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 149 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.8333 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 150 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0154 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 151 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0178 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 152 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.019 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 153 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1849 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 154 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.7012 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 155 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.6149 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 156 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.5216 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 157 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.5455 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 158 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0401 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 159 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0451 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 160 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0465 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 161 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0192 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 162 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1691 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 163 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1777 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 164 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1356 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 165 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.7772 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 166 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1388 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 167 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1025 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 168 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1284 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 169 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0967 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 170 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.7169 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 171 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 4.0618 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 172 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 3.1271 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 173 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0711 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 174 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0548 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 175 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0426 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 176 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0246 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 177 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0788 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 178 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0759 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 179 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0569 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 180 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0056 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 181 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0042 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 182 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0046 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 183 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0185 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 184 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0929 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 185 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0719 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 186 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0048 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 187 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0015 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 188 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0012 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 189 | 10 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0014 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 190 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0097 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 191 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0084 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 192 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0068 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 193 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0084 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 194 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0098 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 195 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0103 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 196 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0201 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 197 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0074 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 198 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0851 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 199 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0892 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 200 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0575 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 201 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0425 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 202 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0327 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 203 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0167 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 204 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0125 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 205 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0077 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 206 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0088 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 207 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0063 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 208 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0045 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 209 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0037 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 210 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.004 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 211 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0033 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 212 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0038 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 213 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0044 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 214 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0045 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 215 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0085 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 216 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0111 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 217 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0131 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 218 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1209 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 219 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 5.693 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 220 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 6.4211 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 221 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 5.0348 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 222 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 1.3951 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 223 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.4688 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 224 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.193 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 225 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0267 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 226 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0499 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 227 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1029 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 228 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0614 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 229 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1104 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 230 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1963 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 231 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0514 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 232 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0223 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 233 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0054 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 234 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0025 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 235 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0011 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 236 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0014 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 237 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0011 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 238 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0032 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 239 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0031 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 240 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0023 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 241 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0028 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 242 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0281 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 243 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.2682 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 244 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1018 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 245 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0298 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 246 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0143 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 247 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0152 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 248 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0093 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 249 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0085 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 250 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0052 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 251 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0085 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 252 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.011 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 253 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0207 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 254 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0155 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 255 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0183 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 256 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0247 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 257 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0297 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 258 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0322 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 259 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0223 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 260 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0078 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 261 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1455 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 262 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0095 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 263 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0099 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 264 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0085 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 265 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0032 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 266 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0033 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 267 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.005 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 268 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0069 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 269 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1618 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 270 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0332 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 271 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0371 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 272 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0236 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 273 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.008 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 274 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0051 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 275 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0061 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 276 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.003 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 277 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0028 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 278 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0037 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 279 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0057 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 280 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0084 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 281 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0101 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 282 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0037 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 283 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0047 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 284 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0049 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 285 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0041 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 286 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0076 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 287 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.005 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 288 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1097 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 289 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1086 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 290 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0696 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 291 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0055 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 292 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.002 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 293 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0022 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 294 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0021 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 295 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0025 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 296 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0021 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 297 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0047 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 298 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0026 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 299 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0075 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 300 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0073 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 301 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0034 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 302 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0134 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 303 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.022 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 304 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0507 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 305 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.041 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 306 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0444 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 307 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0325 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 308 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0306 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 309 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0139 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 310 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1049 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 311 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.2344 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 312 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1597 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 313 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0265 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 314 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0393 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 315 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0228 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 316 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0345 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 317 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0424 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 318 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0653 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 319 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0497 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 320 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0286 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 321 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0414 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 322 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0139 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 323 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.006 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 324 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0021 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 325 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0021 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 326 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0014 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 327 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0012 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 328 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0016 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 329 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.003 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 330 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0054 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 331 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0051 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 332 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0321 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 333 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0225 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 334 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0211 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 335 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0298 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 336 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.017 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 337 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0276 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 338 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0241 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 339 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0262 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 340 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.024 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 341 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0361 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 342 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.2471 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 343 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.3682 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 344 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0601 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 345 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0601 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 346 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0526 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 347 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0502 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 348 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0475 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 349 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0463 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 350 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0154 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 351 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1789 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 352 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0901 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 353 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0783 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 354 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1269 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 355 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1531 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 356 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.195 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 357 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1676 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 358 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.1212 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 359 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0694 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 360 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0475 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 361 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0261 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 362 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0214 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 363 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0322 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 364 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0389 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 365 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0233 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 366 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0029 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 367 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0038 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 368 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0031 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 369 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0038 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 370 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0046 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 371 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0055 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 372 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0038 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 373 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0025 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 374 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0008 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 19159331 | 2009 | Peptide 375 | 16 | 2,4-dichlorophenoxyacetic acid with (CH2)n-spacers | Biotinylation with PEG spacer | Linear | L | None | Synthetic | Not mentioned | 120 minutes | 67 pico molar | 0.0009 | Murine crude intestinal proteases | Proteolysis assay | Murine crude intestinal protease preparetion | in vitro | None | None | Not reported | |||
| 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-Agp | 12 | Free | Amidation | Linear | L | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub3 | Antimicrobial | Not reported | 150 µg/ml | >480 | 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-DAgp | 14 | Free | Amidation | Linear | Mix | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub5 | Antimicrobial | Not reported | 150 µg/ml | >480 | 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-Agp | 12 | Free | Amidation | Linear | L | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub3 | Antimicrobial | Not reported | 150 µg/ml | >480 | 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 | |||
| 20585128 | 2010 | Sub3-DAgp | 14 | Free | Amidation | Linear | Mix | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub5 | Antimicrobial | Not reported | 150 µg/ml | >480 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=2 µg/ml for P. Aeruginosa | |||
| 2533571 | 1989 | Des-enkephalin-γ-endorphin | 12 | Free | Free | Linear | L | None | Endorphin derivative | Neuropeptide | Not reported | 0.1mM | 4.5 | Proteases in SVK14 keratinocytes | HPLC/liquid scintillation counting | SVK14 keratinocytes | in vitro | 3582424 | None | Not reported | |||
| 2533571 | 1989 | Des-enkephalin-γ-endorphin | 12 | Free | Free | Linear | L | None | Endorphin derivative | Neuropeptide | Not reported | 0.1mM | 4.1 | Proteases in fibroblasts | HPLC/liquid scintillation counting | Human fibroblasts | in vitro | 3582424 | None | Not reported | |||
| 2533571 | 1989 | Des-enkephalin-γ-endorphin | 12 | Free | Free | Linear | L | None | Endorphin derivative | Neuropeptide | Not reported | 0.1mM | 4.4 | Proteases in human fresh whole skin | HPLC/liquid scintillation counting | Human fresh whole skin | in vitro | 3582424 | None | Not reported | |||
| 2533571 | 1989 | Des-enkephalin-γ-endorphin | 12 | Free | Free | Linear | L | None | Endorphin derivative | Neuropeptide | Not reported | 0.1mM | 4.6 | Proteases in human fresh epidermis | HPLC/liquid scintillation counting | Human fresh epidermis | in vitro | 3582424 | None | Not reported | |||
| 2533571 | 1989 | Des-enkephalin-γ-endorphin | 12 | Free | Free | Linear | L | None | Endorphin derivative | Neuropeptide | Not reported | 0.1mM | 4.5 | Proteases in human fresh dermis | HPLC/liquid scintillation counting | Human fresh dermis | in vitro | 3582424 | None | Not reported | |||
| 3080478 | 1985 | C0-LAP | 15 | Free | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~300 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C4-LAP | 15 | Saturated acyl chain of 4 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~340 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C8-LAP | 15 | Saturated acyl chain of 8 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~410 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C12-LAP | 15 | Saturated acyl chain of 12 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~410 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C16-LAP | 15 | Saturated acyl chain of 16 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | 513 ±12 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 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 | |||
| 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 | SA21 | 18 | Acetylation | Amidation | Linear | L | None | Synthetic (Phage display library) | Not mentioned | Not reported | 106 cpm/200μl/mouse | 2.3 | Blood proteases | ESI-LC ˆ’MS/MS | Rabbit blood sample | in vivo | None | None | Dissociation equilibrium constant of peptide for albumin,Kd=320 ±22 | |||
| 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 | |||
| 16892368 | 2006 | C46 | 13 | Glycosylation | Amidation | Linear | L | None | Derived from T20 | HIV-1 fusion inhibitory peptide | Not reported | 40 ng peptide/200 mL plasma | 4.75 | Mouse plasma proteases | ELISA | Mouse plasma | in vitro | None | None | IC50=90nM | |||
| 16892368 | 2006 | C46 | 13 | Glycosylation | Amidation | Linear | L | None | Derived from T20 | HIV-1 fusion inhibitory peptide | Not reported | 41 ng peptide/200 mL plasma | 2 | Rat plasma proteases | ELISA | Rat plasma | in vitro | None | None | IC50=90nM | |||
| 16892368 | 2006 | C46 | 13 | Glycosylation | Amidation | Linear | L | None | Derived from T20 | HIV-1 fusion inhibitory peptide | Not reported | 40 ng peptide/200 mL buffer | 0.75 | Not mentioned | ELISA | PBS/1% BSA | in vitro | None | None | IC50=90nM | |||
| 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 | |||
| 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 | |||
| 19413309 | 2009 | PEG10k-HM-3 | 17 | Methoxypoly(ethylene glycol)-aldehyde (mPEG-ALD) | Free | Linear | L | None | RGD- modified endostatin derived peptide | Antitumor | Not reported | 1mg/ml | 162.08 ± 36.57 | Rat blood proteases | RP-HPLC | Rat blood serum (Intravenous injection) | in vivo | None | None | More active in the inhibition of angiogenesis in the chorioallantoic membrane of chick embryos | |||
| 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 | |||
| 19601640 | 2009 | TATp | 11 | Free | Free | Linear | L | None | Synthetic peptide | Cell penetrating peptide | Not reported | 10 µL | >400 | Not mentioned | HPLC | Human plasma | in vitro | None | None | Not available | |||
| 19715558 | 2009 | RIAD | 18 | Free | Free | Linear | L | None | Synthetic peptide | Displaces PKA (protein kinase A) type I from the AKAP (A-kinase-anchoring protein) ezrin | Not reported | Not mentioned | 1.5 | Human serum proteases | HPLC | Human serum | in vitro | None | None | Not available | |||
| 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 | |||
| 19041716 | 2009 | LCNP/SST (encapsulated within Liquid crystalline nanoparticles) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Somatostatin encapsulated within Liquid crystalline nanoparticles | Neurotransmitter | Not reported | 1.8 mg/ml | 1.23 ±0.16 | Rat blood proteases | ELISA | Rat plasma (Intravenous injection) | in vivo | None | None | Not available | |||
| 19533722 | 2009 | C6 | 12 | Free | Free | Linear | L | None | Synthetic peptide | Mimic putative inhibitor epitopes (mimotopes), | Not reported | 150 µM | ~12 | Human plasma proteases | ELISA | Human plasma | in vitro | None | None | IC50 =30 €“50 µM | |||
| 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 | |||
| 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 | 19.3 | Mouse blood proteases | Not mentioned | Mice serum (Intravenous) | in vivo | None | None | LD50>6000mg/kg administered orally to mice | |||
| 3348603 | 1987 | DihydromycoplanecinA (DHMP A) | 10 | Free | 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 | 5.5 | Dog blood proteases | Not mentioned | Dog serum (Intravenous) | in vivo | None | None | LD50>6000mg/kg administered orally to mice | |||
| 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 | |||
| 8910426 | 1996 | LALF-10 (38 €“45) | 12 | Free | Free | Cyclic (C2-C11) | L | None | Analogue of Limulus anti-lipopolysaccharide factor | Antibacterial | Not reported | 2.5 µg/ml | 77 | Proteases present in fetal calf serum | RP-HPLC | Fetal calf serum | in vitro | None | None | LD50=2.58 mg/ml | |||
| 8910426 | 1996 | LALF-14 (36 €“47) | 16 | Free | Free | Cyclic (C2-C15) | L | None | Analogue of Limulus anti-lipopolysaccharide factor | Antibacterial | Not reported | 2.5 µg/ml | 84 | Proteases present in fetal calf serum | RP-HPLC | Fetal calf serum | in vitro | None | None | LD50=2.33 mg/ml | |||
| 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. | 2004 | [NMeEI, αMeL8]-Melan-A | 10 | Free | Free | Linear | L | Methylation of nitrogen of amide bond b/w Glu1 and Leu2 (NMe); Methylation of carboxyl of Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(0.5 nM); isomer2(20 nM) | |||
| N.A. | 2004 | [NMeEI, amide]-Melan-A | 10 | Free | Amidation | Linear | L | Methylation of nitrogen of amide bond b/w Glu1 and Leu2 (NMe) | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 12 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 1 nM | |||
| N.A. | 2004 | [pEI, amide]-Melan-A | 10 | PyroGlutamic acid at 1st position | Amidation | Linear | L | Pyroglutamic acid | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 11 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.3 nM | |||
| N.A. | 2004 | [pEI, αMeL8]-Melan-A | 10 | PyroGlutamic acid at 1st position | Free | Linear | L | Methylation of carboxyl of Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(0.02 nM); isomer2(3 nM) | |||
| N.A. | 2004 | [βAl, amide] -Melan-A | 10 | Beta-Alanine1 | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 11 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.03 nM | |||
| N.A. | 2004 | [βAl, αMeL8]-Melan-A | 10 | Beta-Alanine1 | Free | Linear | L | Methylation of carboxyl of Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(0.02 nM); isomer2(0.06 nM) | |||
| N.A. | 2004 | [βEl, amide]-Melan-A | 10 | Beta-Glu1 | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 20 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.3 nM | |||
| N.A. | 2004 | [βEl, αMeL8]-Melan-A | 10 | Beta-Glu1 | Free | Linear | L | Methylation of carboxyl of Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(0.3 nM); isomer2(0.015 nM) | |||
| N.A. | 2004 | [βDl, amide] -Melan-A | 10 | Beta-Asp1 | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 12 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 10 nM | |||
| N.A. | 2004 | [βDl, αMeL8]-Melan-A | 10 | Beta-Asp1 | Free | Linear | L | Methylation of carboxyl of Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(0.2 nM); isomer2(0.02 nM) | |||
| N.A. | 2004 | [NOHG1, amide]-Melan-A | 10 | Hydroxylation of N-terminal of Glycine | Amidation | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 13 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.04 nM | |||
| N.A. | 2004 | [NOHG1, αMeL8]-Melan-A | 10 | Hydroxylation of N-terminal of Glycine | Free | Linear | L | Methylation of carboxyl of Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(0.15 nM); isomer2(30 nM) | |||
| N.A. | 2004 | [αMeL2, αMeL8]-Melan-A | 10 | Free | Free | Linear | L | Methylation of carboxyl of Leu2 and Leu8 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= Not mentioned | |||
| N.A. | 2004 | [αMeL2, V10-amide]-Melan-A | 10 | Free | Amidation | Linear | L | Methylation of carboxyl of Leu2 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 12 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= isomer1(2.5 nM); isomer2(0.1 nM) | |||
| N.A. | 2004 | [αMeL2, NMeT9] -Melan-A | 10 | Free | Free | Linear | L | Methylation of carboxyl of Leu2 and amino-group of Thr9 used in peptide bond | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.5 nM | |||
| N.A. | 2004 | [αMeL2, dT9]-Melan-A | 10 | Free | Free | Linear | Mix | Methylation of carboxyl of Leu2 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 10.5 nM | |||
| N.A. | 2004 | [βAl, ψ8-9(CH2-NH)]-Melan-A | 10 | Beta-Alanine | Free | Linear | L | Reduced bond between Leu8 and Thr9 | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 24 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.35 nM | |||
| 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. | 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. | 2013 | SP16 | 13 | Free | Free | Linear | L | None | Human alpha-1-antitrypsin | Anti-inflammatory and immune modulator peptide | N.A. | 5 mg/ Kg | 1.9 | Rat blood proteases | LC-MS/MS | Rat plasma (Intravenous) | in vivo | None | WO2013106273A2 | Not mentioned | |||
| 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 | KK1 | 13 | Free | Free | Linear | L | N3-L-Hlys 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 | 153 ±4 | 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 | KK2 | 13 | Free | Free | Linear | L | N3-1d= COOH-CH(NH2)CH2-(CH2)3-CH2-NHMe 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 | 211 ±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 | KK3 | 13 | Free | Free | Linear | L | N3-2= COOH-CH(NH2)CH2-(CH2)3-CH2-NMe2at 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 | 126 ±18 | 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 | KK4 | 13 | Free | Free | Linear | L | N3-3= COOH-CH(NH2)CH2-(CH2)3-CH2-NMe2at 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 | 103 ±10 | 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 | KK5 | 13 | Free | Free | Linear | L | N3-L-lys 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 | 136 ±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 | KK6 | 13 | Free | Free | Linear | L | N3-4d= COOH-CH(NH2)CH2-(CH2)3-CH2-NHMe 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 | 128 ±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 | KK7 | 13 | Free | Free | Linear | L | N3-5d= COOH-CH(NH2)CH2-(CH2)3-CH2-NMe2 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 | 127 ±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 | KK8 | 13 | Free | Free | Linear | L | N3-6d= COOH-CH(NH2)CH2-(CH2)3-CH2-+NMe3 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 | 128 ±30 | 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 | KK9 | 13 | Free | Free | Linear | L | N3-L-Orn 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 | 134 ±27 | 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 | KK10 | 13 | Free | Free | Linear | L | N3-7d= COOH-CH(NH2)CH2-(CH2)3-CH2-+NHMe 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 | 131 ±27 | 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 | KK11 | 13 | Free | Free | Linear | L | N3-8d= COOH-CH(NH2)CH2-(CH2)3-CH2-Nme2 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 | 126 ±9 | 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 | KK12 | 13 | Free | Free | Linear | L | N3-9d= COOH-CH(NH2)CH2-(CH2)3-CH2-+Nme3 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 | 216 ±33 | 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 | KK13 | 13 | Free | Free | Linear | L | N3-L-Hlys 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 | >24 | 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 | KK14 | 13 | Free | Free | Linear | L | N3-L-Hlys 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 | >24 | 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 | KK15 | 13 | Free | Free | Linear | L | N3-L-Arg 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 | 174 ±7 | 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. | |||
| 12220890 | 2002 | Retro-inverso hemagglutinin [(HA) 91 €“108] derivative | 18 | Acetylation | Amidation | Linear | D | None | Derivative of B-cell epitope hemagglutinin (HA) 91 €“108 from influenza | Modulate immune response | Not mentioned | 1 mg/ml | >24 | 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. | |||
| 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 | 0.7 (distribution phase) | Rat blood proteases | RP-HPLC | Male wistar Rats (intravenously) | in vivo | 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 | |||
| 4070016 | 1985 | DEγE (Des-Enkephalin-γ-Endorphin) (β-endorphin-(6--17)) | 12 | Free | Free | Linear | L | None | CNS and piyuitary gland of Humans | Neuropeptide, non-opioid y-type endorphins | Not given | 1.0-1.15 µg | 0.6 (distribution phase) | Rat blood proteases | RP-HPLC | Male wistar Rats (intravenously) | in vivo | None | None | Not reported | |||
| 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. | |||
| 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. | |||
| 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 | |||
| 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 | 5 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 | 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 | 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 | 8 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 | 180 (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 | 9 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 | 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 | 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 | Human Fibrinopeptide A (FPA) | 16 | Free | Free | Linear | L | None | N terminal end of the A-alpha chain of fibrinogen | Blood clotting | 12 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 | 90 | 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 | 2 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 | 30 (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 | 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 | 4 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 | 30 | 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 | |||
| 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 | |||
| 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. | |||
| 2147684 | 1990 | Glucagon(19-29) | 11 | Free | Free | Linear | L | None | Glucagon derivative | Growth Hormone | Not mentioned | 200pmol/2.5ml | <10 | Hepatic plasma membrane proteases | Radioimmunoassay and HPLC | Hepatic plasma membrane | in vitro | None | None | Inhibit calcium pump at 20% concentration | |||
| 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 | |||
| 11778971 | 2001 | Glycosylated sms-14 | 14 | Dextran 70kDa conjugation | Free | Cyclic (C3-C14) | L | Glycosylation | Somatostatin derivative | Growth Hormone | 24 hours | 100 μl | 27 | Mice blood protease | HPLC | Subcutaneously injected in mice | in vivo | None | None | It inhibits tumor growth at IC50 ~2.5 nM | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 20.9 | None | RP-HPLC and Electrochemical Detection | Water | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | >24 | None | RP-HPLC and Electrochemical Detection | Acetic acid | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 4.4 | Human plasma proteases | RP-HPLC and Electrochemical Detection | Human plasma | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 14.6 | Mouse liver proteases | RP-HPLC and Electrochemical Detection | Mouse liver homogenate | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 22.8 | SCLC proteases | RP-HPLC and Electrochemical Detection | Small cell lung cancer (SCLC) | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist G [Arg6, D-Trp7,9, MePhe8] - substance P (6-11) | 17 | Free | Free | Linear | Mix | Methylation of phenylalanine at 3rd position | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 10 μg/ml | >24 | SCLC proteases | RP-HPLC and Electrochemical Detection | Small cell lung cancer (SCLC) | in vitro | None | None | Act as growth factors | |||
| 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 | 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 | |||
| 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 | |||
| 8353526 | 1993 | Trypsin modulating oostatic factor (TMOF) | 10 | Acetylation | Free | Linear | L | None | A. aegypti ovary | Growth regulatory peptide | Not mentioned | Not mentioned | 1.6 | Mosquito ovary endopeptidases | Radioimmunoassay | Ovaries of A. aegypti, Culex quinquefasciatus and Anopheles quadrimaculatus | in vivo | None | None | At concentrations of 3 x 10-9 M and 6.8 x 10-6 M, TMOF inhibited 50 and 90% of trypsin-like enzyme biosynthesis, respectively. | |||
| 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-2 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 1-2 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 67 | 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 | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-4 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 4-5 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 100 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-5 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 5-6 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | >500 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-6 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 6-7 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 80 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-7 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 7-8 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 192 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-8 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 8-9 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 191 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-9 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 9-10 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | 93 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 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 | |||
| 19767127 | 2011 | Peptide 6 | 11 | Acetylation | Amidation | Linear | L | None | Ciliary neurotrophic factor (CNTF) | Neurotrophic peptide | 0, 15, 30, 60 and 120 min | 5 μg | >6 | Rat blood proteases | LC/MS/MS | Sprague-Dawley Rat plasma | in vivo | None | None | Peptide 6 effectively inhibited the LIF-mediated signaling and ˆ¼50% inhibition of 10 pM LIF was achieved with 100 pM Peptide 6. | |||
| 17682073 | 2007 | NC100668 | 13 | Acetylation | Tc chelator (NC100194) | Linear | L | Tyr residue at 8 position is Iodionated | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Tracer tested for nuclear medical imaging | 1, 1.5, 3, 6, 12, and 24 hours | 20, 100, 500, 1000, and 2000 μg | 1.2 | Human plasma proteases | LC-MS | Injected in human plasma | in vivo | None | None | Not reported | |||
| 17682073 | 2007 | NC100668 | 13 | Acetylation | Tc chelator (NC100194) | Linear | L | Tyr residue at 8 position is Iodionated | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Tracer tested for nuclear medical imaging | 1, 1.5, 3, 6, 12, and 24 hours | 20, 100, 500, 1000, and 2000 μg | 10.5 (terminal elimination) | Human plasma proteases | LC-MS | Injected in human plasma | in vivo | None | None | Not reported | |||
| 17704241 | 2007 | FROPDOTA | 13 | Free | lys coupled to the chelator DOTA (DOTA is 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid) | Linear | L | 111In radiolabeling | Somatostatin receptor-binding octreotide | Tumor-Targeting Peptide | 1, 2, 5, 15, 30, 60, and 120 min | 200 μl | 71 | Human serum proteases | Radioimmunoassay and RP-HPLC | Human serum | in vitro | None | None | The inhibition constant was 494 nM. | |||
| 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 | 1μg/100g body wt | 90.6 (t1/2 terminal phase) | Rat serum proteases | Not mentioned | Vaginal 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 | 10μg/100g body wt | 109.8 (t1/2 terminal phase) | Rat serum proteases | Not mentioned | Vaginal 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 | |||
| 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 | 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 | 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- 6 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine, Orn = Ornithine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 76.2 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | 4286483 | None | Similar or higher activity in rat than in rabbit (rat = 0.4*10-6mg/50mg tissue and rabbit = 0.1*10-6mg/50mg tissue | |||
| 4327730 | 1971 | ACTH analogue- 7 | 18 | Free | Amidation | Linear | L | Ibu = α-aminoisobutyric acid | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 80.63 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | 4286483 | None | Similar or higher activity in rat than in rabbit (rat = 0.06*10-6mg/50mg tissue and rabbit = 0.5*10-6mg/50mg tissue | |||
| 4327730 | 1971 | ACTH analogue- 8 | 18 | Free | Amidation | Linear | Mix | βAla = Beta alanine, Orn = Ornithine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 88.12 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | 4286483 | None | Similar or higher activity in rat than in rabbit (rat = 0.07*10-6mg/50mg tissue and rabbit = 0.2*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) | |||
| 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 | 88.2 (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 = 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 | 122.88 (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 = 0.2*10-6mg/50mg tissue and rabbit = 0.002*10-6mg/50mg tissue) | |||
| 4327730 | 1971 | ACTH analogue- 6 | 18 | Free | Amidation | Linear | L | βAla = Beta alanine, Orn = Ornithine | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 102.62 (lipolytic activity t1/2) | Rat muscle proteases | Not mentioned | Rat muscle slices | in vitro | 4286483 | None | Similar or higher activity in rat than in rabbit (rat = 0.4*10-6mg/50mg tissue and rabbit = 0.1*10-6mg/50mg tissue | |||
| 4327730 | 1971 | ACTH analogue- 7 | 18 | Free | Amidation | Linear | L | Ibu = α-aminoisobutyric acid | Octadecapeptide analogues of ACTH | Steroidogenic peptides | 1,2,3 and 4 hours | Not mentioned | 261.78 (lipolytic activity t1/2) | Rat muscle proteases | Not mentioned | Rat muscle slices | in vitro | 4286483 | None | Similar or higher activity in rat than in rabbit (rat = 0.06*10-6mg/50mg tissue and rabbit = 0.5*10-6mg/50mg tissue | |||
| 16287259 | 2005 | H12 (Fibrinogen γ chain dodecapeptide) | 12 | Free | Free | Linear | L | conjugated with PEG | Derived from Fibrinogen gamma chain | Induce Thrombosis | Not mentioned | 40mg/kg peptide infused | 200 ±23 | Proteases from (thrombocytopenic rats)plasma | Spectrofluorometer | Rat(thrombocytopenic)plasma | in vivo | None | None | 10 mg/kg slightly reduced the Bleeding time to 573 ± 127 seconds in comparison control group 618 ± 51 seconds | |||
| 17408666 | 2007 | Cydiastatin 4-alpha | 13 | Free | Amidation | Linear | L | None | Synthetic | Neuropeptides | 30 °C for 20 minutes | 1nmol | 71 | M. sexta larval midgut tissue extract proteases | RP-HPLC | Midgut tissues 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 | 116 | M. sexta larval midgut tissue proteases | RP-HPLC | Midgut tissue | 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 | |||
| 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 | 64 ±1 | Mouse plasma proteases | RP-HPLC | Mouse Plasma | 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 | 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 | |||
| 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 | 167 ±9 | Mouse plasma proteases | RP-HPLC | Mouse Plasma | 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 | |||
| 17766836 | 2003 | Neurotensin (NT) | 13 | Free | Free | Linear | L | Pyr-Glu= pyro-glutamate | Neurotransmitter-like hypothalamic peptide | Regulates luteinizing hormone and prolactinrelease | 37 °C for 2-24 hours | Not mentioned | <2 | Human plasma proteases | HPLC-MS | Human plasma | in vivo | None | None | Tetra-branched NT(8-13)-methotrexate cause 60% reduction in tumor growth was observed with respect to mice treated with free drug | |||
| 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 | 68 ±15 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 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-2 (Oncocin) | 18 | Free | Free | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 120 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 64 μg/mL in E.coli BL21A1 and 128 μg/mL M.luteus | |||
| 21185160 | 2011 | O-4 (Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 120 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC =16μg/mL in E.coli BL21A1 and 64 μg/mL M.luteus | |||
| 21185160 | 2011 | O-5 (Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 90 ±1 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 16 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-6 (Oncocin) | 19 | Free | Amidation | Linear | L | Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 210 ±60 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-7 (Oncocin) | 19 | Free | Amidation | Linear | L | Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 98 ±6 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 8μg/mL M.luteus | |||
| 21185160 | 2011 | O-8 (Oncocin) | 19 | Free | Amidation | Linear | L | Nir=Nitro-arginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 78 ±2 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-9 (Oncocin) | 19 | Free | Amidation | Linear | L | Nmr =N-methylarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 79 ±3 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-10 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 94 ±1 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-11 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 19th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 160 ±5 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4μg/mL in E.coli BL21A1 | |||
| 21185160 | 2011 | O-12 (Oncocin) | 19 | Free | Propylamidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | >120 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-14 (Oncocin) | 19 | Free | Amidation | Linear | L | orn =Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 90 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-15 (Oncocin) | 19 | Free | Amidation | Linear | L | Beta-Hr =β-homoarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 150 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4μg/mL in E.coli BL21A1 and 16 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 | |||
| 21185160 | 2011 | O-18 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine, Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 62 ±4 | 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 | |||
| 21185160 | 2011 | O-19 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine, Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 111 ±6 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 2 μg/mL M.luteus | |||
| 21185160 | 2011 | O-20 (Oncocin) | 19 | Free | Amidation | Linear | L | Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 171 ±20 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC =8 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-21 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=homoarginine, Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 75 ±1 | 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 | |||
| 21185160 | 2011 | O-22 (Oncocin) | 19 | Free | Amidation | Linear | L | Agp = α-amino-3-guanidinopropionic acid, Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 103 ±5 | 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 | |||
| 21185160 | 2011 | O-23(Oncocin) | 19 | Free | Amidation | Linear | L | Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 176 ±8 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-24 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 19th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | >480(79.6 ±0.2%) | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 | |||
| 21185160 | 2011 | O-25 (Oncocin) | 19 | Free | Propylamidation | Linear | L | Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 102 ±2 | 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 | |||
| 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 | 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 | |||
| 25324697 | 2014 | SHSMP(Sadat-Habdan Mesenchymal stimulating Peptide) | 13 | Free | Free | Linear | L | None | SHSMP(Sadat-Habdan Mesenchymal stimulating Peptide) | Angiogenesis Factor | Blood sample collected after 30-480 minutes after the infusion of peptide | 5mg/kg | 90 | Rat plasma proteases | HPLC | Sprague Dawley rats (Dose i/m injected) | in vivo | Patent US7399826 B1 | None | Not reported | |||
| 25894376 | 2015 | P32 (Fibroblast growth factor 2- binding peptide derivative) | 11 | Free | Amidation | Linear | Mix | None | Fibroblast growth factor 2- binding peptide derivative | Anti-proliferative | 37 °C for 1-48hours | 0.3478μM | 12 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | P32 significantly inhibited the proliferation of SGC-7901, MGC-803, and KATOIII cells induced with 20ng/ml of FGF2, and the IC50 values of P32 were 0.77, 1.69, and 1.09 μmol/L, respectively | |||
| 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 | |||
| 26325323 | 2015 | Compound 1(lactose [Q1][w6]LHRH ) | 10 | Lactose | Amidation | Linear | L | Lactose at N-ter, pyro-Glutamine at n-ter, D-Trp at 6 pos | 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 | 2.9 ±0.63 | Rat plasma proteases | LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Increase in the level of LH was observed i.e. nAUC = 11.33 ± 1.65 ng/24 hafter oral administration of 20 mg/kg of compound 1 compared to the control nAUC = 4.45 ± 1.028 ng/24 h | |||
| 26325323 | 2015 | Compound 1(lactose [Q1][w6]LHRH ) | 10 | Lactose | Amidation | Linear | L | Lactose at N-ter, pyro-Glutamine at n-ter, D-Trp at 6 pos | Hypothalamus | Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH) | Blood sample collected after0.5-24 hours after the injection of peptide | 10mg/Kg | 2.6 ±0.84 | Rat plasma proteases | LC/MS | Rat Plasma (Dose i/p injected) | in vivo | None | None | Increase in the level of LH was observed i.e. nAUC = 11.33 ± 1.65 ng/24 hafter oral administration of 20 mg/kg of compound 1 compared to the control nAUC = 4.45 ± 1.028 ng/24 h | |||
| 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 | |||
| 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 | |||
| 16266798 | 2005 | Spantide II (Neurokinin-1 receptor (NK-1R) antagonist) | 11 | Nicotinoylation | Amidation | Linear | Mix | Pal=3-(2-Pyridyl)-L-alanine , k(Nic)=Nicotinoyl)Lys , Nle=NorLeucine, Dichloro at 5th Phenyl | Neurokinin-1 receptor (NK-1R) antagonist | Anti-inflammatory | Not mentioned | 5mg/ml | 95 days at pH 3 at 60 C | None | HPLC, LC-MS | Ethanol -water mixture | in vitro | None | None | Not reported | |||
| 1329046 | 1992 | Bombesin | 14 | Free | Amidation | Linear | L | Pyr=Pyro-glutamine | Autocrine peptide of SCLC cell line | Growth stimulator | 0-1080 minutes | 50μM | 417 | Degradative enzymes or SCLC cell line proteases | RP-HPLC | SCLC cell line NCI-H345 | in vitro | None | None | IC50= 1nM, Peptide were added at a 1 μM dose to inhibit growth of SCLC cell line | |||
| 1329046 | 1992 | [Psi13,14]BN [Bombesin antagonist] | 14 | Free | Amidation | Linear | L | Pyr=Pyro-glutamine | Bombesin analogue | Growth inhibitors | 0-1080 minutes | 50μM | 646 | Degradative enzymes or SCLC cell line proteases | RP-HPLC | SCLC cell line NCI-H345 | in vitro | None | None | IC50= 30nM, Peptide were added at a 1 μM dose to inhibit growth of SCLC cell line | |||
| 1346149 | 1992 | SS-14 (Somatostatin-14) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 140.1 ±36.5 (Metabolic half life) | Brodmann Area tissues proteases | Radioimmunoassay | Brodmann Area tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY) | in vitro | None | None | Not reported | |||
| 1346149 | 1992 | SS-14 (Somatostatin-14) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 129.8 ±53.2(Metabolic half life) | Hippucampul tissues proteases | Radioimmunoassay | Hippucampus tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY) | in vitro | None | None | Not reported | |||
| 1346149 | 1992 | SS-14 (Somatostatin-14) | 14 | Free | Free | Cyclic (C3-C14) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 79.8 ±11.1(Metabolic half life) | Hippucampul tissues proteases | Radioimmunoassay | Posterior Hippucampus tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY) | in vitro | 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 | |||
| 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 | |||
| 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 | >84 (beta t1/2) | Dog plasma proteases | HPLC | Two male Beagle dogs plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 2970910 | 1988 | Naferlin | 10 | Free | Amidation | Linear | L | pE=Pyro-glutamate, D-alanin= 3-(2Naphthyl)-D-alanine | GnRH (Gonadotropin releasing hormone) agonist | It decreases pituitary secretion of the gonadotropins | Not mentioned | 400 µg | 2.3 ±0.2 | Human serum proteases | Radioimmunoassay | Subcutaneous route of injection in human serum | in vivo | None | None | Not reported | |||
| 2970910 | 1988 | Naferlin | 10 | Free | Amidation | Linear | L | pE=Pyro-glutamate, D-alanin= 3-(2Naphthyl)-D-alanine | GnRH (Gonadotropin releasing hormone) agonist | It decreases pituitary secretion of the gonadotropins | Not mentioned | 304 ± 2.2 µg | 2.7 ±0.2 | Human serum proteases | Radioimmunoassay | Nasal route of injection in human serum | in vivo | None | 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 | 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 | 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 | 0.69 (t1/2 alpha) | Rat plasma proteases | Radioimmunoassay | (Dose i/m 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-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 | 0.83 | 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 | 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 | |||
| 2298867 | 1990 | Antide(Nal-Lys) | 10 | Acetylation | Amidation | Linear | Mix | None | Nal-Lys GnRH antagonist | Regulates or inhibits LH release or gonadotropins | Blood collected upto 30 days after peptide injection | 3.5mg/kg injected i/v | 6.5 | Proteases from OVX monkey serum | Radioactive assay | (Dose i/v injected)OVX monkey Serum | in vivo | None | None | Gonadotropin inhibition;Following sc or iv Antide injection, peripheral Luteinizing hormone (LH) levels declined from 281 + 19 ng/ml to 29 + 3 ng/ml within one day | |||
| 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 | |||
| 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 | DE-gamma-E (Des-enkephalin-gamma-endorphin) | 18 | Free | Free | Linear | L | None | Neuroleptic peptide | Neuroregulator | Not mentioned | Peptide 0.04 w/v in 154mM KCl + 0.25% w/v Na2EDTA co-administeration | 93 ±45 | 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 | 9.2 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (2.5%) | in vitro | 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 | 4 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (5%) | in vitro | 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 | 1.9 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (10%) | in vitro | 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 | |||
| 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 | 44.6 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (2.5%) + converting enzyme inhibitor (MK422) with conc 10-6 M | in vitro | 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 | 8.3 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (5%) + converting enzyme inhibitor (MK422) with conc 10-6 M | in vitro | 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 | 4 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum(10%) + converting enzyme inhibitor (MK422) with conc 10-6 M | in vitro | 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 | 1.2 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (20%) + converting enzyme inhibitor (MK422) with conc 10-6 M | in vitro | 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 | 12.6 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (5%) + heat inactvation | in vitro | 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 | 8.7 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (10%) + Heat inactivation | in vitro | 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 | 9.9 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum(10%) + converting enzyme inhibitor (MK422) with conc 10-6 M + heat inactivation | in vitro | None | None | Not mentioned | |||
| 8353526 | 1993 | TMOF (Trypsin modulatinf oostatic factor) | 10 | Free | Free | Linear | L | None | Hormone is secreted from the ovary of Mosquitoes | Inhibitor of trypsin and chymotrypsin biosynthesis | Not mentioned | 30ng/group | 1.6 | Proteases from A. aegypti blood | RP-HPLC | A. aegypti 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 2 (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 | 67 | 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 | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 4 (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 | 100 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 5 (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 | >500 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 6 (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 | 80 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 7 (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 | 192 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 8 (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 | 191 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 9 (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 | 93 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 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 | 8 (Elimination half life t1/2 alpha) | Rat blood proteases | HPLC | Rat blood | in vivo | None | 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 | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 11 | 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 | 1.15 ±0.17(t1/2β) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00178 | 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 | |||
| 23696181 | 2013 | Cx43MP (Connexin43 mimetic peptides) | 12 | Free | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 145.57 ±14.57 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00181 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 90% approx. after 48 hours | |||
| 23696181 | 2013 | C12-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | C12-Laa | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 301.34 ±18.93 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00182 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 85% approx. after 48 hours | |||
| 23696181 | 2013 | C12-C12-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | Two C12-Laa | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 353.39 ±13.63 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00183 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 80% approx. after 48 hours | |||
| 23696181 | 2013 | GlcNS-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | N-β-D-glucosamine succinamic acid(GlcNS) | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 318.04 ±75.13 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00184 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 85% approx. after 48 hours | |||
| 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 | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 1 mg | 17.9 ± 2.1 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 3 mg | 21.3 ± 6.2 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 10 mg | 26.1 ± 7.0 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 20 mg | 35.4 ± 9.6 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 40 mg | 45.0 ± 13 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides therapy for PV and Hemochromatosis | N.A. | 80 mg | 52.5 ± 17 | Human plasma protease | HPLC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides Therapy For Pv And Hemochromatosis | N.A. | 40 mg | 49.6 ± 18 | Human Plasma Protease | high-performance liquidchromatography–tandem mass spectrometry method | Human plasma after 2 once weekly repeated dose | In Vivo | None | None | N.A. | |||
| 38785334 | 2024 | Rusfertide (PTG-300) | 18 | IsoV = Isovaeryl at position 1 | Amidation | Cyclic(C7-C17 Disulfide Linkage) | L | Lys8 conjugation with palmitoyl-Glu(2)-OH | Synthetic | Provides Therapy For Pv And Hemochromatosis | N.A. | 40 mg | 36.1 ± 21 | Human Plasma Protease | high-performance liquidchromatography–tandem mass spectrometry method | Human plasma after 2 once weekly repeated dose | In Vivo | None | None | N.A. | |||
| 38613996 | 2024 | vCPP2319 | 20 | 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 | 280.40 ± 59.20 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | IC50 = 4.00±1.03 for TNBC MDA-MB-231 Monolayer | |||
| 38555444 | 2024 | Aβ11/T80@CSs-TGC | 12 | Free | Linked with Chol using PEG2k linker | Linear | L | None | Synthetic | Treating intracranial infections caused by multidrug resistant Acinetobacter Baumannii | Blood samples were collected at predetermined time points (0.25, 0.5, 1, 2, 4, 6, and 8 h), | 12.5 mg/kg | 1.26 ± 0.21 | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | Both free TGC and Aβ11/T80@CSs-TGC displayed potent antimicrobial activity with a minimum inhibitory concentration of 2 μg/mL | |||
| 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) | |||
| 37880318 | 2023 | L1 | 15 | Acetylation | Free | Linear | L | None | Derived from calcitermin | Antimicrobial | 37 °C | 0.0001 M | >2 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 40 ± 10 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 | L2 | 15 | Acetylation | Amidation | Linear | L | None | Derived from calcitermin | Antimicrobial | 37 °C | 0.0001 M | 68 | Human plasma protease | HPLC | Human plasma with 1 ml of ammonium acetate buffer (pH 7.4) | In Vitro | None | None | CFU = 211 ± 25 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 | 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) | |||
| 37835489 | 2023 | QQT*-IRDye800 | 12 | QQT* conjugated with IRDye800 at C terminus using linker | Free | Linear | L | None | Synthetic | Used for in vivo imaging to identify premalignant Colorectal Lesions | RP-HPLC was performed at 0, 0.5, 1, 2, 4, 8, and 24 h | 30 μM | 3.6 | APC mice serum protease | RP-HPLC | APC mice serum | In Vivo | None | None | Not mentioned | |||
| 37384895 | 2023 | CLA-coated PTX-SPIONs@HRH | 12 | Free | Free | Linear | L | None | Synthetic | Antiangiogenic (used for targeted delivery of Paclitaxel in non-small cell lung carcinoma) | Mice were euthanized over 24 h at t = 0.5, 1, 4, 8, and 24 h | 15.6 μg/mL | 17.1 | Mice Plasma Protease | HPLC | Mice plasma | In Vivo | None | None | The activity value for CLA-coated PTX-SPIONs@HRH at the maximal therapeutic concentration (100 μg/mL) resulted in 12.8% cell viability on A549 lung adenocarcinoma cells | |||
| 37384895 | 2023 | CLA-coated PTX-SPIONs@HRH | 12 | Free | Free | Linear | L | None | Synthetic | Antiangiogenic (used for targeted delivery of Paclitaxel in non-small cell lung carcinoma) | Mice were euthanized over 24 h at t = 0.5, 1, 4, 8, and 24 h | 15.6 μg/mL | 17.1 | Mice Plasma Protease | HPLC | Mice plasma | In Vivo | None | None | The activity value for CLA-coated PTX-SPIONs@HRH at the maximal therapeutic concentration (100 μg/mL) resulted in 12.8% cell viability on A549 lung adenocarcinoma cells | |||
| 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 | 164 | Human plasma protease | Triple Quadrupole Mass spectrometry | Human plasma | 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 | Timepoints of 0, 10, 20, 30, 60, and 120 min | 2 μM | 82.5 | SD rats plasma protease | Triple Quadrupole Mass spectrometry | SD rats 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 | 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 | 372 | Gastric fluid protease | Triple Quadrupole Mass spectrometry | Simulated Gastric Fluid (SGF) at pH = 1.3 | 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 | 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 | 120 minutes | 2 μM | >120 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 1.3 (acidic) | 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 | 120 minutes | 2 μM | >120 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 5.5 (slightly acidic) | 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 | 120 minutes | 2 μM | 433 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 7.4 (basic) | 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) | |||
| 36902021 | 2023 | PDC | 16 | Free | PEG4 spacer was designed and subsequently reacted with a cysteine at the carboxyl terminus then, the elongated thiol-modified homodimer peptide was conjugated with DOX | Linear | L | None | HER2-targeting peptide–DOX conjugate | Antitumor | The PDC was incubated with human plasma (final peptide concentration of 50 μM) for 0, 2, 4, 8, 12, 24, and 48 h | 50 μM | 24 | Human plasma protease | HPLC | Human plasma | In Vitro | None | None | The IC50 value for the PDC (Peptide-Drug Conjugate) is 140 nM. This value indicates that the PDC is more potent in killing HER2-positive SKBR-3 cells compared to free DOX, which has an IC50 of 410 nM | |||
| 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 | |||
| 36631971 | 2023 | Onc72 | 19 | Free | Amidation, Orn=Ornithine at position 19 | Linear | L | Orn=Ornithine at position 15 | Synthetic | Antimicrobial | Aliquots weretaken in triplicates after 0, 1, 2, 4, and 8 h for Onc72 and 0, 4, 8, and 24 hfor both prodrugs | 31.5 μmol/L | ≈80 | Cell lysate protease (Obtained From An E. Coli Bw25113 Culture) | RP-HPLC | E. coli BW25113 cell lysate | In Vitro | None | None | (Onc72 in 19% MHB2 medium) MIC = 12.5 μmol L−1 (29 mg L−1) on E.coli BW25113 | |||
| 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. | |||
| N.A. | 2023 | RTD-1 | 16 | Free | Free | Linear | L | None | Theta Defensin | Antimicrobial | Blood samples were collected at 0.25, 1, 2, 4, 8, and 24 H post-dose via terminal cardiac puncture | 5 mg/kg | 6.05 (Elimination Half Life) | Mouse plasma protease | LC-MS with reverse phase liquid chromatography | Mouse plasma | In Vivo | None | US 2022/0048569 W | Administering an effective amount of the effective 9-defensin or the effective 0-dcfcnsin analog to the individual in need of treatment, wherein the effective amount provides antimicrobial activity directed to the microbe | |||
| 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. | |||
| 36588717 | 2022 | [3H]BPC157 | 15 | Free | Free | Linear | L | all Proline radiolabelled with [3H] | Isolated from human gastric juice | Treatment of various wounds in rats and dogs | Whole blood and plasma samples of six JVC rats were collected at 0.05, 0.167, 0.5, 1, 2, 4, 8, 24, 48, and 72 h after administration (three males and three females at each time point) for the examination of radio pharmacokinetics of total plasma | 100 µg/300 μCi/kg | 102 ± 32 | JVC rats plasma protease | Liquid scintillation counter | JVC Rats 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) | |||
| 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 | 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 | 0.7 | 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. | |||
| 36142749 | 2022 | PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | opioid–neurotensin hybrid peptide | Analgesic | 37°C for 24 h | 50 μg/mL | 204.4 | N.A. | LC-MS | 1M HCl | In Vitro | None | None | Emax = 149.17% ± 2.9 for PK20 (intrinsic activity of the receptor) | |||
| 36142749 | 2022 | PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | opioid–neurotensin hybrid peptide | Analgesic | 37°C for 24 h | 50 μg/mL | 11.36 | N.A. | LC-MS | 1M NaOH | In Vitro | None | None | EC50 = 79 nM (potency at mu opioid receptor) | |||
| 36142749 | 2022 | [Ile9]PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | PK20 derivative | Analgesic | 37°C for 24 h | 50 μg/mL | 117.7 | N.A. | LC-MS | 1M HCl | In Vitro | None | None | Emax = 151.2% ± 74.5 for [Ile9]PK20 (intrinsic activity of the receptor) | |||
| 36142749 | 2022 | [Ile9]PK20 | 10 | Replacing tyrosine (Tyr) with 2,6-dimethyltyrosine (Dmt) at position 1 | Free | Linear | Mix | D-amino acid residue (D-Lys) inserted at position 2 | PK20 derivative | Analgesic | 37°C for 24 h | 50 μg/mL | 4.69 | N.A. | LC-MS | 1M NaOH | In Vitro | None | None | EC50 = 1244 nM (potency at mu opioid receptor) | |||
| 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) | |||
| 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. | 1.25 mg/kg | 1.7 | NHP plasma protease | LC-MS/MS | NHP plasma | In Vivo | None | None | KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP) | |||
| 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 | 24 hours | 2 µM | >57.8 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | KD(nM) = 2.5±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in human) | |||
| 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 | 24 hours | 2 µM | >57.8 | NHP plasma protease | LC-MS/MS | NHP plasma | In Vitro | None | None | KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP) | |||
| 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 | 24 hours | 2 µM | 60.7 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 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 | 24 hours | 2 µM | 2.3 - 4.4 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | 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 | 24 hours | 2 µM | 26.1 | Human blood Protease | LC-MS/MS | Human blood sample | In Vitro | None | None | KD(nM) = 2.5±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in human) | |||
| 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 | 24 hours | 2 µM | 28.3 | NHP blood protease | LC-MS/MS | NHP blood sample | In Vitro | None | None | KD(nM) = 6.3±1.3 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in NHP) | |||
| 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 | 24 hours | 2 µM | 8.5 | Rats blood protease | LC-MS/MS | Rats blood sample | In Vitro | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 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 | 24 hours | 2 µM | 5 | Mouse blood protease | LC-MS/MS | Mouse blood sample | In Vitro | None | None | KD(nM) = 2.9±1.1 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Mouse) | |||
| 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. | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 4.4 ± 0.3 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35653695 | 2022 | KLK7 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 6.2 ± 0.9 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK7)(nM) = 32, Kd(albumin)(nM) = 164 (for KLK7(1)-tag) | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 5.1 ± 0.7 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 5.8 ± 0.4 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35414877 | 2022 | B_1275.3 | 14 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 159 | |||
| 35414877 | 2022 | B_1275.5 | 14 | Acetylation | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 2300 | |||
| 35414877 | 2022 | B_1275.6 | 14 | C18 diacid-gGlu-2xOEG | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 860 | |||
| 35414877 | 2022 | B_1275.5 | 14 | Acetylation | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 2.367 (Elimination half life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 2300 | |||
| 35414877 | 2022 | B_1275.6 | 14 | C18 diacid-gGlu-2xOEG | Free | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 250 (Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 860 | |||
| 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 | |||
| 35359494 | 2022 | CSP1-E1A/F7Cha | 17 | Free | Free | Linear | L | introduction of Cha = cyclohexylalanine residues at position 7,E1A substituitions | CSP1 analog | 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 | 4 | Trypsin | RP-HPLC | PBS solution | In Vitro | None | None | IC50(nM) = 36 for CSP1-E1A/F7Cha against ComD1 receptor | |||
| 35359494 | 2022 | CSP1-E1A/F7Cha | 17 | Free | Free | Linear | L | introduction of Cha = cyclohexylalanine residues at position 7 | CSP1 analog | 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 | 4 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | IC50(nM) = 36 for CSP1-E1A/F7Cha against ComD1 receptor | |||
| 35359494 | 2022 | CSP1-F7Cha/I12Cha | 17 | Free | Free | Linear | L | introduction of Cha residues at positions 7 and 12 | CSP1 analog | 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 | 3 | Trypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 0.97 for CSP1-F7Cha/I12Cha against ComD1 receptor, EC50(nM) = 70 for CSP1-F7Cha/I12Cha against ComD2 receptor | |||
| 35359494 | 2022 | CSP1-F7Cha/I12Cha | 17 | Free | Free | Linear | L | introduction of Cha residues at positions 7 and 12 | CSP1 analog | 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 | 6 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 0.97 for CSP1-F7Cha/I12Cha against ComD1 receptor, EC50(nM) = 70 for CSP1-F7Cha/I12Cha against ComD2 receptor | |||
| 35053417 | 2022 | (WR)8WK(Glutaryl-Dox)βA] | 19 | Free | βAlanine at C terminal conjugation | Cyclic | L | An ester bond is utilized to attach Dox with a glutaryl linker | Synthetic | Treat Breast, Leukemia, and Lymphoma Malignancies | 4 h at 37 °C | 5 µM | ∼6 | Human Serum Protease | HPLC | 25% Human serum | In Vitro | None | None | At 10 μM: 65% reduction in cell viability after 72 hours for SK-OV-3 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 19% cell viability after 72 hours for MDA-MB-231 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 77% reduction in cell viability after 72 hours for MCF-7 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 64% reduction in cell viability after 24 hours for MES-SA/MX2 Cells (DOX-resistant) Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ) | |||
| 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 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 | |||
| 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 2, 6, 10, 15, 20, 40, 60, 90, 135, 180 min | 0.1 mg/kg | 82 ± 9 | Male göttingen minipigs plasma protease | LC-MS/MS | Male göttingen minipigs plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 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 5, 10, 20, 40, 60, 90, 120, 180, 240, 300 min | 0.25 mg/kg | 264 ± 80 | Male göttingen minipigs plasma protease | LC-MS/MS | Male göttingen minipigs 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 | 0.2 mg/kg | 69 ± 7 | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys 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 | 0.1 mg/kg | 65 ± 5 | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys 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. | |||
| 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 | P26 | 12 | N-Acetylated Arg2 | Free | Linear | Mix | D-Leu, D-ala = l and 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 | 86 | 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) = 2.11 ± 0.40 | |||
| 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 | |||
| 35177945 | 2022 | LIT01-196 | 17 | FC [CF3(CF2)7(CH2)2C(O)] conjugation at N terminal | Free | Linear | L | None | Apelin Analog | Diuretic and Cardiovascular effects | Incubated at 37°C for various times, from T0 to T4 h | 5 μM | 1440 | 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) = 0.08 ± 0.01 | |||
| 35177945 | 2022 | Apelin-13 | 13 | Free | Free | Linear | L | None | Secreted by White Adipose Tissue (Wat) in both humans and animals | Antidiabetes, Anorexic Effects | N.A. | N.A. | 2.1 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 7.4 x 10⁻⁹ M | |||
| 35177945 | 2022 | (Lys8GluPAL)apelin-13-amide | 13 | Free | Amidation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 1.2 x 10⁻¹⁰ M | |||
| 35177945 | 2022 | Lys8GluPAL(Tyr13)apelin-13 | 13 | Free | Tyr13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 1.1 x 10⁻⁹ M | |||
| 35177945 | 2022 | Lys8GluPAL(Val13)apelin-13 | 13 | Free | Val13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 2.2 x 10⁻¹⁰M | |||
| 35177945 | 2022 | pGlu(Lys8GluPAL)apelin-13-amide | 13 | pGlu = Pyroglutamate | Amidation | Linear | L | None | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | N.A. | N.A. | >24 | Mouse plasma protease | RP-HPLC | Mouse plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 3.1 x 10⁻¹⁰M | |||
| 35177945 | 2022 | Lys8GluPAL(Tyr13)apelin-13 | 13 | Free | Tyr13 modifcation, carboxylation | Linear | L | I125 radioactive labeled | Apelin-13 Analogue | Antidiabetes, Anorexic Effects | Blood (20 microliter) collected at 0, 15, 30, 45, 60, 90, 120, 240, 480, 960 and 1440 min after injection | 4.1 nmol/kg | 2.5 - 3 | NIH swiss mice plasma protease | RP-HPLC | NIH swiss mice plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50 = 1.1 x 10⁻⁹ M | |||
| 35177945 | 2022 | (Ala13)apelin-13 | 13 | Free | Ala13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 10.3 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.74e-009 (In vitro insulin secretion) | |||
| 35177945 | 2022 | (pGlu)apelin-13 | 13 | pGlu = Pyroglutamate | Amidation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 3.8 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.10e-008 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Ala13)apelin-13 | 13 | pGlu = Pyroglutamate | Ala13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic activity | 0, 2, 4, 8, 24 h | 20 μg | 11.1 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 7.68e-009 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Val13)apelin-13 | 13 | pGlu = Pyroglutamate | Val13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic Activity | 0, 2, 4, 8, 24 h | 20 microgram | 9.8 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.59e-008 (In vitro insulin secretion) | |||
| 35177945 | 2022 | pGlu(Tyr13)apelin-13 | 13 | pGlu = Pyroglutamate | Tyr13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic Activity | 0, 2, 4, 8, 24 h | 20 microgram | 12.2 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.48e-008 (In vitro insulin secretion) | |||
| 35036703 | 2021 | [64Cu]CM-1 | 13 | 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 1 hour | ∼100 μCi | 22.4 Of Intact [64Cu]Cm-1 Remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | CM1 shows high binding affinity for CD133 (KD = 7.37 nM), 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35036703 | 2021 | [64Cu]CM-1 | 13 | 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 2 hour | ∼100 μCi | 20.1% Of Intact [64Cu]Cm-1 Remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | CM1 shows high binding affinity for CD133 (KD = 7.37 nM), 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35036703 | 2021 | [64Cu]CM-2 | 14 | 6-aminohexanoic acid (Ahx) linker is anchored between the N terminus of the peptide and the (DOTA) 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid , 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 1 hour | ∼100 μCi | 94.9 of intact tracers remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35036703 | 2021 | [64Cu]CM-2 | 14 | 6-aminohexanoic acid (Ahx) linker is anchored between the N terminus of the peptide and the (DOTA) 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid , 64Cu labeling | Free | Linear | L | None | Synthetic | PET Radiotracer For Cd133 | 2 hour | ∼100 μCi | 91.9% of intact tracers remained | Mouse serum protease | radio-HPLC | mouse serum | In Vitro | None | None | 64Cu]CM-2 showed a binding affinity (IC50) of 44.95 nM, which is similar to that of [64Cu]CM-1 (IC50 = 52.55 nM) | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 2.35 mg/kg | 2.946 ± 2.048 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 4.7 mg/kg | 2.941 ± 1.399 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 9.4 mg/kg | 2.781 ± 1.021 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 35011324 | 2021 | AWRK6 | 18 | Free | Free | Linear | L | None | Based on the natural occurring peptide dybowskin-2CDYa | Antimicrobial | Blood samples were collected from orbital venous plexus at 0.083, 0.167, 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, 8, and 10 h | 4.7 mg/kg | 1.983 ± 0.583 | SPF-grade male SD rats plasma protease | LC-MS/MS | SPF-grade male SD rats plasma | In Vivo | None | None | N.A. | |||
| 34859381 | 2021 | M89b | 17 | pGlu = Pyroglutamate at position 1 | Free | Linear | L | None | galanin analog | Interacts With Different G Protein-Coupled Receptors | >23 hours | 10 µM | 40% Of M89B Had Been Degraded | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | EC50 ratios to Gal-(1-15)(n) = NA(3) (in GAL1R) (B-Arrestin), EC50 ratios to Gal-(1-15)(n) = NA(3) (in GAL1R) (Ca-efflux) | |||
| 34859381 | 2021 | GAL-(1–15) | 15 | Free | Free | Linear | L | None | isolated from the porcine intestine | Interacts With Different G Protein-Coupled Receptors | >30 minutes | 10 µM | 80% Of Gal-(1–15) Was Degraded | Rats serum protease | HPLC | Rats serum | In Vitro | None | None | EC50 ratios to Gal-(1-15)(n) = 1.7(3) (in GAL2R) (B-Arrestin), EC50 ratios to Gal-(1-15)(n) = 1.4(3) (in GAL2R) (Ca-efflux) | |||
| 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) | |||
| 34661390 | 2021 | Gd4-TESMA | 19 | Gd4 | Free | Linear | L | Mal links KKK and other peptide | Synthetic | For imaging Atherosclerotic Plaque vulnerability | 2 hours | 0.6 mM which is diluted in water at a final concentration of 0.06 mM when aliquoting | No Degradation | 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) | |||
| 34393794 | 2021 | LIT01-196 | 17 | Fluorocarbon chain (CF3(CF2)7(CH2)2C(O)) attached to the N-terminal part of K17F | Free | Linear | L | None | Apelin-17 Analog | Treatment of Hypertension | N.A. | 15 nmol/kg | 156 | Rats plasma protease | RIA | Rats plasma | In Vivo | Pubchem CID Apelin: 56841713 | None | IC50 = 0.56 ± 0.04 nmol/l for LIT01-196 | |||
| 34393794 | 2021 | K17F | 17 | Free | Free | Linear | L | None | Apelin-17 Analog | Treatment of Hypertension | N.A. | 250 nmol/kg | 50 | Rats plasma protease | RIA | Rats plasma | In Vivo | Pubchem CID Apelin: 56841713 | None | IC50: 0.11 ± 0.01 nmol/l for K17F | |||
| 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 | |||
| 34358122 | 2021 | AT1-HSA-MRN-NPs | 12 | Free | HSA linked through PEG4 | Linear | L | None | Synthetic | Treatment of Cardiovascular Disease | Blood was collected from the jugular vein at the following timepoints: 0, 5, 15, 30, 45, 60, 120, and 360 min | 50 μg/kg | 101.3 | Rats plasma protease | HPLC | Rats plasma | In Vivo | None | None | N.A. | |||
| 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. | |||
| 34163352 | 2021 | NOPT | 16 | OPT substituted with an N-methyl proline at position 1 | Free | Linear | L | None | Derived from OPT | Binds To Pser68-Plm | Aliquots of 50 μl were collected at different time points (0–48 h) | 300 μM | 14.9 | Human serum protease | Mass spectrometry | Human serum | In Vitro | None | None | N.A. | |||
| 34122400 | 2021 | CbTP | 18 | Free | TP5 conjugation | Linear | L | None | A hybrid peptide combining TP5 and fragments of CATH2 | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 353 ± 41.3 | Human serum protease | HPLC | Human serum | In Vitro | None | None | CbTP induced cytotoxicity in a dose-dependent manner, while even a high dose (80 µg/mL) of CbTP was nontoxic to RAW264.7 cells | |||
| 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. | |||
| 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. | 20 mg/kg | 8.69 ± 1.19 | 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. | |||
| 33940058 | 2021 | OPBP-1@TMC | 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. | 20 mg/kg | 14.55 ± 1.43 | 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. | |||
| 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 | |||
| 33129837 | 2021 | OM19r-8 | 19 | Free | Amidation | Linear | Mix | replacing L-Arg15,19 with D-Arg15,19 | Derived from the antibacterial peptide OM19R | Antibacterial | Aliquots were analyzed after 0, 20, 30, 40, 60, 80, 90, 100, 120, 150, 180, 210, 240, 175 and 270min | 31.5 μmol/L | 71.10 ± 3.43 | Wistar rats blood plasma protease | HPLC | Wistar rats blood plasma | In Vitro | 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 | Aliquots were analyzed after 0, 20, 30, 40, 60, 80, 90, 100, 120, 150, 180, 210, 240, 270, 300, 400, 600 and 1000min | 31.5 μmol/L | 242.44 ± 39.21 | Wistar rats blood plasma protease | HPLC | Wistar rats blood plasma | In Vitro | 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 | |||
| 33008433 | 2020 | Hypoxic-Ischemic Brain Damage Associated Peptide (HIBDAP) | 17 | Free | Free | Linear | L | None | derives from the 210st to 226st amino acids of HSP90AA1 | Involved In The Nod-Like Receptor (Nlr) Signaling Pathway | N.A. | N.A. | 3.5 | Mammalian reticulocytes protease | N.A. | Mammalian reticulocytes with OGD ( oxygen and glucose deprivation (OGD)) | 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 | |||
| 32858124 | 2020 | Cmpd# 6 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 | 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 | 2.31 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 2.31 ± 0.57 | |||
| 32858124 | 2020 | Cmpd# 10 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13 | 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 | 3.4 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6 | |||
| 32858124 | 2020 | Cmpd# 12 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C15 | 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 | 1.84 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.39 ± 0.73 | |||
| 32858124 | 2020 | Cmpd# 14 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17 | 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 | 2.18 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE =7.42 ± 0.9 | |||
| 32858124 | 2020 | Cmpd# 17 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 diacid | 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 | 2.32 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.10 ± 0.62 | |||
| 32858124 | 2020 | Cmpd# 23 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C18-diacid | 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 | 19.7 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 117 ± 23.3 | |||
| 32858124 | 2020 | Cmpd# 6 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 2.6 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 2.31 ± 0.57 | |||
| 32858124 | 2020 | Cmpd# 10 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C13 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 10.2 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 6.22 ± 1.6 | |||
| 32858124 | 2020 | Cmpd# 12 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C15 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 6.3 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.39 ± 0.73 | |||
| 32858124 | 2020 | Cmpd# 14 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C17 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 10.3 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE =7.42 ± 0.9 | |||
| 32858124 | 2020 | Cmpd# 17 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C6 diacid | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 4.1 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.10 ± 0.62 | |||
| 32858124 | 2020 | Cmpd# 23 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C18-diacid | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | > 24 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 117 ± 23.3 | |||
| 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. | |||
| 32781586 | 2020 | TAMRA-HPA3NT3-A2 | 15 | Free | Free | Linear | L | TAMRA labeled | HPA3NT3 analogue | Antimicrobial | Incubation times (0, 60, 120 min) at 37 °C | 128, 64, 32, 16, 8, 4, 2, 1, and 0.5 µM | Degradation occured initially after 10 min | Human serum protease | HPLC | Human serum | In Vitro | None | None | Hemolysis % =0.3 for 250 micromolar (Toxicity of HPA3NT3 analogue peptide against RBCs) | |||
| 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 | |||
| 32506501 | 2020 | des-Ac-a-MSH | 14 | Free | Amidation | Linear | L | None | Derived from POMC | Antiinflammatory, Antipyretic | 37 °C | 2 µM | 32.06 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human CSF | 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 | 1.44 | Human CSF protease | Glo-sensor transfected cell-based luminescence assay | Human CSF | In Vitro | None | None | EC50 (M) = 7.749E-10 for MC1R-g2-MSH | |||
| 32380198 | 2020 | Apelin-12 | 12 | Free | Free | Linear | L | None | Smallest fragment of a 77 amino acid prepropeptide | Cardioprotective Properties | N.A. | 2-3 mg/ml | 165 (Terminus Half Life) | Human blood plasma protease | 1H-NMR | Human blood plasma | In Vitro | None | None | peptide M showed a significantly more pronounced effect in improving LV systolic function in Dox-induced cardiomyopathy compared to apelin-12 at a dose of 50 μg/kg | |||
| 32301996 | 2020 | 89Zr-NFP | 13 | mPEG2000, 89Zr labeling | Cy5.5 labelling | Linear | L | None | Synthetic | Diffuse intrinsic pontine glioma treatment | Mice were euthanized after 4 and 21 days for organ collection | 20 μCi | 60.3 | Mice brain homogenize protease | Gamma counter | Mice brain homogenize | In Vivo | None | None | IC50 (nM) = 5.6 ± 0.4 for DM1 in SF8628 | |||
| 32235388 | 2020 | TxIB | 16 | Free | Free | Linear | L | None | α-conotoxin derived from the venom of the cone snail species Conus textile | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Stable | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | 42% inhibition of α6β2* nAChRs by TxIB | |||
| 32235388 | 2020 | cTxIB-4 | 20 | Linker | Free | Cyclic (C2-C8, C3-C16 Disulfide Bond And Linker-C16 Bond) | L | None | α-conotoxin TxIB analogue | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Slightly lower stability than TXIB | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | Inhibition of cTxIB-4 is 35% | |||
| 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 | |||
| 31926774 | 2020 | PEG5K-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 | 1.28 ± 0.64 | 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 | PEG5K-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 | 1.51 ± 0.127 | 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 | |||
| 31841696 | 2020 | P9 | 11 | Free | Amidation | Linear | L | None | Synthetic | Anticancer | 37 °C for 5, 10, 20, 25, 30, 45 min | N.A. | 19 | Human plasma protease | HPLC | Human plasma | In Vitro | https://sci-hub.se/10.1007/s13277-015-3435-x | None | IC50 of P48 for Hela229 = 0.6 nM | |||
| 31841696 | 2020 | P48 | 10 | Leucine reduction | Amidation | Linear | L | None | Generated with P9 degradation | Anticancer | 1, 2, 3, 4, 5, 10, 12 h. | N.A. | 4 | Human plasma protease | HPLC | Human plasma | In Vitro | https://sci-hub.se/10.1007/s13277-015-3435-x | None | IC50 of P48 for Hela229 = 0.6 nM | |||
| 31809037 | 2020 | ApoE-Ms-SF | 19 | Free | PEG-P(CL-DTC) | Linear | L | None | Synthetic | Targeted Delivery Of Sorafenib To Hepatocellular Carcinoma | At fixed time points, 75 μL of blood was taken from the ophthalmic vein into a heparinized tube | 6 mg SF equiv/kg | 6.8 (Elimination Half-Lives) | BALB/c mice plasma protease | HPLC | BALB/c mice plasma | In Vivo | None | None | IC50: 8.5 μg/mL for ApoE-MS-SF | |||
| 31786794 | 2020 | DR10601 | 15 | Free | IgG4 hinge-Fc fragment | Linear | L | None | Synthetic | Antiobesity, Antidiabetes | Blood samples were collected at 3, 8, 24, 36, 48, 72, 96, 120, 144 and 168 h after administration | 16.3 nmol/kg | 51.9 ± 12.2 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | (EC50) value of DR10601 for GCGR was 37.39±3.95 nmol/L | |||
| N.A. | 2020 | Ac-(06-34-18) (wildtype) | 12 | Acetylation | Free | Linear | L | None | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 2.3 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 1.7 | |||
| N.A. | 2020 | Ac-(06-34-18) (HomoArg5) | 12 | Acetylation | Free | Linear | L | HomoArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 10.7 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 64 | |||
| N.A. | 2020 | Ac-(06-34-18) ( 4GuanPhe5) | 12 | Acetylation | Free | Linear | L | 4GuanPhe6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | 2.8 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 21 | |||
| N.A. | 2020 | Ac-(06-34-18) (NMeArg5) | 12 | Acetylation | Free | Linear | L | NMeArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | >20 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 98 | |||
| N.A. | 2020 | Ac-(06-34-18) Aze3 (HomoArg5) | 12 | Acetylation | Free | Linear | L | Aze replaces Pro (P)at position 4 , HomoArg6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Aze3 (4GuanPhe5) | 12 | Acetylation | Free | Linear | L | Aze replaces Pro (P)at position 4 , 4GuanPhe6 replaces Arg (R) | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Aze3 (NMeArg5) | 12 | Acetylation | Free | Linear | L | Aze replaces Pro (P)at position 4, NMeArg replaces Arg (R) at position 6 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| 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 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 HomoArg5 | 12 | Acetylation | Free | Linear | L | HomoArg replaces Arg (R) at position 6,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 | 12.2 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 19.7 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 4GuanPhe5 | 12 | Acetylation | Free | Linear | L | 4GuanPhe replaces Arg (R) at position 6,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 | 5 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 2.5 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Tyr4 NMeArg5 | 12 | Acetylation | Free | Linear | L | NMeArg replaces Arg (R) at position 6,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 | >20 | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = 60.2 | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Aze3 Tyr4 HomoArg5 | 12 | Acetylation | Free | Linear | L | HomoArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr, Aze substituitons at position 4 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Aze3Tyr4 4GuanPhe5 | 12 | Acetylation | Free | Linear | L | 4GuanPhe replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr, Aze substituitions at position 4 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| N.A. | 2020 | Ac-(06-34-18) Phe2 Aze3Tyr4 NMeArg5 | 12 | Acetylation | Free | Linear | L | NMeArg replaces Arg (R) at position 6,Tryptophan (W) at position 3 is replaced with Phe, alanine (A) at position 5 is replaced with Tyr, Aze substituitions at position 4 | Synthetic | Targets plasma kallikrein | N.A. | 5 uM | N.A. | Rats plasma protease | Waters Xevo TQ-MS | Rats plasma | In Vitro | None | US 201214350192 A | IC50(nM)(rat kallikrein) = NA | |||
| 31840306 | 2020 | conjugate 1 b | 16 | 2A-Gossypol Conjugate Linked By Thiazolidine Imine Linkage | Free | Linear | L | None | Synthetic | Cancer‐cell‐specific drug delivery | After 10 hours | 0.1 mg | 52% Cleavage of the peptide | N.A. | HPLC | 50 μL of 6M Gn·HCl, 200 mM phosphate buffer at pH 7 | In Vitro | None | None | N.A. | |||
| 33270417 | 2020 | INGAP-P | 15 | Free | Free | Linear | L | None | Synthetic | N.A. | N.A. | N.A. | 55.9 (Deamidation Half Life) | N.A. | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 31843919 | 2019 | ZY4 | 17 | Free | Amidation | Cyclic (C2-C16 Disulfide Bond) | L | None | Cathelicidin-BF15 analogs | Antimicrobial | Blood samples were drawn retroorbitally under short-term anesthesia at different time points (1, 5, 10, 30, 60 min, and 2, 5, 10, 18, 24 h) | 8 mg/kg | 1.859 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | MIC (µM) = 1.9 for ZY4 in P. aeruginosa CICC21625 , MIC (µM) = 2 for ZY4 in B. subtilis , MIC (µM) = 2 for ZY4 in S. aureus , MIC (µM) = 2 for ZY4 in C. albicans | |||
| 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. | |||
| 31277465 | 2019 | Dox-peptide conjugate 13 | 14 | DOX | Free | Cyclic (Lys6-Glu14 bond) | L | C6 fatty acid linked between | Synthetic | Anticancer | An aliquot (40 µL) was removed at different time intervals, such as 4, 24, and 84 h | 0.25 mM | 10 | N.A. | RP-HPLC | PBS having pH values ranging from 6.5 to 7.4 | 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 | |||
| 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 | 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-Proline6,O=Ornithine8 | Synthetic | Cell penetrating peptide | 37°C | 2 mg/ml | 420 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 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. | |||
| 31181805 | 2019 | TxID | 15 | Free | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Cloned from Hainan native Conus textile | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | At 37 °C for 0, 1, 3, 6, 12, 24, and 48 h, respectively | 0.25 mM | Less Stable | Human serum protease | RP-UPLC | Human serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31181805 | 2019 | DSPE-PEG-TxID | 15 | DSPE-PEG | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Derived from TXID | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | At 37 °C for 0, 1, 3, 6, 12, 24, and 48 h, respectively | 0.25 mM | Stable | Human serum protease | RP-UPLC | Human serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31181805 | 2019 | DSPE-PEG-TxID | 15 | DSPE-PEG | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Derived from TXID | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | Investigations were made at 0, 30, 60, 90, 120, and 180 min (SIF) incubations | N.A. | Stable | Simulated intestinal fluid serum protease | N.A. | Simulated intestinal fluid serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31181805 | 2019 | TxID | 15 | Free | Amidation | Cyclic (C2-C8, C3-C15 Disulfide Linkage) | L | None | Cloned from Hainan native Conus textile | Treatment of Neuropathic Pain, Addiction And Small Cell Lung Cancer | Investigations were made at 0, 30, 60, 90, 120, and 180 min (SIF) incubations | N.A. | Less Stable | Simulated intestinal fluid serum protease | N.A. | Simulated intestinal fluid serum | In Vitro | None | None | DSPE-PEG-TxID was still effective in inhibiting the α3β4 receptor, relative to TxID with slower reversible recovery. | |||
| 31079216 | 2019 | NT | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Isolated from bovine hypothalamus | Dual function as a neurotransmitter/neuromodulator in the Central Nervous System (CNS) and as a hormone/cellular mediator in peripheral tissues, such as the gastrointestinal tract and adipose tissue | 24 h incubation at 37 °C | 160 μM | Lower Stability | Human plasma protease | UHPLC | Human plasma | In Vitro | PDB id: 2LNE | None | −LogIC50±SE = 9.54±0.42 in Neurotensin (1–13) for NTS1 receptor | |||
| 30986342 | 2019 | P-T4-Cy5.5 | 11 | PEGylation | Conjugated with Cy5.5 | Linear | L | Diethylaminopropyl isothiocyanate (DEAP) conjugation at Lys1 side chain | Synthetic | Antitumor | N.A. | N.A. | 2 | 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, 8 hr, and 24 hr | 0.28 mM | 4 | N.A. | HPLC | pH 7.2 buffer | In Vitro | None | None | EC50 (nM) = 1.15 for GBAP | |||
| 30973007 | 2019 | GBAP 12 | 11 | Free | Free | Linear | L | None | GBAP analogs | Antibacterial | Time points were taken at 0 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, and 24 hr | 0.28 mM | >20 | N.A. | HPLC | pH 7.2 buffer | 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, 8 hr, and 24 hr | 0.28 mM | Highly Stable | Chymotrypsin | HPLC | PBS buffer + chymotrypsin | In Vitro | None | None | EC50(nM) = 6.3 for GBAP-[N-MeF7] | |||
| 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] | |||
| 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 | |||
| 30814652 | 2019 | Adnectin C-PAS#1(200) | 20 | Free | PAS#1(200) | Linear | L | None | Adnectin C analogs | 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 | 226.2 | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | Kd(1/s) =2.476E − 5 | |||
| 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 | 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. | >30 | RHNEP | LC-MS | Apelin3 | In Vitro | None | None | EC50(nM) = 4.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin4 | 17 | Free | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RHNEP | LC-MS | Apelin4 | In Vitro | None | None | EC50(nM) = 568 ± 34 | |||
| 30690406 | 2019 | Apelin5 | 17 | Free | Free | Linear | L | R2=Me, Methylation at Gln5 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RHNEP | LC-MS | Apelin5 | In Vitro | None | None | EC50(nM) = 176 ± 21 | |||
| 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. | 1.5 | RHNEP | LC-MS | Apelin6 | In Vitro | None | None | EC50(nM) = 2.6 ± 0.8 | |||
| 30690406 | 2019 | Apelin7 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin7 | In Vitro | None | None | EC50(nM) = 6.3 ± 1.0 | |||
| 30690406 | 2019 | Apelin8 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin8 | In Vitro | None | None | EC50(nM) = 11.3 ± 2.1 | |||
| 30690406 | 2019 | Apelin9 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | >30 | RHNEP | LC-MS | Apelin9 | In Vitro | None | None | EC50(nM) = 2.5 ± 1.5 | |||
| 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 | Apelin4 | 17 | Free | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RhKLKB1 | LC-MS | Apelin4 | In Vitro | None | None | EC50(nM) = 568 ± 34 | |||
| 30690406 | 2019 | Apelin5 | 17 | Free | Free | Linear | L | R2=Me, Methylation at Glu5 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | RhKLKB1 | LC-MS | Apelin5 | In Vitro | None | None | EC50(nM) = 176 ± 21 | |||
| 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 | Apelin7 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 1.4 | RhKLKB1 | LC-MS | Apelin7 | In Vitro | None | None | EC50(nM) = 6.3 ± 1.0 | |||
| 30690406 | 2019 | Apelin8 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 2.1 | RhKLKB1 | LC-MS | Apelin8 | In Vitro | None | None | EC50(nM) = 11.3 ± 2.1 | |||
| 30690406 | 2019 | Apelin9 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 2.9 | RhKLKB1 | LC-MS | Apelin9 | In Vitro | None | None | EC50(nM) = 2.5 ± 1.5 | |||
| 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 | |||
| 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. | 1.2 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 4.9 ± 1.0 | |||
| 30690406 | 2019 | Apelin4 | 17 | Free | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 568 ± 34 | |||
| 30690406 | 2019 | Apelin5 | 17 | Free | Free | Linear | L | R2=Me, Methylation at Glu5 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | N.A. | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 176 ± 21 | |||
| 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. | 4.5 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 2.6 ± 0.8 | |||
| 30690406 | 2019 | Apelin7 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | None | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 18 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 6.3 ± 1.0 | |||
| 30690406 | 2019 | Apelin8 | 20 | R1 = PALM-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 20.5 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 11.3 ± 2.1 | |||
| 30690406 | 2019 | Apelin9 | 20 | R1 = PEG-Lys-Phe-Arg | Free | Linear | L | R2= Me, Methylation at Gln8 | Apelin analogs | Blood Pressure lowering agents | 37 C for up to 72 h | N.A. | 27 | hplasma protease | LC-MS | hplasma | In Vitro | None | None | EC50(nM) = 2.5 ± 1.5 | |||
| 30658804 | 2019 | ES2 | 11 | Free | FITC | Linear | L | None | derived from the C-terminus of endostatin | Antiangiogenic | Immediately, 0.5, 1, 2, 4, 6, 8, 12, 24, and 36 h after injection, blood was collected | 20 mg/kg | 18.04 ± 2.38 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Antitumor activity = 35.31% | |||
| 30658804 | 2019 | HTCOSC-ES2 | 11 | Chitooligosaccharide chloride | FITC | Linear | L | None | derived from the C-terminus of endostatin | Antiangiogenic | Immediately, 0.5, 1, 2, 4, 6, 8, 12, 24, and 36 h after injection, blood was collected | 80 mg/kg | 29.17 ± 3.91 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Antitumor activity = 68.21% | |||
| 30624060 | 2019 | Compound 19 | 10 | C18 fatty acid | Amidation | Linear | Mix | sTyr = Sulfated-Tyrosine, Nle = Nor-leucine, DMeAsp = N-methylated DAsp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 36 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.67 (In Vitro CCK-1R Potency) | |||
| 30606721 | 2019 | BCY-B5 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | 11.5 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-B3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Mouse plasma protease | Radio-HPLC | Mouse plasma | In Vitro | None | None | KD(nM) = 1.22 ± 0.40 | |||
| 30606721 | 2019 | BCY-C3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-C2. | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Mouse plasma protease | Radio-HPLC | Mouse plasma | In Vitro | None | None | KD(nM) = 0.5 ± 0.2 | |||
| 30606721 | 2019 | BCY-B5 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-B3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C8, C15) | L | None | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | Radio-HPLC | Human plasma | In Vitro | None | None | KD(nM) = 1.22 ± 0.40 | |||
| 30606721 | 2019 | BCY-C3 | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | LC-MS | Human plasma | In Vitro | None | None | N.A. | |||
| 30606721 | 2019 | BCY-C2. | 15 | Acetylation | Free | Cyclic (Cyclized With 1,3,5-Trismethylbenzene On C2, C9, C15) | Mix | (1Nal),(D-Ala) at position 3,(tBuGly) at Asp14 | Bicyclic peptide derivative | For imaging and targeting of proteins overexpressed by tumors | 37C up to 24 hours | 4 μmol/L | >48 | Human plasma protease | Radio-HPLC | Human plasma | In Vitro | None | None | KD(nM) = 0.5 ± 0.2 | |||
| 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. | |||
| 30605634 | 2019 | (Pyr)1-apelin-13 | 13 | pGlu = Pyroglutamate | Free | Linear | L | None | Apelin analogs | Hemodynamic Effects In Humans | N.A. | 50 mg/kg | 11 | 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. | 10 mg/kg | 3.6 | Dogs plasma protease | LC-MS/MS | Dogs 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. | 10 mg/kg | 11 | Dogs plasma protease | LC-MS/MS | Dogs plasma | In Vivo | None | None | N.A. | |||
| 30600870 | 2019 | cot-biPEPEDB-VEGF | 20 | Acetylation | Amidation | Cyclic (C5-C13 Disulfide Bond In pepVEGF) | Mix | Lys10 linked with (OEG-Cotinine-OEG-SSSPIQGSWTWENGKWTWKGIIRLEQ-NH2), D-alanine | Synthetic | Antitumor | N.A. | 200nM | 1.18 (Clearance Half Life) | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | tumor growth inhibition was not significantly different between cot-biPEPEDB-VEGF and PBS control groups, despite a trend toward greater inhibition in the cot-biPEPEDB-VEGF group | |||
| 30600066 | 2019 | GSHP-ES2 | 11 | FITC-GSHP | Free | Linear | L | None | Synthetic | Antitumour, Antiangiogenic | Blood samples were collected through the fundus venous plexus 0.5–72 h after administration | 20 mg/kg | 9.11 | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | When the concentration was 5, 25, 50, 75, 100 and 125 μg/ml, the inhibitory rate of GSHP-ES2 was 6.47%, 16.47%, 24.57%, 31.36%, 44.45%, and 67.26%, respectively | |||
| 31536939 | 2019 | ALL*labeled nanocarriers | 12 | Free | D-Α-Tocopherol Succinate Linked Via Peg | Linear | L | Peptides are attached via a GGGSK linker to the nanocarrier surface via a thioether-mediated conjugation | Synthetic | Anticancer (therapy of hepatocellular carcinoma) | 37 °C for 0, 1, 2, 6, 12, and 24 h | 30 μM | 22.7 ( Sorafenib Release Half Life) | Mouse serum protease | HPLC | Mouse serum | N.A. | None | None | IC50 = 3.6 μM show greater toxicity to Hep3B cells in vitro | |||
| 31536939 | 2019 | QLE* labeled nanocarriers | 12 | Free | D-Α-Tocopherol Succinate Linked Via Peg | Linear | L | Peptides are attached via a GGGSK linker to the nanocarrier surface via a thioether-mediated conjugation | Synthetic | Anticancer (therapy of hepatocellular carcinoma) | 37 °C for 0, 1, 2, 6, 12, and 24 h | 30 μM | 19.5 (Sorafenib Release Half Life) | Mouse serum protease | HPLC | Mouse serum | N.A. | None | None | IC50 = 6.0 μM show lesser toxicity to Hep3B cells in vitro | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N29G30 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 1100 ± 700(Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 14 | Free | Free | Linear | L | N111G112 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 18 ± 2 (Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 20 | Free | Free | Linear | L | N238G239 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N196A197 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 120 ± 10 (Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N360A361 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 630 ± 30 ( Deamidation Half Life) | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N29G30 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 500 ± 200 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 14 | Free | Free | Linear | L | N111G112 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 12 ± 5 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 20 | Free | Free | Linear | L | N238G239 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N196A197 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 50 ± 2 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N360A361 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 µM | 120 ± 4 (Deamidation Half Life) | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 17 | Free | Free | Linear | L | N216A217 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 17 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Trypsin | LC-MS | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 17 | Free | Free | Linear | L | N216A217 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 17 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | N.A. | Pepsin | LC-MS | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N23G24 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 980 ± 60 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 13 | Free | Free | Linear | L | N29G30 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 1300 ± 100 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 10 | Free | Free | Linear | L | N238G239 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 10,900 ± 400 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 14 | Free | Free | Linear | L | N196A197 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 19 | Free | Free | Linear | L | N360A361 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 15 | Free | Free | Linear | L | N216A217 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 270 ± 30 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 13 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 3800 ± 400 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Tryptic peptide | 19 | Free | Free | Linear | L | N278A279 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 35,000 ± 900 (Hx Half Life) | Trypsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | WT - MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N23G24 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 700 ± 60 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 13 | Free | Free | Linear | L | N29G30 | MBP analog | Model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 600 ± 20 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 10 | Free | Free | Linear | L | N238G239 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 7800 ± 100 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 14 | Free | Free | Linear | L | N196A197 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 19 | Free | Free | Linear | L | N360A361 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 15 | Free | Free | Linear | L | N216A217 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | <30 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 13 | Free | Free | Linear | L | N278A279 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 2600 ± 100 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30684538 | 2019 | Peptic peptide | 19 | Free | Free | Linear | L | N278A279 | MBP analog | model protein | Wild-type and mutant MBP samples were collected after 1, 3, 6, 9, and 12 and 1, 3, 5, 7, 9, and 12 calendar months,pH 7.0 at 23 ± 2C | 20 μM | 16,700 ± 20 (Hx Half Life) | Pepsin | Hydrogen Exchange Mass Spectrometry (HX-MS) | Mutant MBP | In Vitro | None | None | N.A. | |||
| 30555549 | 2018 | AuNp-DPA | 13 | Free | Au | Linear | L | None | Synthetic | Antitumor | N.A. | 2 mg/kg | 7.5 ± 0.8 | Mice blood protease | HPLC | Mice blood sample | In Vivo | None | None | AuNP-DPA inhibited tumor growth by 88% on day 13 compared to the control, even better than DOX (inhibition ratio of 64.3% in comparison with the control) | |||
| 30411073 | 2018 | sPIF | 15 | Free | Free | Linear | L | None | Human embryo‐derived peptide analogs | Treatment of Autoimmune Hepatitis | Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8 | 0.1 mg/kg | N.A. | Human serum protease | LC-MS | Human serum | In Vivo | None | None | N.A. | |||
| 30411073 | 2018 | sPIF | 15 | Free | Free | Linear | L | None | Human embryo‐derived peptide analogs | Treatment Of Autoimmune Hepatitis | Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8 | 0.5 mg/kg | 63 | Human serum protease | LC-MS | Human serum | In Vivo | None | None | N.A. | |||
| 30411073 | 2018 | sPIF | 15 | Free | Free | Linear | L | None | Human embryo‐derived peptide analogs | Treatment Of Autoimmune Hepatitis | Patients’ serum samples were collected and analyzed at five different time points: screening (day ‐28 to day 0), pre‐injection (day 0), and postinjection days 1, 2, and 8 | 1 mg/kg | 109 | Human serum protease | LC-MS | Human serum | In Vivo | None | None | N.A. | |||
| 30407790 | 2018 | GENP-Gem-Ola | 12 | C18-EEG | Amidation | Linear | L | None | Synthetic | Treat Pancreatic Cancer With Breast Cancer 2 (Brca2) Mutation | Blood samples were collected at 0.5, 1, 2, 3, 5, 8, 12, and 24 h postinjection | equivalent concentrations of Gem (5 mg/kg) and Ola (50 mg/kg) | 4 | Mice plasma protease | HPLC | Mice plasma | In Vivo | None | None | Tumors from the GENP-Gem-Ola group showed extensive apoptosis (51% c-caspase-3 positive) | |||
| 30226777 | 2018 | E1 | 18 | Free | Free | Linear | L | None | Derived from the E1 envelope protein of GBV-C | HIV-1 fusion inhibitor peptide | At different incubation times (30 min, 1, 2, 4, 8, and 24 h) | 1 mg/mL | 8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 30226777 | 2018 | E1-NP | 18 | Free | Free | Linear | L | None | Derived from the E1 envelope protein of GBV-C | HIV-1 fusion inhibitor peptide | At different incubation times (30 min, 1, 2, 4, 8, and 24 h) | 1 mg/mL | 24 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 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. | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment | 2.2 mg/kg | 14.1 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Mild Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment | 2.2 mg/kg | 15.9 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Moderate Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion. For subjects with renal impairment, additional samples were taken at 30, 36, and 48 h, and at 72 h for subjects with severe renal function impairment | 2.2 mg/kg | 24.1 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Severe Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion | 2.2 mg/kg | 7.7 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Healthy Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 29738954 | 2018 | γTatM4 | 12 | Acetylation | Amidation | Linear | L | None | Tat peptide analogue | Antibacterial and Anti-Tb | N.A. | 10 mM | 16 | Trypsin | RP-HPLC | Tris-EDTA buffer | In Vitro | None | None | MIC(micrmolar) = 1.12 ± 0.01 for E.coli | |||
| 29738954 | 2018 | CtrlTat | 11 | Acetylation | Amidation | Linear | L | None | Derived from the human immunodeficiency virus 1 (HIV-1) tat protein | Antibacterial and Anti-Tb | N.A. | 10 mM | 4 | Trypsin | RP-HPLC | Tris-EDTA buffer | In Vitro | None | None | MIC (micromolar) = 6.27 ± 0.05 for E.coli | |||
| 29721065 | 2018 | 64Cu-DOTA-F56-CM | 12 | 64Cu-DOTA | maleimidopropionic acid (MPA) at the C-terminal | Linear | L | None | Maleimidopropionic acid-conjugated peptide | Antiangiogenic | At 10, 30, 60, and 120 min | 7.4 mBq | 6.967 | SD rats blood protease | Radioactivity assay | SD rats blood | In Vivo | None | None | F56 and F56-CM reduced the angiogenesis of zebrafish embryos in a dose-dependent way | |||
| 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 | |||
| 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 | |||
| 29577579 | 2018 | Fc‐apelin‐13 fusion protein | 12 | Fc linked by (GGGS)3 linker at N terminus | Free | Linear | L | None | Fc‐apelin‐13 fusion protein | Antidiabetes and Anti‐Heart Failure Activities | About 10 μL of blood was collected at each time point of 0, 1, 2, 4, 8, 24, 32, 48, 56, and 72 hours after administration | 5 mg/kg | ~33 | Mice Plasma Protease | Western blotting | Mice plasma | In Vivo | None | None | EC50 values of the Fc‐apelin‐13 fusion protein= 12.0 ± 1.1 nM for cAMP suppression | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a 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 | 78 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 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 | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 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, | 10 mg/kg | N.A. | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 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) | The animals were sacrificed 15 min, 1 h, 4 h, 8 h, 24 h, 48, and 96 h after injection | 2 mg/mL | 39 ± 2 | Rabbit eye plasma protease | HPLC | Rabbit eye plasma | In Vivo | None | None | Ki Values (nM) = 3,400 ± 200 against PKal from Rabbit | |||
| 29517911 | 2018 | 4b | 17 | Acetylation | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C7, C14 By 1,3,5 Trismethylbenzene) | L | HArg, Aze substituitions | synthetic | Antidiabetes (Treatment of Diabetic Macular Edema) | The animals were sacrificed 15 min, 1 h, 4 h, 8 h, 24 h, 48, and 96 h after injection | 2 mg/mL | ~22 | Rabbit eye plasma protease | HPLC | Rabbit eye plasma | In Vivo | None | None | Ki Values (nM) = ∼2,650 against PKal from Rabbit | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Human vitreous protease | LC-MS/MS | Human vitreous | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 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) | 24 h at 37 °C | 0.16 mM | >24 | Human vitreous protease | LC-MS/MS | Human vitreous | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Human vitreous protease | LC-MS/MS | Human vitreous | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 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) | 24 h at 37 °C | 0.16 mM | >24 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | 1.5 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | >24 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 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) | 24 h at 37 °C | 0.16 mM | >24 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes (Treatment of Diabetic Macular Edema) | 24 h at 37 °C | 0.16 mM | 2.8 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29517911 | 2018 | 1b | 18 | Replaced the Nterminal Ala with an acetyl group | Cterminal extension following the C-terminal alanine composed of 3 sarcosines and 2 D-arginine residues | Bicyclic (Cyclized On C1, C8, C15 By 1,3,5 Trismethylbenzene) | Mix | None | 1a analogue | Antidiabetes | 24 h at 37 °C | 0.16 mM | >24 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 3.4 ± 1.1 against PKal from Rats | |||
| 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 | 24 h at 37 °C | 0.16 mM | >24 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 30 ± 9 against PKal from Rats | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes | 24 h at 37 °C | 0.16 mM | 7 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 29464007 | 2018 | 99mTc-F1A | 18 | 99mTc-HHEDEG | Free | Cyclic (C-C Disulfide Bond In C Terminal) | L | Interconnected through a diethylene glycol (DEG) spacer | Fibrin-specific natural peptide analogue | 99MTC-F4A is a high-avidity prototype probe for characterizing thrombus in Lvads | Serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 124.7 ± 41.3 (T1/2b Elimination Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | 99mTc-F4A probe was not displaced by F1A | |||
| 29464007 | 2018 | 99mTc-F1A | 18 | 99mTc-HHEDEG | Free | Cyclic (C-C Disulfide Bond In C Terminal) | L | Interconnected through a diethylene glycol (DEG) spacer | Fibrin-specific natural peptide analogue | 99MTC-F4A is a high-avidity prototype probe for characterizing thrombus in Lvads | Serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 174.2 ± 26.2 (T1/2b Elimination Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | Kd ~10.2 µM for 99mTc-F1A (bound to uniform fibrin clots in PBS) | |||
| 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 3 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Rx2-X6 Bond) | L | X= allylglycine, Rx=Na-ally-arginine, 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 | 2.2 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 4.5 ±1.4 for 3 | |||
| 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 | |||
| 29461833 | 2018 | Pyr analogue 5 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X3-X7 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 | 3.9 ± 0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 3 ±0.1 for 5 | |||
| 29461833 | 2018 | Pyr analogue 6 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Rx4-X8 Bond) | L | X= allylglycine, Rx=Na-ally-arginine, 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 | 7.7 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 9.1 ±1.4 for 6 | |||
| 29461833 | 2018 | Pyr analogue 7 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X4-X8 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 | 9.9 ± 1.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 489 ±186 for 7L | |||
| 29461833 | 2018 | Pyr analogue 8 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X5-X9 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 | 3.5 ± 0.8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 3.9 ±1.4 for 8L | |||
| 29461833 | 2018 | Pyr analogue 9 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Sx6-X10 Bond) | L | X= allylglycine, Sx=Na-allyl-serine, 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 | >24 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 41 ±4 for 9L | |||
| 29461833 | 2018 | Pyr analogue 10 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X6-X10 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 | 4.1 ±0.8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 194 ±70 for 10L | |||
| 29461833 | 2018 | Pyr analogue 11 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X7-X11 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 | 6.6 ±0.4 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 1.4 ±0.4 for 11 | |||
| 29461833 | 2018 | Pyr analogue 12 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X8-X12 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 | 4.6 ±0.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 14 ±7 for 12 | |||
| 29461833 | 2018 | Pyr analogue 13 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X9-X13 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 | 8.6 ±0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 1.1 ±0.1 for 13 | |||
| 29461833 | 2018 | Pyr analogue 14 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X10-X14 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 | 7.8 ±1.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 445 ±62 for 14L | |||
| 29461833 | 2018 | Pyr analogue 15 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X9-X13 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 | 6.8 ±1.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 0.15 ±0.01 for 15 | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | Day 1 (cycle 1 - 28days) | 6 mg/m2 | 2.3 | Human plasma protease | ELISA | Human plasma | In Vivo | https://www.lens.org/lens/patent/124-764-042-412-641/fulltext?l=en | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 12 mg/m2 | 2.1 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 24 mg/m2 | 3.2 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 48 mg/m2 | 4.9 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 96 mg/m2 | 6 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 6 mg/m2 | 2.8 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 12 mg/m2 | 2 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 24 mg/m2 | 3.7 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 48 mg/m2 | 4.6 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 96 mg/m2 | 8.5 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 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. | |||
| 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 | 0.8 | Mice serum protease | ELISA | Mice serum | In Vivo | 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 | 5 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | 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. | |||
| 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. | |||
| 28954201 | 2018 | RTD-1 | 18 | Free | Free | Cyclic | L | None | Derived from rhesus | Attenuates Endotoxin-Induced Acute Lung Injury | Received RTD-1 at 0, 0.2, 1,5, or 25 mg/kg 0.5 hour before LPS challenge | 5 or 25 mg/kg | 30 (Terminal Half Life) | Mice plasma protease | LC-MS | Mice plasma (LPS-challenged ) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3024902/ | None | IC50= 4.5 μg/ml | |||
| 29464007 | 2018 | 99mTc-F1A | 18 | 99MTC-HHEDEG-DEG | Free | Cyclic (C-C Disulfide Bond In C Terminal) | L | None | Fibrin-specific natural peptide analogue | 99mTc-F4A is a high-avidity prototype probe for characterizing thrombus in LVADs | serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 8.6 ± 1.9(T1/2A Distribution Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 29176766 | 2017 | M10 | 10 | Free | Free | Linear | L | None | Derived from the C-terminal part of the MET receptor tyrosine kinase | Antifibrotic | Plasma samples were collected by cardiac puncture in the presence of 0.01% of Na-Citrate at time intervals of 15 min, 30 min, 1h, 2h, 4h, 6h, 12 h, 24 h, and 48 h following injection | 1 mg/kg | 6.8 ± 0.7 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4789156/ | None | N.A. | |||
| 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 | |||
| 28575099 | 2017 | Api134 | 18 | Gu: N,N,N′,N′-tetramethylguanidine, O denotes L-ornithine | Amidation | Linear | L | Orn=Ornithine | Apidaecin analog | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Highly Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Api137 | 18 | Gu: N,N,N′,N′-tetramethylguanidine, O denotes L-ornithine | Free | Linear | L | Orn=Ornithine | Apidaecin analog | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Highly Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Onc112 | 19 | Free | Amidation | Linear | Mix | D-amino acid substituitons | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Highly Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Onc18 | 19 | Free | Amidation | Linear | L | None | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Medium Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Onc72 | 19 | Free | Amidation | Linear | L | L-ornithine (Orn) | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Medium Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | Api88 | 18 | Gu: N,N,N′,N′-tetramethylguanidine, O denotes L-ornithine | Amidation | Linear | L | Orn=Ornithine | Apidaecin analog | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Low Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28494253 | 2017 | Peptide 22 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | Free | Linear | L | X1=Asn at position 1, X2=Leu at position , X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 77% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 22 = 1.01 ± 0.21 | |||
| 28494253 | 2017 | Peptide 24 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | Amidation | Linear | L | X1=Asn, X2=Leu, X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 52% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 24 = 1.19 ± 0.30 | |||
| 28494253 | 2017 | Peptide 25 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | Free | Linear | Mix | X1=D-Asn, X2=Leu, X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 80% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 25 = 1.36 ± 0.42 | |||
| 28494253 | 2017 | Peptide 26 | 20 | 111In-DTPA = diethylenetriaminepentaacetic acid | X4 = D-Thr at C terminal | Linear | Mix | X1=D-Asn, X2=Leu, X3=Lys, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 77% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 26 = 1.19 ± 0.40 | |||
| 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. | |||
| 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. | |||
| 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. | |||
| 28138743 | 2017 | Indolicidin | 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 | 1.53 | Mouse plasma protease | LC-HRMS. | Mouse plasma | In Vitro | 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 | P26 | 12 | Acetylation | Pro(4-Br)Phe substituition | Linear | Mix | Aib, DLeu,ProNle, D-Ala | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 86 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 138 ± 30 | |||
| 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 | |||
| 27815337 | 2017 | LIT01-196 | 18 | CF3(CF2)7(CH2)2C(O) | Free | Linear | L | None | Apelin analogs | Diuretic and Cardiovascular Effects | 37°C | 5 μM | 1440 | Mouse plasma protease | LC-MS | Mouse plasma | In Vitro | None | None | Recruitment of b-arrestin2 by BRET, EC50 (nM) = 16 ± 5.6 | |||
| 28714475 | 2017 | PK128 | 15 | Free | Free | Bicyclic (C2-C8,C8-C14 Disulfide Bond In Pk128) | L | None | Synthetic | Inhibit plasma kallikrein | Probes were taken at different time points (5 min, 0.5, 1, 2, 4, 8, 24 and 48 h) at 37 C , diluted to 3 mM (urokinase inhibitor) or 0.75 mM (plasma kallikrein inhibitor) with assay buffer (10 mM TrisCl, pH 7.4, 150 mM NaCl, 10 mM MgCl2, 1 mM CaCl2, 0.01% v/v Tween-20, and 0.1% (w/v) casein) | 20 microM | 1.8 ± 0.3 (Activity Half Life) | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin for tagPK128 | |||
| 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 | Nle= Nor-leucine at position 11, Aib = 2-Aminoisobutyric acid 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 | 29 | Wistar rats plasma protease | ESI-MS | Wistar rats plasma | In Vitro | None | None | EC50(nM) = 21.6 ± 4.5 for compound 31 | |||
| 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 | ~4 | Porcine liver homogenate protease | HPLC using a fluorescence detector | Porcine liver homogenate | In Vitro | None | None | EC50(nM) = 21.6 ± 4.5 for compound 31 | |||
| 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 | |||
| 27337048 | 2016 | SFTI-a | 14 | Free | Free | Cyclic (C1-C9 Disulfide Bond) | L | None | Sunflower trypsin inhibitor derivative | Immunomodulatory inhibitors of the CD2:CD58 protein–protein interaction | 37 °C at various time points from 0 min to 24 h | 2 mg/ml | <=24 | Human serum protease | HPLC, MS | Human serum | In Vitro | None | None | Cell adhesion inhibition IC50 (µM) = 0.043 ± 0.025 in T cell OVCAR-3 | |||
| 27243004 | 2016 | Api793 | 20 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (WO)2 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 246 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/L) = 0.64 ± 0.05 in HEK293 | |||
| 27243004 | 2016 | Api795 | 20 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (IO)2 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 354 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) > 0.6 in HEK293 | |||
| 27157666 | 2016 | cMBP2-PEG-Stp/NIS Polyplex | 12 | Free | PEG-Stp = succinoyl-tetraethylene pentamine/NIS gene | Linear | L | 123I labeling | Synthetic | Antitumor | 48 hours after polyplex administration, mice received an intraperitoneal injection of 18.5 MBq 123I | 18.5 MBq 123I | 3 | Huh7 subcutaneous mice xenografts protease | Gamma counter | Huh7 subcutaneous mice xenografts | In Vivo | https://sci-hub.st/10.1016/j.nucmedbio.2009.01.005 | None | N.A. | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Bicarinalin displayed no cytotoxicity against human lymphocytes in concentrations ranging from 0.066 to 8.5 mol L−1 and its LC50 value was 67.8 mol L−1 | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 24.4, 5.8, 12.2, 8.7, 5.4 for E.coli, C.sakazakii, P.aeruginosa CIP 82118, P.aeruginosa [R]ATCC 15442, S.enterica respectively. | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 12.2, 3, 8.7, 0.45, 24.4 for E.hirae, S.aureus, MRSA, S.xylosus, B.subtilis respectively | |||
| 27058430 | 2016 | Bicarinalin | 20 | Free | Amidation | Linear | L | None | Ant venom peptide | Antimicrobial | 37 ◦C until 48 h | N.A. | 15 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | MIC [micromole/L] = 0.75, 17.3, 17.3, 97.5, 6.1 for A.niger, C.albicans, C.albicans[R], G.candidum, S.cerevisiae and MIC[micromole/L] = 1.5 for L.infantum | |||
| 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 | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 8 | 13 | R8( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | 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 | 24 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 2 | 13 | R2( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | 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 | >20 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 5 | 13 | R5( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | 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 | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 7 | 13 | R7( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | 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 | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26808199 | 2016 | PYY24–36-Leu31 conjugates 9 | 13 | R9( structure given in paper) at NH terminal | Amidation | Linear | L | Leu31 substituitions | 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 | >12 | SD rats plasma protease | LC–MS/MS | SD rats plasma | In Vitro | None | None | HSA binding correlated well with plasma stability | |||
| 26565554 | 2016 | NG29-TFacetate | 10 | SarLys = N-methyl glycine and Lysine | TFacetate = Trifluoroacetate addition at C terminal | Linear | Mix | D-Phenyalanine substituitions for L-Phenylanine and Arg9 removal from C terminal | BK analogue | Role in Neurological and Ischemic Cardiovascular diseases and brain cancer | N.A. | 75 mg/kg | 2.28 (Elimination Half Life) | Wistar Han rats plasma protease | LC-MS/MS | Wistar Han rats plasma | In Vivo | https://sci-hub.st/10.1139/y02-053 | None | IC50(nM) = 0.3 for SarLys[dPhe8]desArg9BK ( for hB1R ) | |||
| 26565554 | 2016 | NG29-acetate | 10 | SarLys = N-methyl glycine and Lysine | Acetate addition at C terminal | Linear | Mix | (f) D-Phenyalanine substituitions for L-Phenylanine (F) and Arg9 removal from C terminal | BK analogue | Role in Neurological and Ischemic Cardiovascular diseases and brain cancer | N.A. | 75 mg/kg | 2.38 (Elimination Half Life) | Wistar Han rats plasma protease | LC-MS/MS | Wistar Han rats plasma | In Vivo | None | None | IC50(nM) = 0.3 for SarLys[dPhe8]desArg9BK ( for hB1R ) | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 3 min, 5 min, 10 min, 15 min, 30 min, 1 h, 4 h, 1 d, 2 d, 7 d, 28 d | 3.3 mg/kg | 59 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 62 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 60 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 18 h, 1 d, 2 d, 3 d, 7 d, 28 d | 10 mg/kg | 58 (Terminal Half Life) | Mouse plasma protease | TLC | Mouse plasma | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 3 min, 5 min, 10 min, 15 min, 30 min, 1 h, 4 h, 1 d, 2 d, 7 d, 28 d | 3.3 mg/kg | 60 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 61 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 10 min, 20 min, 30 min, 1 h, 2 h, 4 h, 6 h, 1 d, 2 d, 7 d, 28 d | 10 mg/kg | 94 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 26381279 | 2016 | 3H-RD2 | 12 | 3H labelled | Amidation | Linear | D | All D-amino acid substituitions | D3 derivative | Therapeutically active against toxic Β-Amyloid oligomers | Time points: 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 18 h, 1 d, 2 d, 3 d, 7 d, 28 d | 10 mg/kg | 73 (Terminal Half Life) | Mouse brain homogenate protease | TLC | Mouse brain homogenate | In Vivo | DB id: DB09045 | None | Fraction unbound to AGP (fu) at a RD2 concentration of 0.23 μM: 12.3% | |||
| 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. | |||
| 136-103-666-814-603 | 2016 | bi-specific fusion protein | 19 | Free | Free | Linear | L | None | NA | non-immunogenic protein | NA | NA | between 2 hours and 24 hours, greater than 24 hours, or greater than one week | NA | ELISA | in vivo | https://www.lens.org/lens/patent/136-103-666-814-603 | US 9238080 B2 | N.A. |