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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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 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 | |||
| 15322125 | 2004 | Aβ(1 €“ 40) | 40 | Free | Free | Linear | L | None | Derivative of human A precursor protein APP770 | Neurodegenerative | 120 minutes | 2x107 cpm of 125I-Aβ42 peptide | 2.4 | Mouse plasma proteases | Radioactivity measured by scintillation counter | Intravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samples | in vivo | None | None | Neurodegeneration caused by oligomerization | |||
| 15322125 | 2004 | Aβ(1 €“ 42) | 42 | Free | Free | Linear | L | None | Derivative of human Aprecursor protein APP771 | Neurodegenerative | 121 minutes | 2x107 cpm of 125I-Aβ40 peptide | 2.8 | Mouse plasma proteases | Radioactivity measured by scintillation counter | Intravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samples | in vivo | None | None | Neurodegeneration caused by oligomerization | |||
| 15012592 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 1.25 mU of DPP IV | 5 ·8 | DPP IV | LC/MS equipped with a microbore C-18 HPLC | DPP IV | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 1.25 mU of DPP IV | >12 | DPP IV | LC/MS equipped with a microbore C-18 HPLC | DPP IV | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-pyroglutamyl-GLP-1 | 30 | PyroGlutamic acid at 1st position | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 1.25 mU of DPP IV | >12 | DPP IV | LC/MS equipped with a microbore C-18 HPLC | DPP IV | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 7.5 µl of human plasma | 6 ·2 | Human plasma proteases | LC/MS equipped with a microbore C-18 HPLC | Human plasma | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 7.5 µl of human plasma | >12 | Human plasma proteases | LC/MS equipped with a microbore C-18 HPLC | Human plasma | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | N-pyroglutamyl-GLP-1 | 30 | PyroGlutamic acid at 1st position | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 7.5 µl of human plasma | >12 | Human plasma proteases | LC/MS equipped with a microbore C-18 HPLC | Human plasma | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 25 nM/kg body weight | < 2 | Adult obese diabetic (ob /ob ) mice blood protease | LC/MS equipped with a microbore C-18 HPLC | Intraperitoneally administered to adult obese diabetic (ob /ob ) mice | in vivo | None | None | IC50 = 0 ·37 nM of binding to a receptor | |||
| 15012592 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 25 nM/kg body weight | Completely resistant to degradation | Adult obese diabetic (ob /ob ) mice blood protease | LC/MS equipped with a microbore C-18 HPLC | Intraperitoneally administered to adult obese diabetic (ob /ob ) mice | in vivo | None | None | IC50 = 32 ·9 of binding to a receptor | |||
| 15012592 | 2004 | N-pyroglutamyl-GLP-1 | 30 | PyroGlutamic acid at 1st position | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 25 nM/kg body weight | Completely resistant to degradation | Adult obese diabetic (ob /ob ) mice blood protease | LC/MS equipped with a microbore C-18 HPLC | Intraperitoneally administered to adult obese diabetic (ob /ob ) mice | in vivo | None | None | IC50 = 6 ·7 nM of binding to a receptor | |||
| 11553691 | 2001 | APP-C59 | 59 | Free | Free | Linear | L | None | Amyloid precursor protein derivative | Regulator of synapse formation | 2 hours | Not mentioned | ~5 | Fetal calf serum proteases | Pulse chase experiment | BHK cell line | in vitro | None | None | Not reported | |||
| 11553691 | 2001 | APP-C59 | 59 | Free | Free | Linear | L | None | Amyloid precursor protein derivative | Regulator of synapse formation | 2 hours | Not mentioned | ~5 | Fetal calf serum proteases | Pulse chase experiment | Primary cultures of neurons from PS1 knockout mice's 14 day embryos | in vitro | None | None | Not reported | |||
| 12039708 | 2002 | Glucagon-like peptide-1 (GLP-1) | 30 | Free | Amidation | Linear | L | None | Derived from proteolytic cleavage of proglucagon | Insulinotropic | Not reported | Not mentioned | 1.5 €“5 | Plasma proteases | Radioimmunoassay | Rat plasma | in vivo | 24199154 | None | GLP-1 normalizes blood glucose levels | |||
| 12859428 | 2003 | BNP-32 | 32 | Free | Free | Linear | L | None | Canine B-type natriuretic peptide | Diuretic, natriuretic, hypotensive and smooth muscle relaxant activities | Not reported | Not mentioned | 1.57 ± 0.14 | Dog plasma proteases | Radioimmunoassay | Injected intravenously into dogs | in vivo | None | None | 44.7 ±0.3% RBC during BNP-32 infusion | |||
| 12578830 | 2003 | iAβ5p | 5 | Free | Free | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | 100% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A1 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A4 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A5 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A7 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-B1 | 5 | Acetylation | Amidation | Linear | L | αMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C1 | 5 | Free | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 5 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C2 | 5 | Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 7 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C3 | 5 | (NMe)Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 6 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p | 5 | Free | Free | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 15 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | 100% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A1 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A4 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 5 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A5 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-A7 | 5 | Acetylation | Amidation | Linear | L | NMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-B1 | 5 | Acetylation | Amidation | Linear | L | αMe | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | >24 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C1 | 5 | Free | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | <1 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C2 | 5 | Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 41 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C3 | 5 | (NMe)Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 25 | Proteases in rat brain homogenate | RP-HPLC | Rat brain homogenate | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 15246869 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon-like peptide-1(7-36)amide | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 6.2 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=6.1 ±1.8nM | |||
| 15246869 | 2004 | (Abu8)GLP-1 | 30 | Free | Free | Linear | L | 2-aminobutyric acid (Abu) | Synthetic | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=4.7 ±1.3nM | |||
| 15246869 | 2004 | GIP | 42 | Free | Free | Linear | L | None | Gastrointestinal incretin hormone | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 6 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | 8446620 | None | cAMP EC50=21.8 ±1.5nM | |||
| 15246869 | 2004 | (Abu2)GIP | 42 | Free | Free | Linear | L | 2-aminobutyric acid (Abu) | Synthetic | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 7.1 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=36.8 ±1.6nM | |||
| 15246869 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon-like peptide-1(7-36)amide | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma proteases except DPP | Radioimmunoassay | Human plasma+DPA (DPA is DPP inhibitor) | in vitro | None | None | cAMP EC50=6.1 ±1.8nM | |||
| 15246869 | 2004 | GIP | 42 | Free | Free | Linear | L | None | Gastrointestinal incretin hormone | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma proteases except DPP | Radioimmunoassay | Human plasma+DPA (DPA is DPP inhibitor) | in vitro | 8446620 | None | cAMP EC50=21.8 ±1.5nM | |||
| 15487959 | 2004 | Melagatran | 1 | N.A. | N.A. | Linear | L | N.A. | Synthetic | Anticoagulant | Not reported | 10-10 €“10-5 M | 4 | Human plasma protease | Not mentioned | Human plasma | in vivo | None | None | Not reported | |||
| 14759771 | 2004 | Glucagon-like peptide-1(7-36)amide | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide-1 | Regulate blood glucose | 12 hours | 2 mM | 4.4 | Purified DPP IV | ESI-MS | Purified DPP IV | in vitro | None | None | 0 ±0% insulin intensity in ARIP cells | |||
| 14759771 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Amidation | Linear | L | None | Derivative of glucagon-like peptide-1 | Regulate blood glucose | 12 hours | 2 mM | >12 | Purified DPP IV | ESI-MS | Purified DPP IV | in vitro | None | None | 12 ±0.4% insulin intensity in ARIP cells | |||
| 14759771 | 2004 | Glucagon-like peptide-1(7-36)amide | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide-1 | Regulate blood glucose | 12 hours | 2 mM | 4.7 | Serum proteases | ESI-MS | Serum | in vitro | None | None | 0 ±0% glucokinase intensity in ARIP cells | |||
| 14759771 | 2004 | N-acetyl-GLP-1 | 30 | Acetylation | Amidation | Linear | L | None | Derivative of glucagon-like peptide-1 | Regulate blood glucose | 12 hours | 2 mM | >12 | Serum proteases | ESI-MS | Serum | in vitro | None | None | 16 ±0.1% glucokinase intensity in ARIP cells | |||
| 14980787 | 2004 | Leucyl-tryptophane | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 7.4 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=15 µM | |||
| 14980787 | 2004 | Seryl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 5.2 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=41 µM | |||
| 14980787 | 2004 | Valyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 15 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=11 µM | |||
| 14980787 | 2004 | Leucyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 4.3 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=44 µM | |||
| 14980787 | 2004 | Alanyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 9.4 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=40 µM | |||
| 14980787 | 2004 | Tyrosyl-tyrosine | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 16 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=9 µM | |||
| 14980787 | 2004 | Alanyl-aspartate | 2 | Free | Free | Linear | L | None | Synthetic | Angiotensin Coverting Enzyme inhibitor | Not mentioned | Not mentioned | 64 | Rat plasma proteases | Spectrophotometry | Rat plasma | in vitro | None | None | IC50=>1600 µM | |||
| 12047915 | 2002 | LY315902 | 35 | 2-indolyl-propionyl | Free | Linear | L | Oct-octanoic moiety | Glucagon-like peptide-1 analogue | Insulinotropic and glucagonostatic | Not mentioned | Not mentioned | 1.1 | Canine plasma protease | Radioimmunoassay | Canine plasma after subcutaneous injection of 100 µg/kg | in vivo | 9232514 | None | Plasma insulin 255 pmol/l on intravenous infusion of 20 pmol/kg/min of LY315902 | |||
| 14499707 | 2003 | GRF1-29 | 29 | Free | Amidation | Linear | L | None | Growth hormone-releasing hormone (GRF) analogue | Stimulates release of growth hormone | Not mentioned | Not mentioned | 10 to 20 | Human plasma proteases | Not mentioned | Human plasma | in vivo | None | None | EC50=0.18nM | |||
| 14499707 | 2003 | GRF-1PEGLys12 | 29 | Free | Amidation | Linear | L | PEGylation on Lys12 | Growth hormone-releasing hormone (GRF) analogue | Stimulates release of growth hormone | 24 hours | Not mentioned | 10 | Human plasma proteases | Reporter gene assay | Human plasma | in vitro | None | None | Not reported | |||
| 14499707 | 2003 | GRF-1PEG5000 | 29 | Free | Amidation | Linear | L | PEGylation | Growth hormone-releasing hormone (GRF) analogue | Stimulates release of growth hormone | 25 hours | Not mentioned | 3.6 | Human plasma proteases | Reporter gene assay | Human plasma | in vitro | None | None | EC50=1.06nM | |||
| 14499707 | 2003 | GRF-1PEGLys21 | 29 | Free | Amidation | Linear | L | PEGylation on Lys21 | Growth hormone-releasing hormone (GRF) analogue | Stimulates release of growth hormone | 26 hours | Not mentioned | 4 | Human plasma proteases | Reporter gene assay | Human plasma | in vitro | None | None | Not reported | |||
| 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 | |||
| 10544005 | 2001 | PVP6,000 -YIGSR | 5 | Addition of Polyvinyl pyrrolidone(PVP6,000) | Free | Linear | L | None | Core sequence located at the β-1 chain of laminin | Antimetastatic effect. | Not reported | Not mentioned | 14.5 | Blood protease | Radioactivity measured with a gamma counter | Intravenous injection of labelled peptide in C57BL/6 mice | in vivo | None | None | At 0.015μmol reduced number of colonies of B16-BL6 melanoma cells in lung by 70% approx. | |||
| 15769092 | 2005 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 10 µg/kg | 9.09 | Rat blood proteases | ELISA | Rat blood plasma (Subcutaneous Injection) | in vivo | None | None | 100nmol/L GLP-1 enhanced insulin release by 3.4 ±0.7-fold per islet in presence of 16.8mmol/L glucose | |||
| 15769092 | 2005 | PEG2k-Lys-GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at Lysine | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 10 µg/kg | 21.67 | Rat blood proteases | ELISA | Rat blood plasma (Subcutaneous Injection) | in vivo | None | None | 100nmol/L GLP-1 stimulated insulin release of 306.6 ±72.8 pmol/L per islet in presence of 16.8mmol/L glucose | |||
| 15769092 | 2005 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 1 µg/kg | 2.61 | Rat blood proteases | ELISA | Rat blood plasma (Intravenous injection) | in vivo | None | None | 100nmol/L GLP-1 enhanced insulin release by 3.4 ±0.7-fold per islet in presence of 16.8mmol/L glucose | |||
| 15769092 | 2005 | PEG2k-Lys-GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at Lysine | Proglucagon molecule | Glucose-dependent insulinotropic effect | Not reported | 1 µg/kg | 33.36 | Rat blood proteases | ELISA | Rat blood plasma (Intravenous injection) | in vivo | None | None | 100nmol/L GLP-1 stimulated insulin release of 306.6 ±72.8 pmol/L per islet in presence of 16.8mmol/L glucose | |||
| 15882144 | 2005 | Ucn1 (urocortin 1) | 40 | Free | Free | Linear | L | None | Urocortin 1 | Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetite | Not reported | 50 μg | 54 ±3 | Human blood proteases | Not mentioned | Human blood plasma(Male patients with stable congestive heart failure) (Intravenous injection) | in vivo | None | None | Not given | |||
| 15882144 | 2005 | Ucn1 (urocortin 1) | 40 | Free | Free | Linear | L | None | Urocortin 1 | Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetite | Not reported | 50 μg | 52 ±3 | Human blood proteases | Not mentioned | Human blood plasma (Normal humans) (Intravenous) | in vivo | None | None | Not given | |||
| 16099941 | 2005 | proADM 45 €“92 (Adrenomedullin) | 48 | Free | Free | Linear | L | None | Synthetically synthesised proADM 45 €“92 | Vasodilatory peptide | Not reported | 0.29nmol/L | 22 | Human blood proteases | Sandwich immunoluminometric Assay | Human blood plasma | in vitro | None | None | Not given | |||
| 16467916 | 2005 | RGD | 9 | Acetylation | Amidation | Linear | L | Pen=Penicillamine, Methylation at Tyrosine, Tic=tetrahydroisoquinoline carboxylic acid | Human Glioma cells | Integrin Protein | Not reported | Not mentioned | ~20 | Proteases present in rat brain homogenates suspended in aCSF | RP-HPLC | Rat brain homogenates suspended in aCSF | in vitro | None | None | No activity found | |||
| 11962721 | 2001 | CTR-S domain | 124 | Free | Free | Linear | L | None | CTR (Calreticulin) | It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathway | Not reported | Not mentioned | 1.21 ± 0.34 in distribution phase | Serine Proteases | Radioactivity measured with a gamma counter | Rat plasma | in vivo | None | None | Biological activity =2 m Ci/nmol | |||
| 11962721 | 2001 | CTR-S domain | 124 | Free | Free | Linear | L | None | CTR (Calreticulin) | It binds to C1q, prevents the formation of C1 and so inhibits activation of the classical pathway | Not reported | Not mentioned | 40.5 ± 2.7 in elimination phase | Serine Proteases | Radioactivity measured with a gamma counter | Rat plasma | in vivo | None | None | Biological activity =2 m Ci/nmol | |||
| 11976797 | 2002 | GLP-1 | 30 | Free | Amidation | Linear | L | Radiolabelling of GLP-1by [123I] | Proglucagon molecule | Antidiabetic | Not reported | 10 MBq of the radiolabelled peptides | 7.0 ±2.1 for É‘ phase | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 11976797 | 2002 | GLP-1 | 30 | Free | Amidation | Linear | L | Radiolabelling of GLP-1by [123I] | Proglucagon molecule | Antidiabetic | Not reported | 10 MBq of the radiolabelled peptides | 110 ±13 for β phase | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 11976797 | 2002 | Exendin 3 | 39 | Free | Free | Linear | L | Radiolabelling of exendin 3 at position 1 (histidine) | Heloderma horridum venom | GLP-1 agonist | Not reported | 10 MBq of the radiolabelled peptides | 13 ±3.2 | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 11976797 | 2002 | Exendin 3 | 39 | Free | Free | Linear | L | Radiolabelling of exendin 3 at position 1 (histidine) | Heloderma horridum venom | GLP-1 agonist | Not reported | 10 MBq of the radiolabelled peptides | 108 ±16 | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 15587934 | 2004 | Human BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 3.1 | Not mentioned | EIA | Mice plasma (Intravenous injection) | in vivo | None | None | EC50 =0.46 ± 1.1 nM | |||
| 15587934 | 2004 | AlbuBNP | 32 | Human serum albumin | Free | Linear | L | None | B-type cardiac natriuretic peptides fused to HAS at N-terminal | Vasodilator | Not reported | 2.19 mg/kg | 11.2 | Mouse blood proteases | EIA | Mice plasma (Intravenous injection) | in vivo | None | None | EC50 =28.4 ± 1.2 nM | |||
| 15587934 | 2004 | AlbuBNP | 32 | Human serum albumin | Free | Linear | L | None | B-type cardiac natriuretic peptides fused to HAS at N-terminal | Vasodilator | Not reported | 2.19 mg/kg | 19.3 | Mouse blood proteases | EIA | Mice plasma (Subcutaneous injection) | in vivo | None | None | EC50 =28.4 ± 1.2 nM | |||
| 16023182 | 2005 | Ã…6 | 8 | Acetylation | Amidation | Linear | L | None | Urokinase plasminogen activator (uPA) | Anti tumor | Not reported | 100mg/ml | 2 | Serine Proteases | HPLC, MS-MS | Human blood plasma | in vitro | None | None | Not available | |||
| N.A. | 2004 | Melan-A27-35 | 9 | Free | Free | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 5 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 4 nM | |||
| N.A. | 2004 | Melan-A26-35 | 10 | Free | Free | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 45 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.25 nM | |||
| N.A. | 2004 | Melan-A26-35 A27L | 10 | Free | Free | Linear | L | None | Melan peptide which binds to HLA | Immunogenic and HLA binding peptides | N.A. | 25 nM | 40 | Human serum proteases | HPLC-ESI-MS | Serum (human) | in vitro | None | EP1395276A1 | EC50= 0.01 nM | |||
| N.A. | 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 | |||
| 20503261 | 2001 | Val8-GLP-1-Fc | 31 | Free | Addition of Fc | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 5.6 nM/ Kg | 45 | Monkey blood proteases | Radioimmunoassay | Monkey plasma (Intravenous) | in vivo | None | EP1355942B1 | Activation of GLP1 receptor (with respect to Val8-GLP-1(7-37)OH) 1.00% | |||
| 20503261 | 2001 | Val8-GLP-1-Human serum albumin (HSA) | 31 | Free | Human serum albumin | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 5.6 nM/ Kg | 87 | Monkey blood proteases | Radioimmunoassay | Monkey plasma (Intravenous) | in vivo | None | EP1355942B1 | Not mentioned | |||
| 20503261 | 2001 | Gly8-Glu22-GLP-1-CEx-Linker-IgG1 | 31 | Free | Linking IgG1 using CEx-Linker (SSGAPPPS-GGGGSGGGGSGGGGS) | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 55 | Dog blood proteases | Radioimmunoassay | Dog plasma (Intravenous) | in vivo | None | EP1355942B1 | Activation of GLP1 receptor (with respect to Val8-GLP-1(7-37)OH) 150.00% | |||
| 20503261 | 2001 | Gly8-Glu22-GLP-1-CEx-Linker-IgG1 | 31 | Free | Linking IgG1 using CEx-Linker (SSGAPPPS-GGGGSGGGGSGGGGS) | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 38 | Not mentioned | Radioimmunoassay | Dog plasma (Subcutaneous) | in vivo | None | EP1355942B1 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 1.2 mg/ Kg | 2.02 | Not mentioned | HPLC | Rat plasma (Subcutaneous) | in vivo | None | US6656906 | Fold fusion-inhibition (CEM cells and Molt-4 cells) with respect to T20 (DP-178) against HIV2-NIH-Z strain 840 Fold | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 1.5 mg/ Kg | 2.46 | Rat blood proteases | HPLC | Rat plasma (Intravenous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.8 mg/ kg | 4.83 | Not mentioned | HPLC | Monkey plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.8 mg/ kg | 5.57 | Not mentioned | HPLC | Monkey plasma (Intramuscular) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.8 mg/ kg | 5.35 | Monkey blood proteases | HPLC | Primate plasma (Intravenous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 15 mg/ Kg | 2 | Not mentioned | HPLC | Rat plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 5 mg/ Kg | 1.86 | Rat blood proteases | HPLC | Rat plasma (Intravenous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.4 mg/ kg | 6.23 | Monkey blood proteases | HPLC | Monkey plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 1.6 mg/ kg | 5.55 | Monkey blood proteases | HPLC | Monkey plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| 15369394 | 2004 | PEG40-FMS-IFNα2 | 146 | Pegylation [40kdaPEG linked to INFα2 via 2-sulfo-9-fluorenylmethoxycarbonyl (FMS)] | Free | Cyclic(C1-C98, C29-138) | L | None | IFNα2 derivative | Antiviral and antiproliferative | 0-150 hours | 10 µg | 65 (t1/2 of rate of regeneration of native interferon) | Rat blood proteases | BIAcore binding assay | Intravenously administered to wistar rats | in vivo | http://www.drugbank.ca/drugs/DB00105 | None | Following subcutaneous administration to rats and monitoring circulating antiviral activity, active IFNα2 levels peaked at 50 h, with substantial levels still being detected 200 h after administration. | |||
| 15369394 | 2004 | Interferon α2 (IFNα2) | 146 | Free | Free | Cyclic(C1-C98, C29-138) | L | Glycosylation at Thr-105 | IFNα2 | Antiviral and antiproliferative | 0-25 hours | 10 μg/rat in 0.2 mL of PBS | ~1 | Rat blood proteases | BIAcore binding assay | Intravenously administered to wistar rats | in vivo | http://www.uniprot.org/uniprot/P01563 | None | Following administration of IFNα2 (100 μg/rat), the circulating antiviral activity declined with a t1/2 value of ˆ¼1 h, reaching a level lower than 20 pM IFNα2, 12 h after administration. | |||
| 730072 | 2001 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | None | Porcine VIP | Antiinflammatory and vasodilatory | 0 5, 1, 2,3, 4, 5, 6, 7, 8, 9, 10, 12, 15, 20, and 30 minutes | 0.6, 1.3, and 3.3 pmol/kg/min infused over 30 minutes | ~1 | Human blood proteases | Radioimmunoassay | Intravenous infusion to humans | in vivo | http://www.uniprot.org/uniprot/P01282 | None | Infusion of the highest dose of VIP, plasma concentrations of glucose were significantly raised from a basal level of 5.05 ± 0.29 to 5.61 ± 0.27mmol/l. Plasma levels of free fatty acids were increased from 0.40 ± 0.06 to 0.96 ± 0.09 mmol/l | |||
| 12954066 | 2003 | Neurotensin | 13 | Free | Free | Linear | L | None | Bovine hypothalamus | Induction of cyclic nucleotide production, intracellular calcium influx, Na+K+-ATPase activation, muscle relaxation, decreased food consumption, catalepsy,decreased locomotion, hypothermia, antinociception, antipsychosis | Not mentioned | 1.07mM | 5.9 ±0.2 | Rat serum protease | MALDI-TOF-MS | Rat serum | in vitro | None | None | Biological effect of peptide is evaluated by binding to its receptor i.e hNTR. Cell membranes are tansfected with either hNTR-1 or hNTR-2 were incubated with 0.4 nM 125I-Tyr (3)-NT (2000 Ci/mmol) and various concentrations of unlabeled NT, or NT analogue.Total binding 8500 and nonspecific binding 2500 for 70 μg of protein per formed on whole cells. | |||
| 12954066 | 2003 | 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. | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 21.2 ±1.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Thioridazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 19.6 ±1.0 | Human blood plasma proteases | TLC | Human plasma mixed with drug Fluphenazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 17.2 ±0.9 | Human blood plasma proteases | TLC | Human plasma mixed with drug AS-1397 | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 17.1 ±1.0 | Human blood plasma proteases | TLC | Human plasma mixed with drug Promethazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 17.1 ±1.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Chlorpromazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.5 ±0.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Methotrimeprazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.1 ±0.2 | Human blood plasma proteases | TLC | Human plasma mixed with drug Methotrimeprazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.9 ±0.2 | Human blood plasma proteases | TLC | Human plasma mixed with drug Prochlorperazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.4 ±0.3 | Human blood plasma proteases | TLC | Human plasma mixed with drug Trifluoperazine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.4 ±0.3 | Human blood plasma proteases | TLC | Human plasma mixed with drug Molindone | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.4 ±0.4 | Human blood plasma proteases | TLC | Human plasma mixed with drug Loxapine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 12.1 ±0.1 | Human blood plasma proteases | TLC | Human plasma mixed with drug Clozapine | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.9 ±0.3 | Human blood plasma proteases | TLC | Human plasma mixed with drug Haloperidol | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.9 ±0.4 | Human blood plasma proteases | TLC | Human plasma mixed with drug Sulpiride | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 11.3 ±0.4 | Human blood plasma proteases | TLC | Human plasma mixed with drug Thiothixene | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 31.3 ±0.7 | Human blood plasma proteases | TLC | Human plasma mixed with Bacitracin | in vitro | None | None | Not mentioned | |||
| 12444298 | 2001 | Leucine Enkephalin | 5 | Free | Free | Linear | L | None | Human brain | Regulation of various physiological and behavioral processes | 2, 4, 6, 10, 30, 60 and 90, 180 minutes | 10 €“8 M | 41.1 ±0.9 | Human blood plasma proteases | TLC | Human plasma mixed with Bacitracin | in vitro | None | None | Not mentioned | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.033 ±0.004 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 1.22 ±0.237 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 5.88 ±0.374 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.064 ±0.052 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.971 ±0.336 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 8.97 ±4.50 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.032 ±0.005 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.321 ±0.0.091 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 6.23 ±1.47 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 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 | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 1.25 μg/kg | 14 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 32 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 2.5 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 33 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 5.0 μg/kg | 8.1 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Intravenously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 34 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 5.0 μg/kg | 15 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 35 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 10 μg/kg | 14 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 36 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 12.5 μg/kg | 12 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 37 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 15 μg/kg | 13 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 38 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 17.5 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 39 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 20 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12489813 | 2002 | Bradykinin | 5 | Free | Free | Linear | L | None | Kininogen | Vasodilating peptide | Not mentioned | 100 ng/ml | 15 | Rat blood proteases | Radioimmunoassay using new radioionated analogue RPPG(125I)F | Cultured rat aortic smooth muscle cells | 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 | |||
| 15740458 | 2005 | Rat AM (Adrenomedullin) | 50 | Free | Free | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 200 μl | 2 (distribution t1/2) | Rat blood proteases | Competitive Radioimmunoassay | Intravenous administration in Rat | in vivo | http://www.anaspec.com/products/product.asp?id=304 | None | Not reported | |||
| 15740458 | 2005 | Rat AM (Adrenomedullin) | 50 | Free | Free | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 200 μl | 15.9 (elimination t1/2) | Rat blood proteases | Competitive Radioimmunoassay | Intravenous administration in Rat | in vivo | http://www.anaspec.com/products/product.asp?id=304 | None | Not reported | |||
| 15828822 | 2005 | Peptide1 | 7 | Acetylation | N-Ethylmaleimidation | Linear | Mix | None | Second type 1 repeat of thrombospondin-1 | Antiangiogenic activity | Not mentioned | 5mg/kg | <1 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = >100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.2 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 1.2 | Mouse plasma proteases | Not mentioned | Mouse plamsa | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.5 | Monkey plasma proteases | Not mentioned | Monkey plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 5 (ABT-526) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.5 | Proteases from dog plasma | Not mentioned | Dog plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.03 ± 0.015 nM, Inhibition of HMVEC tube formation with IC50 = 200-100nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.2 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.15 | Mouse plasma proteases | Not mentioned | Mouse plamsa | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 1.2 | Monkey plasma proteases | Not mentioned | Monkey plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compond 6 (ABT-510) | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | 4th AA is D isoform of allo- Ile, Sar- Sarcosine | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.8 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.89 ± 0.029 nM, Inhibition of HMVEC tube formation with IC50 = 10-50nM | |||
| 15828822 | 2005 | Compund 4 | 8 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine, Nva-Norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.3 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 = 0.07 ± 0.004 nM, | |||
| 15828822 | 2005 | Compound 7 | 9 | NHIsp | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , Nva-Norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.9 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =29 ± 0.003 nM, Inhibition of HMVEC tube formation with IC50 = >1000nM | |||
| 15828822 | 2005 | Compound 8 | 9 | Succinylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine ,Nva-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.2 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.26 ± 0.110 nM, Inhibition of HMVEC tube formation with IC50 = 10-5nM | |||
| 15828822 | 2005 | Compound 9 | 9 | Acetylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , NMeNva- N-methyl-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 1 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.54 ± 0.150 nM, Inhibition of HMVEC tube formation with IC50 = 50-25nM | |||
| 15828822 | 2005 | Compound 10 | 9 | Succinylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , NMeNva- N-methyl-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 2.1 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.45 ± 0.110 nM, Inhibition of HMVEC tube formation with IC50 = 10 -5nM | |||
| 15828822 | 2005 | Compound 11 | 9 | Succinylation | N-Ethylmaleimidation | Linear | Mix | Sar- Sarcosine , NMeNva- N-methyl-norvaline | Synthetic (derived from peptide 1) | Antiangiogenic activity | Not mentioned | 5mg/kg | 0.3 | Rat plasma proteases | Not mentioned | Rat plasma | in vivo | None | None | Inhibition of HMVEC migration with IC50 =0.06 ± 0.030 nM, Inhibition of HMVEC tube formation with IC50 = 0.25- 0.10nM | |||
| 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 | |||
| 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 | |||
| 17766836 | 2003 | NT (Neurotensin) [8-13] | 24 | Free | Pegylation | Linear (Tetra-branched) | L | 4 Hexapeptide bound to PEG-Biotin to form tetra branched | Synthetic | Regulates luteinizing hormone and prolactinrelease | 37 °C for 2-24 hours | Not mentioned | >24 | 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 | |||
| 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 | |||
| 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 | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 100μg/kg | 8.4 ±4(t1/2α) | Diestrous female rats blood proteases | Radioimmunoassay | Intravenous injection in diestrous female rats | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 100μg/kg | 33.2 ±6.8(t1/2β) | Diestrous female rats blood proteases | Radioimmunoassay | Intravenous injection in diestrous female rats | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 1mg | 2.9 ±60.5(t1/2β) | Diestrous female rats blood proteases | Radioimmunoassay | Intravenous injection in 6 healthy humans serum | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 1mg | 3.6 ±1.2(t1/2β) | Diestrous female rats blood proteases | Radioimmunoassay | Subcutaneous injection in 6 healthy humans serum | in vivo | None | None | Not mentioned | |||
| 12083977 | 2002 | Leuprorelin | 9 | 5-oxo | Ethylacetate | Linear | Mix | None | Synthetic agonist analogue of gonadotropin-releasing hormone | Suppression of gonadal steroid synthesis, resulting in pharmacological castration | Not mentioned | 10 µg | 32(t1/2β) | Pregnant female rats blood proteases | Radioimmunoassay | Subcutaneous injection in pregnant rats | in vivo | 3083092 | None | Not mentioned | |||
| 12083977 | 2002 | GnRH (Gonadotropin-releasing hormone) | 10 | PyroGlu=Pyroglutamic acid | Free | Linear | L | pGlu=pyroglutamic acid | Hypothalamic neurons | Regulating the synthesis and secretion of the gonadotropins luteinising hormone (LH) and follicle-stimulating hormone (FSH). | Not mentioned | Not mentioned | less than 15 | Human plasma proteases | Radioimmunoassay | Human blood | in vivo | None | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.17 ±0.05 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Breast fed healthy infants(0-1years)serum sample | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.48 ±0.007 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Formula fed healthy infants(0-1years)serum sample | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.26 ±0.06 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of healthy infant boys(0-1 years) | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.51 ±0.08 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of healthy infant girls(0-1 years) | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 2.37 ±0.05 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of children(0-1 years) | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15452596 | 2004 | Leu-enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid ligand | Indicator of Endogenous opioid system which is characterized by biological effects, including adaptogenic and antinociceptive activity, regulation of the emotional sphere, behavior research,learning and memory. | Not mentioned | Not mentioned | 3.10 ±0.05 | Enkephalin-degrading enzymes present in blood serum | Accumulation of radioactive 3H-leu-enkephalin degradation products ,Thin layer chromatography | Serum sample of adults | in vivo | O. Yu. Sokolov, M. V. Gabaeva, K. G. Gurevich, et | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 90mg | 3.16(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Intravenous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 45mg | 3.46(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Subcutaneous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 90mg | 3.8(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Subcutaneous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 180mg | 4.35(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Subcutaneous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned |