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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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 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 | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 11.95 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch1 | in vitro | None | None | Not reported | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 18.73 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch2 | in vitro | None | None | Not reported | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 4.62 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch3 | in vitro | None | None | Not reported | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 7.29 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch4 | 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 | |||
| 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 | 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 | |||
| 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 | |||
| 11054637 | 2000 | Ovine Brain natriuretic peptide (oBNP) | 29 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 2.6 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | None | None | Kd=16pM for receptor binding | |||
| 11054637 | 2000 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | 1826098 | None | Kd=10pM for receptor binding | |||
| 11054637 | 2000 | Ovine Brain natriuretic peptide (oBNP) | 29 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3.1 | Human blood proteases | HPLC | Injected in humans | in vivo | None | None | Kd=16pM for receptor binding | |||
| 11054637 | 2000 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 22 | Human blood proteases | HPLC | Injected in humans | in vivo | 1826098 | None | Kd=10pM for receptor binding | |||
| 20382695 | 2010 | Taspoglutide | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Derivative of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 9.8 | Rat plasma protease | RP-HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.06nM for stimulating cAMP production | |||
| 20382695 | 2010 | hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | None | Glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 50 | Rat plasma protease | RP-HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.08nM for stimulating cAMP production | |||
| 20418955 | 2010 | Glucagon | 29 | Free | Free | Linear | L | None | Glucagon | Regulate blood glucose | Not mentioned | Not mentioned | <10 | Not reported | Not mentioned | Not reported | in vivo | None | None | Elevated blood glucose levels for <2 hours | |||
| 21114599 | 2010 | hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | None | Glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 0.9 ±0.1 | Rat plasma proteases | HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.08 ±0.03nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib8]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 5.9 ±1.0 | Rat plasma proteases | HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.29 ±0.22nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib35]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 2.0 ±0.3 | Rat plasma proteases | HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.05 ±0.01nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib8,35]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide1 | Regulate blood glucose | Not mentioned | Not mentioned | 20.4 ±1.8 | Rat plasma proteases | HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.06 ±0.04nM for cAMP stimulation | |||
| 21114599 | 2010 | hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | None | Glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 10.3 | Human plasma proteases | HPLC | Human plasma | in vitro | 14759771 | None | EC50=0.08 ±0.03nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib8]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 12.1 | Human plasma proteases | HPLC | Human plasma | in vitro | 14759771 | None | EC50=0.29 ±0.22nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib35]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 18.4 | Human plasma proteases | HPLC | Human plasma | in vitro | 14759771 | None | EC50=0.05 ±0.01nM for cAMP stimulation | |||
| 21114599 | 2010 | [Aib8,35]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide1 | Regulate blood glucose | Not mentioned | Not mentioned | 66 | Human plasma proteases | HPLC | Human plasma | in vitro | 14759771 | None | EC50=0.06 ±0.04nM for cAMP stimulation | |||
| 20631047 | 2010 | Xenin | 25 | Free | Free | Linear | L | None | Secreted from intestinal K-cells | Regulates insulin | 360 minutes | Not mentioned | 162 ±6 | Mice plasma proteases | HPLC | Mice plasma | in vitro | 1429581 | None | Stimulated insulin secretion at 5.6 mM In clonal BRIN-BD11 cells | |||
| 22286034 | 2012 | Motilin | 22 | Free | Free | Linear | L | None | Motilin is a gastro-intestinal peptide hormone | Endocrine regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 3.3 ±1.0 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.9x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“28) | 29 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.6x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(14 €“28) | 27 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.0 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=6.1x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(16 €“28) | 25 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 9.4 ±0.6 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.2x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(18 €“28) | 23 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 5.3 ±1.3 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.0x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(19 €“28) | 22 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 6.0 ±0.3 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.1x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“26) | 27 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 10.4 ±0.1 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.5x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“24) | 25 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 5.8 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=4.8x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“22) | 23 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 6.3 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=2.4x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“20) | 21 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 7.0 ±2.6 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=7.3x10-11nM for GPR38 agonist activity | |||
| 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 | |||
| 22592200 | 2012 | Ghrelin | 28 | Free | Free | Linear | L | Fatty acid ie n-octanoic acid present at serine at position 3, (125)I labelling | Ghrelin | GH-releasing and appetite stimulating peptide | Not reported | Not mentioned | 15-18 | Rat blood proteases | Radioactivity measured by scintillation counter | Administered into blood of rats | in vivo | 15788704 | None | Not reported | |||
| 17904340 | 2008 | GLP-1 | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 0.51 ±0.02 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | Oral hypoglycemic efficacy in db/db mice was 2.7 ±12.1% | |||
| 17904340 | 2008 | GLP-1 | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 0.79 ±0.01 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | Oral hypoglycemic efficacy in db/db mice was 2.7 ±12.1% | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.17 ±0.08 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | Intraperitoneal hypoglycemic efficacy in db/db mice was 30 ±7.2% | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.34 ±0.07 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | Intraperitoneal hypoglycemic efficacy in db/db mice was 30 ±7.2% | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 4.34 ±0.21 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | Oral hypoglycemic efficacy in db/db mice was 25.3 ±6.6% | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 2.77 ±0.05 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | Oral hypoglycemic efficacy in db/db mice was 25.3 ±6.6% | |||
| 17904340 | 2008 | GLP-1 | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 0.51 ±0.02 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | EC50=3.64 ±0.25nM insulinotropic activity | |||
| 17904340 | 2008 | GLP-1 | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 0.79 ±0.01 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | EC50=3.64 ±0.25nM insulinotropic activity | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.17 ±0.08 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | EC50=3.82 ±0.32nM insulinotropic activity | |||
| 17904340 | 2008 | Lys34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 1.34 ±0.07 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | EC50=3.82 ±0.32nM insulinotropic activity | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 4.34 ±0.21 | Proteases in rat intestinal fluid | RP-HPLC | Rat intestinal fluid | in vitro | None | None | EC50=3.85 ±0.21nM insulinotropic activity | |||
| 17904340 | 2008 | Lys26,34-biotin-GLP-1 | 30 | Free | Amidation | Linear | L | Biotinylation at Lys at 34th and 26th position | Biotinylated derivative of GLP-1 | Regulates blood glucose levels | Not reported | 200 µg/ml | 2.77 ±0.05 | Proteases in rat intestinal homogenate | RP-HPLC | Rat intestinal homogenate | in vitro | None | None | EC50=3.85 ±0.21nM insulinotropic activity | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 0.42 ±0.03 | Rat blood proteases | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | ANP' | 26 | Free | Free | Cyclic | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 1.04 | Rat blood proteases | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 7.81 ± 0.38 | Kallikrein and Endopeptidase 24.11 in presence of inhibitor Phosphoramidon | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 2.51 ±0.25 | Kallikrein and Endopeptidase 24.11 in presence of inhibitor Aprotinin | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 1697165 | 1990 | Atrial natriuretic peptide (ANP) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 0.17-0.25 MBq | 15.2 ± 1.01 | Kallikrein and Endopeptidase 24.11 in presence of inhibitors phosphoramidon and aprotinin both | Radioimmunoassay and RP-HPLC | Rat blood plasma (infused into fumoral vein and right carotid artery) | in vivo | None | None | Not given | |||
| 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 | |||
| 16472750 | 2006 | E2-PEST | 29 | Free | Free | Linear | L | None | E2 protein from papillomavirus | Gene transcription | Not reported | Not mentioned | 63 | in aCSF | Pulse chase experiment | pMEP-E2 CV-1 cell lines | in vitro | 15014086 | None | Not mentioned | |||
| 16472750 | 2006 | E2-PESTP299A | 29 | Free | Free | Linear | L | None | E2 protein from papillomavirus | Gene transcription | Not reported | Not mentioned | 94 | Not mentioned | Pulse chase experiment | pMEP-E2 CV-1 cell lines | in vitro | 15014086 | None | Not mentioned | |||
| 16472750 | 2006 | E2-PESTE304Q | 29 | Free | Free | Linear | L | None | E2 protein from papillomavirus | Gene transcription | Not reported | Not mentioned | 24 | Not mentioned | Pulse chase experiment | pMEP-E2 CV-1 cell lines | in vitro | 15014086 | None | Not mentioned | |||
| 16586064 | 2006 | GLP1 | 30 | Free | Amidation | Linear | L | None | Synthetically synthesized Glucagon-like peptide-1 | Insulinotropic | Not reported | Not mentioned | 114 ±28 | Rat plasma proteases | RP-HPLC | Rat plasma | in vitro | 16505481 | None | 380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | GLP1 | 30 | Free | Amidation | Linear | L | None | Synthetically synthesized Glucagon-like peptide-1 | Insulinotropic | Not reported | Not mentioned | 6 ±0.5 | Rat liver proteases | RP-HPLC | Rat liver homogenate | in vitro | 16505481 | None | 380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | GLP1 | 30 | Free | Amidation | Linear | L | None | Synthetically synthesized Glucagon-like peptide-1 | Insulinotropic | Not reported | Not mentioned | 1 ±0.2 | Rat kidney proteases | RP-HPLC | Rat kidney homogenate | in vitro | 16505481 | None | 380 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | N-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at N terminus His7 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 7560 ±5635 | Rat plasma proteases | RP-HPLC | Rat plasma | in vitro | 16505481 | None | 290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | N-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at N terminus His7 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 250 ±117 | Rat liver proteases | RP-HPLC | Rat liver homogenate | in vitro | 16505481 | None | 290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | N-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation at N terminus His7 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 23 ±7 | Rat kidney proteases | RP-HPLC | Rat kidney homogenate | in vitro | 16505481 | None | 290 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | Lys-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation on Lys34 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 4471 ±1822 | Rat plasma proteases | RP-HPLC | Rat plasma | in vitro | 16505481 | None | 150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | Lys-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation on Lys34 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 62 ±23 | Rat liver proteases | RP-HPLC | Rat liver homogenate | in vitro | 16505481 | None | 150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16586064 | 2006 | Lys-PEG/GLP-1 | 30 | Free | Amidation | Linear | L | Pegylation on Lys34 | Synthetically synthesized Glucagon-like peptide-1 analogues | Insulinotropic | Not reported | Not mentioned | 28 ±1 | Rat kidney proteases | RP-HPLC | Rat kidney homogenate | in vitro | 16505481 | None | 150 ([pmol/l] islet-1 h-1) insulin release at -7 (log [mol/l]) | |||
| 16892368 | 2006 | Dimeric C46 | 26 | Glycosylation | Amidation | Linear | L | None | Derived from T20 | HIV-1 fusion inhibitory peptide | Not reported | 40 ng peptide/200 mL plasma | 1.75 | Mouse plasma proteases | ELISA | Mouse plasma | in vitro | None | None | Not given | |||
| 16892368 | 2006 | Dimeric C46 | 26 | Glycosylation | Amidation | Linear | L | None | Derived from T20 | HIV-1 fusion inhibitory peptide | Not reported | 40 ng peptide/200 mL plasma | 1 | Rat plasma proteases | ELISA | Rat plasma | in vitro | None | None | Not given | |||
| 16892368 | 2006 | Dimeric C46 | 26 | Glycosylation | Amidation | Linear | L | None | Derived from T20 | HIV-1 fusion inhibitory peptide | Not reported | 40 ng peptide/200 mL buffer | 4.25 | Not mentioned | ELISA | PBS/1% BSA | in vitro | None | None | Not given | |||
| 17479256 | 2007 | ANP | 26 | Free | Free | Linear | L | None | Synthetic peptide | Atrial natriuratic peptide | Not reported | 0.05 μg/kg per minute | 2.4 ±0.7 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not given | |||
| 17537541 | 2007 | Vasoactive intestinal peptide (VIP) | 28 | Free | Free | Linear | L | None | Vasoactive intestinal peptide | Neurotransmitter | Not reported | Ki=2.63 ±0.87 nM | 1.38 | Not mentioned | Not mentioned | Rat lung alveolar L2 cells | in vitro | None | None | Not given | |||
| 17986790 | 2007 | GLP-1/HAS | 30 | Free | Human serum albumin | Linear | L | None | Glucagon | Glucose-dependent insulinotropic effect | Not reported | 0.1 µmol/kg | 10 | Mouse blood proteases | ELISA | Mouse plasma (Intraperitoneally administered) | in vivo | None | None | 0.1 mmol/kg had glucose-lowering effect up to 4 h after administration | |||
| 18085721 | 2007 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Counter-regulatory hormone | Not reported | Not mentioned | ~2 | DPP-IV | ELISA | Mouse plasma | in vivo | None | None | Not given | |||
| 19053766 | 2008 | CGRP(8-37)-NH2 derivative 32 | 30 | Acetylation | Amidation | Linear | L | None | Calcitonin gene-related peptide | Neuropeptide | Not reported | 10 µg/ml | 38 | Monkey plasma proteases | ELISA | Monkey plasma | in vitro | None | None | IC50=3.57 ± 0.04 nM | |||
| 19053766 | 2008 | CGRP(8-37)-NH2 derivative 32 | 30 | Acetylation | Amidation | Linear | L | None | Calcitonin gene-related peptide | Neuropeptide | Not reported | 10 µg/ml | 68 | Human plasma proteases | ELISA | Human plasma | in vitro | None | None | IC50=3.57 ± 0.04 nM | |||
| 19403044 | 2008 | GLP-1/Fc | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | 16nM | ~20 | Rabbit serum proteases | Luciferase reporter assay | Rabbit serum | ex vivo | None | None | Not available | |||
| 19403044 | 2008 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | 0.4nM | <5 | Rabbit serum proteases | Luciferase reporter assay | Rabbit serum | ex vivo | None | None | Not available | |||
| 19458086 | 2009 | ANP | 28 | Free | Free | Cyclic (C7-C23) | L | None | C terminus of atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 1 µM | 2.6 | Human kidney membrane proteases | Radioimmunoassay | Human kidney membranes | in vitro | None | None | IC50=2.4nM | |||
| 19531053 | 2009 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | Not mentioned | 20 | DPP IV | ELISA | Mice (Subcutaneous injection) | in vivo | None | None | Not available | |||
| 19552923 | 2011 | GLP-1-Tf | 30 | Human transferrin protein | Amidation | Linear | L | None | Proglucagon molecule | Insulinomimetic and insulinotropic | Not reported | 27.9 ± 5.8 μg/ml | 27 | Rabbit blood proteases | ELISA | Rabbit serum (Intravenous injection) | in vivo | None | None | Not available | |||
| 19552923 | 2011 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Insulinomimetic and insulinotropic | Not reported | 27.9 ± 5.8 μg/ml | 1 to 2 | Rabbit blood proteases | ELISA | Rabbit blood | in vivo | None | None | Not available | |||
| 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 | |||
| 18353507 | 2008 | PACAP27 | 27 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | 39 ±4 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 9.6 ±2.4 nM | |||
| 18353507 | 2008 | PACAP27 | 27 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | >120 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 9.6 ±2.4 nM | |||
| 18353507 | 2008 | Acetyl-PACAP27 | 27 | Acetylation | Amidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 9.6 ±1.5 nM | |||
| 18353507 | 2008 | Hexanoyl-PACAP27 | 27 | Hexanoylation | Amidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 10.6 ±2.4 nM | |||
| 18353507 | 2008 | [Aib2]PACAP27 | 27 | Free | Amidation | Linear | L | Aib | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | 145 ±23 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 7.9 ±1.8 nM | |||
| 18353507 | 2008 | [D-Ser2]PACAP27 | 27 | Free | Amidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 10.3 ±2.1 nM | |||
| 18353507 | 2008 | Acetyl-PACAP27-propylamide | 27 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 6.7 ±1.2 nM | |||
| 18353507 | 2008 | Acetyl-PACAP27-propylamide | 27 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | >120 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 6.7 ±1.2 nM | |||
| 18353507 | 2008 | Acetyl-PACAP27-hexylamide | 27 | Acetylation | Hexylamidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 5.6 ±1.3 nM | |||
| 18353507 | 2008 | Acetyl-PACAP27-hexylamide | 27 | Acetylation | Hexylamidation | Linear | L | None | Synthetic analog of PACAP27 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | >120 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 5.6 ±1.3 nM | |||
| 21664938 | 2011 | GLP-1 | 30 | Free | Free | Linear | L | None | Proglucagon molecule | Anti-hyperglycemic hormone | Not reported | 300 μg/kg | <2 | Rat blood proteases | ELISA | Serum of rats (Subcutaneous injection) | in vivo | None | None | Binding constants to the GLP-1 receptor= 27.62 ± 2.13nM | |||
| 22698865 | 2012 | TRAF6 Inhibitory peptide | 27 | Free | Free | Linear | L | None | TNF receptor associated factors 6 | Intracellular adapter protein | Not reported | 1.5 mg (peptide)/mice | 5.08 | Mouse blood proteases | Spectrofluorometry | Mice serum | in vivo | None | None | Not mentioned | |||
| 22698865 | 2012 | PEGylated TRAF6 Inhibitory peptide | 27 | Pegylation | Free | Linear | L | None | TNF receptor associated factors 6 | Intracellular adapter protein | Not reported | 1.5 mg (peptide)/mice | 8.99 | Mouse blood proteases | Spectrofluorometry | Mice serum | in vivo | None | None | Not mentioned | |||
| 23836030 | 2013 | HNG ( substitution at position 14 (Gly for Ser) in HN seq) | 24 | Free | Free | Linear | L | None | Synthetic peptide | Cytoprotective | Not reported | 16 fold higher than original concentration | ~30 | Mouse plasma proteases | ELISA | Mice plasma | in vitro | 15655255 | None | Not available | |||
| 6117506 | 1981 | Vasoactive Intestinal Peptide | 28 | Free | Amidation | Linear | L | None | Porcine vasoactive intestinal peptide | Vasoactive intestinal peptide | Not reported | 103.7 ± 14.8 ml/kg | 1.80 ± 0.1 | Dog blood proteases | Radioimmunoassay | Dog plasma (Intravenous) | in vivo | None | None | 150-220 µci/ µg | |||
| 8181115 | 2014 | Atrial natriuretic factor (ANF) | 28 | Free | Free | Linear | L | None | Cardiac atria | Peptide hormone | Not reported | Not mentioned | 2.5 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not available | |||
| 8406670 | 2014 | Atrial natriuretic factor (ANF) | 28 | Free | Free | Linear | L | None | Cardiac atrium in response to myocardial stretch | Peptide hormone | Not reported | Not mentioned | 20 to 180 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not available | |||
| 20418955 | 2010 | Glucagon | 29 | Free | Free | Linear | L | None | Pancreas | Plays a major regulatory role in controlling hypoglycemia | Not reported | Not mentioned | <10 | Human blood proteases | ELISA | Human serum | in vitro | None | None | Not available | |||
| 20418955 | 2010 | Gcg-XTEN-288 (glucagon-XTEN fusion peptide) | 29 | Free | XTEN-288 | Linear | L | None | Glucagon-288 amino acid XTEN fusion peptide | Glucose homeostasis | Not reported | 12 nmol/kg | 9 | Monkey blood proteases | ELISA | Monkey plasma (Subcutaneous) | in vivo | None | None | Biologically active in cynomolgus monkeys for 6 hours | |||
| N.A. | 2011 | Motilin | 22 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 3.26 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin H | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.43 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin I | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.76 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin J | 25 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 6.34 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin K | 23 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 6.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin L | 21 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 4.89 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin N | 28 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.12 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin O | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.73 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin P | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.67 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Q | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.65 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin R | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.13 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin S | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.29 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin T | 29 | Free | Free | Linear | L | Ornithine | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.47 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin U | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.66 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin V | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin W | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin X | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.89 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Y | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.6 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Z | 30 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.53 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-i | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.55 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-iv | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.73 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-v | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.94 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-ix | 26 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 4.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-x | 28 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.25 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xi | 26 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.29 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 2.88 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 11.2 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 7.8 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 2.93 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-58 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 1.11 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| 15817669 | 2007 | Derivative of Growth hormone releasing factor | 30 | Free | Addition of maleimidopropionic acid (MPA) and amidation | Linear | Mix | None | GRF peptide | Growth harmone and somatostatin releasing factor | N.A. | 1microM/ Kg | 25.8 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | US7268113B2 | Area under curve (AUC) for growth hormone (GH) release >10000 (ng/ml)*minute | |||
| 15817669 | 2007 | Derivative of Growth hormone releasing factor | 30 | Free | Addition of maleimidopropionic acid (MPA) and amidation | Linear | Mix | None | GRF peptide | Growth harmone and somatostatin releasing factor | N.A. | 100 nM/ Kg | 18.7 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | US7268113B2 | Not mentioned | |||
| 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 | |||
| 641324 | 1983 | Peptide histidine isoleucine | 27 | Free | Free | Linear | L | None | Porcine intestine | Neurotransmitter | 1, 2, 3, 4, 5, 10 and 15 min. | 4.7 pmoles/kg | 3.1 ±0.5 | Human plasma proteases | Radioimmunoassay | Intravenous administration to human plasma | in vivo | None | None | PHI effect on secretion on gastrointestinal hormone and monitor its effect on gastric secretion of pepsin. PHI infused at 4.7pmoles/kg in human and gastric juice were aspirated by suction, gastric secretion was improved to be in case of PIH. | |||
| 6127205 | 1982 | Somatostatin 28 | 28 | Free | Free | Cyclic (C17-C28) | L | None | Ovine hypothalamus | Regulates the endocrine system and affects neurotransmission and cell proliferation | 30-45 minute | 20 µg | 2.8 ±0.3 | Dog blood plasma | SS Radioimmunoassay assay | Intravenous infusion in Dog plasma | in vivo | http://www.anaspec.com/products/product.asp?id=574 | None | When 50ng of SS14 was injected there is 85.1% decreasedportal venous blood flow was observed as compared to percentage of basal flow. | |||
| 6128770 | 1982 | Somatostatin 28 | 28 | Free | Free | Cyclic (C17-C28) | L | None | Ovine hypothalamus | Regulates the endocrine system and affects neurotransmission and cell proliferation | 1 hour | 4.8nmol | 6.1 | cat blood protease | Not mentioned | Intravenous infusion to cat plasma | in vivo | http://www.anaspec.com/products/product.asp?id=574 | None | Gastrin exocrine inhibitor assay were performed. 80 % gastric inhibition observed at 7ug/kg of peptide. | |||
| 6239307 | 1984 | Atrial Natriuretic peptide | 28 | Free | Free | Cyclic (C7-C23) | L | None | Human heart | Depressor and natriuretic activity | 2 hours | 1nmol | 30 | Rat blood proteases | RP-HPLC | Intravenous administered to Rat | in vivo | None | None | Gastric exocrine inhibitory assay was performed. 80 % inhibition observed at 8ug/kg body weight of peptide | |||
| 6239307 | 1984 | Atriopeptin 3 | 24 | Free | Free | Cyclic (C3-C19) | L | I125 radiolabeled | Human heart | Depressor and natriuretic activity | 2 hours | 1nmol | 2.5 | Rat blood proteases | RP-HPLC | Intravenous administered to Rat | in vivo | None | None | Time course depression is seen and Atropeptin 3 shows 2 time more depressor activity as compared to control alpha heart ANP. | |||
| 6736205 | 1984 | Gastrin releasing peptide | 27 | Free | Free | Linear | L | None | Porcine nonantral gastric juice | Stimulate release of gastrin | Not given | GRP I (0-30 min) bolus injection of 1.41 pmol kg-1, followed by an infusion of 0.12 pmol kg-1 x min- | 2.8 ±0.4 min | Human serum proteases | Radioimmunoassay | Human serum | in vivo | http://www.anaspec.com/products/product.asp?id=301 | None | Plasma gastrin concentration increased immediately after administration of peptide intravenously. After two doses of peptide(1.50pmol/kg) gastrin concentration found to be 1551pmol as compared to basal level of 370pmol. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 0.8 ±0.1 (t1/2 fast phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats treated with carvedilol | in vivo | None | None | ANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 0.9 ±0.1 (t1/2 fast phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats | in vivo | None | None | ANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 7.7 ±0.8 (t1/2 slow phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats treated with carvedilol | in vivo | None | None | ANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group. | |||
| 9421401 | 1998 | Atrial Natriuretic peptide | 28 | Free | Free | Linear | L | None | Human Heart muscle cells | Antihypertensive | 0.5, 1, 1.5, 2, 3, 5, 8, 15, and 25 min | 2 μg | 4.9 ±0.5 (t1/2 slow phase) | Rat plasma proteases | Radioimmunoassay | Exogenously administered to Male SHR-SP/Izm rats | in vivo | None | None | ANP role in antihypertension and blood pressure is determined by injecting ANP peptide(8mg/kg of body weight) in carvedilol and control group. The systolic blood pressure was decreased after 1 week of treatment in carvedilol treated group. | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling and encapsulation of VIP in Liposome | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 5.29 ±0.62 (t1/2 elimination) | Rat plasma proteases | Not mentioned | Intravenously administration to rat plasma | in vivo | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 0.62 ±0.05 (t1/2 elimination) | Rat plasma proteases | Not mentioned | Intravenously administration to rat plasma | in vivo | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling and encapsulation of VIP in Liposome | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 9.28 ±0.76 (t1/2 elimination) | Rat lung proteases | Not mentioned | Intravenously administration to rat lung | in vitro | PMID 5450698 | None | Not tested | |||
| 10708307 | 1999 | Vasoactive intestinal peptide | 28 | Free | Free | Linear | L | I125 radiolabeling | Porcine intestine | Relaxation of the airway smooth muscle, attenuation of acute inflammation, regulation of mucus secretion | 1.5, 2.5, 5, 10, 15, 20, 30, 40, and 60 min | 0.33 nM | 3.18 ±0.22 (t1/2 elimination) | Rat lung proteases | Not mentioned | Intravenously administration to rat lung | in vitro | PMID 5450698 | None | Not tested | |||
| 10973845 | 2000 | Alpha 2-antiplasmin (α2AP ) | 24 | Free | Free | Linear | L | I125 radiolabeling | Human SERPINF2 gene | Clotting factor | 2 hours | 2 mg/ml | 19 | Mouse blood proteases | Not mentioned | Mouse blood fibrin clots | in vitro | None | None | Immunoblotting assay was done by taking 50 µL of fibrin clots with 2mg/ml of alpha2 AP and alpha2 AP peptide and cross linking was determined by electroblotting to PVDF membrane and detected by streptavidin-peroxidase. | |||
| 2182027 | 1990 | Endothelin 1 (ET-l) | 21 | Free | Free | Linear | L | Labelled with I125 | Synthetic peptide with the sequence of human and porcine Endothelin 1 | Vasoconstrictiong peptide | 15sec-6min | 0.2pmol | 40 | Wistar rats blood protease | HPLC | Wistar rats | in vivo | None | None | Causes vasoconstriction | |||
| 18937214 | 2009 | Carbofuran (methylcarbamyl-)-labeled tryptic peptide | 29 | Free | Free | Linear | L | Methylcarbamylated at serine (position 8) | Human Bche protein | Pesticide | Not mentioned | Not mentioned | 2 | Human blood proteases | HPLC | Human serum | in vivo | None | None | BChE activity was 88% inhibited at time zero, but became less inhibited with time as carbofuran was released from the active site Ser 198. | |||
| 7522585 | 1994 | Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP | 22 | Free | Free | Linear | Mix | None | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 9 | Mouse liver proteases | RP-HPLC and Electrochemical Detection | Mouse liver homogenate | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP | 22 | Free | Free | Linear | Mix | None | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 10 μg/ml | 4.6 | Mouse liver proteases | RP-HPLC and Electrochemical Detection | Mouse liver homogenate | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP | 22 | Free | Free | Linear | Mix | None | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 11.8 | SCLC proteases | RP-HPLC and Electrochemical Detection | Small cell lung cancer (SCLC) | in vitro | None | None | Act as growth factors | |||
| 7522585 | 1994 | Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP | 22 | Free | Free | Linear | Mix | None | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 10 μg/ml | >24 | SCLC proteases | RP-HPLC and Electrochemical Detection | Small cell lung cancer (SCLC) | in vitro | None | None | Act as growth factors | |||
| 7529108 | 1994 | Human endothelin-1 (Human ET-1) | 21 | Free | Free | Linear | L | None | Human Endothelin-1 | Vasoconstricting peptide | 180 minute | 3 nmol of peptide with 200 ng of enzyme | 37 (t1/2 of hydrolysis) | Endopeptidase-24.11(E-24.11) | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | Porcine endothelin-1 (Porcine ET-1) | 21 | Free | Free | Linear | L | None | Porcine Endothelin-1 | Vasoconstricting peptide | 80 minute | 3 nmol of peptide with 50 ng of enzyme | 56 (t1/2 of hydrolysis) | Thermolysin | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7689499 | 1993 | Galanin | 30 | Free | Free | Linear | L | None | Human tissue | Neuropeptide | 60 minutes | 74 pmol/kg | 3.7 ±0.4 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | 1370155 | None | Growth hormone concentrations increased markedly during galanin infusion reaching a plateau value eight times the pre-infusion concentrations after 40-min infusion p < 0.01 | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 28 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 13.3 (slow component) | None | Not mentioned | None | in vitro | 6223192 | None | Not reported | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 28 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 1.7 (fast component) | None | Not mentioned | None | in vitro | 6223192 | None | Not reported | |||
| 9234336 | 1993 | Vasoactive intestinal peptide (VIP) | 28 | Free | Free | Linear | L | None | Small intestinal mucosa | Vasoactive peptide | 2,3,6,10,20,40,60 minutes | 250 μg | 0.45 ±0.05 | Rat blood proteases | Radioimmunoassay | Intravenous injection to Rat blood | in vivo | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Regulate of blood flow and smooth muscle relaxation in specific mammalian organs | |||
| 9234336 | 1993 | Vasoactive intestinal peptide (VIP) | 28 | Free | Free | Linear | L | None | Small intestinal mucosa | Vasoactive peptide | 2,3,6,10,20,40,60 minutes | 250 μg | 2.3 ±0.8 | Rat blood proteases | Radioimmunoassay | Intravenous injection to Rat blood | in vivo | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Regulate of blood flow and smooth muscle relaxation in specific mammalian organs | |||
| 8388403 | 1993 | ANP (Atrial natriuretic Peptide) | 28 | Free | Free | Linear | L | None | Human Heart | Diuretic,natriuretic and vasodilatory peptide | 2 hours | 1.5 pmol/lg/min | 4.1 ±0.4 | Human serum proteases | Radioimmunoassay | Human serum | in vivo | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No significant differences in systolic blood pressure, diastolic blood pressure or pulse rate were observed when values on active and placebo infusions were compared (P = 0.85) | |||
| 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 | |||
| 18697865 | 2008 | Ghrelin | 28 | Free | Free | Linear | L | n-octanoyl group at ser 3 | Secreted by stomach P/D1-type cells | Stimulates apetite and GH secretion | Blood collected after 20 minutes to 2200 h after i/v injection of peptide | 1 µg/kg i/v injected | 21 ±3.0 | Human plasma proteases | Competitive Radioimmunoassay | Human plasma | in vivo | 15788704 | None | Not reported | |||
| 18697865 | 2008 | Ghrelin | 28 | Free | Free | Linear | L | n-octanoyl group at ser 3 | Secreted by stomach P/D1-type cells | Stimulates apetite and GH secretion | Blood collected after 20 minutes to 2200 h after i/v injection of peptide | 3 µg/kg i/v injected | 45 | Human plasma proteases | Competitive Radioimmunoassay | Human plasma | in vivo | 15788704 | None | Not reported | |||
| 22263969 | 2012 | ANP-Fc (Atrial natriuretic peptide- Fc) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation. | Natriuretic and vasodilator | 4-72 hours | 0.5mg/kg of protein | 2 to 5 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | GLP-1(7 €“36)NH2 [Glucagon-like peptide-1] | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulate blood glucose | Blood sample collected after 32-60 minutes after the infusion of peptide | 20pmol/kg | 4.8 ±0.8 | Pig kidneys proteases | Radioactivity measurement | Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | Ex(1 €“30) or Exendin(1 €“30) | 30 | Free | Free | Linear | L | None | Synthetic derived from Exendin 4 | GLP-1 receptor agonist | Blood sample collected after 42-130 minutes after the infusion of peptide | 20 pmol/kg | 28.4 ±1.7 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 5-120 minutes | 10mg/ml | >240 | Serum and plasma proteases | LC-MS | Male beagle dog plasma | in vitro | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 4 hours at 37C | 1 µM | >110 | Dog hepatocyte proteases | LC-MS | Male beagle dog hepatocyte | in vitro | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 2-120 minutes | 20μg/Kg | 0.05 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 3-120 minutes | 50μg/Kg | 0.54 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(7-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 4-120 minutes | 50μg/Kg | 2.1 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 25039358 | 2014 | Gly8-GLP-1(7-36)(Glucagon Like protein-1) | 30 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 37 °C for 2-72 hours | 1000ng/ml | 0.6 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 8.3 ± 0.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 6 | 30 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 15 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 18.1 ± 0.9 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 7 | 30 | Free | Amidation | Linear | L | X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 52.2 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 18.6 ± 1.3 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 8 | 30 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 12.9 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 7.1 ± 0.9 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 9 | 30 | Free | Amidation | Linear | L | X-2 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 21.6 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 8.1 ± 0.6 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 10 | 30 | Free | Amidation | Linear | L | X-1 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 11.8 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =12.1 ± 0.5 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 11 | 30 | Free | Amidation | Linear | L | X-2 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 20.3 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 19.9 ± 1.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 7 | 30 | Free | Amidation | Linear | L | X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 22 .9 ±7.2 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 = 18.6 ± 1.3 pM in HEK-293 cells | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 13 ±0.7 | Human plasma proteases + DPP IV | MS | Human Plasma+ Heparin | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 4 ±0.2 | Human plasma proteases + DPP IV | MS | Citrate + Human plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 4 ±0.2 | Human serum proteases + DPP IV | MS | Serum | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp and on Ice | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P700 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp and on Ice | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P800 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | Apr-24 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 12 ±3 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 2 ±0.4 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | Apr-14 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 10 ±0.5 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 37-96 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | Glucagon | 29 | Free | Free | Linear | L | None | Peptide hormone of pancrease | Regulates hypoglycemia | Room Temp | 0.4 µM | May-20 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | Glucagon | 29 | Free | Free | Linear | L | None | Peptide hormone of pancrease | Regulates hypoglycemia | Room Temp | 0.4 µM | 45 | Human plasma proteases + DPP IV | MS | P800 plasma | in vitro | None | None | Not reported | |||
| 26400022 | 2015 | Peptide 1 (Hirudin mimetic peptide) | 22 | Free | Amidation | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 13+-2.6 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 13.40 ± 0.46 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 5.80 ± 0.55nM | |||
| 26400022 | 2015 | Peptide S2 (Hirudin mimetic peptide) | 22 | Free | Amidation | Linear | Mix | Stearic acid at Lys | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 212.2 ±58.4 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 15.24 ± 0.18 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.75 ± 0.46nM | |||
| 21459096 | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Derived from parotid gland | Vasorelaxing | 37 °C for 0-125 minutes | Not mentioned | 1.3 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 21459096 | 2011 | CNP(C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | Secreted from vascular endothelium | Vasodialator | 37 °C for 0-125 minutes | Not mentioned | 4.3 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | 19395584 | None | Not reported | |||
| 24462899 | 2014 | APTEDB-DTX (Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate) | 27 | Free | Free | Linear | L | Modified Gly at 16th postion i.e. propargylglycine and peptide conjugated with drug DTX at this position | Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate | Drug(anticancer agent i.e. DTX) Delivery vehicle | Not mentioned | 5 mg DTX/kg Dose | 0.491 | Mice serum proteases | HPLC | C57BL6 mice Serum | in vivo | None | None | Stimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS | |||
| 1387608 | 1992 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Blood collected 1-60 minutes after peptide infused | 2μg/min | 12.5 (Terminal half life) | Human plasma proteases | IRM(Immunoradiometric assays) | Young Human plasma (average age 23.3) (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 1387608 | 1992 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Blood collected 1-60 minutes after peptide infused | 2μg/min | 9.6 (Terminal half life) | Human plasma proteases | IRM(Immunoradiometric assays) | Older Human plasma(average age 75.3) (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 1346149 | 1992 | SS-28 (Somatostatin-28) | 28 | Free | Free | Cyclic (C17-C28) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 228.1 ±76.5 (Metabolic half life) | Brodmann Area tissues proteases | Radioimmunoassay | Brodmann Area tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY) | in vitro | None | None | Not reported | |||
| 1346149 | 1992 | SS-28 (Somatostatin-28) | 28 | Free | Free | Cyclic (C17-C28) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 257.81 ±86.2(Metabolic half life) | Brodmann Area tissues proteases | Radioimmunoassay | Brodmann Area tissues of brain of SDAT(Medical Research Council Brain Bank, Cambridge, England) | in vitro | None | None | Not reported | |||
| 1346149 | 1992 | SS-28 (Somatostatin-28) | 28 | Free | Free | Cyclic (C17-C28) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 260.4 ±129.8 (Metabolic half life) | Hippucampal tissues proteases | Radioimmunoassay | Hippocampus tissues of brain of SDAT(Alzheimer's Disease Brain Bank, Bronx, NY) | in vitro | None | None | Not reported | |||
| 1346149 | 1992 | SS-28 (Somatostatin-28) | 28 | Free | Free | Cyclic (C17-C28) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 335.7 ±100.8 (Metabolic half life) | Hippucampul tissues proteases | Radioimmunoassay | Posterior Hippucampus tissues of brain of SDAT(Medical Research Council Brain Bank, Cambridge, England) | in vitro | None | None | Not reported | |||
| 1646465 | 1991 | rANP(99-126) (Recombinant atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | Not mentioned | 114 ±38.6 | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma | in vivo | None | None | Not reported | |||
| 1646465 | 1991 | 125I-rANP(1-45) (Recombinant atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | Iodinated at Tyr | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | 1 x 106 cpm | 20.2 ±5.3 (α- t1/2) | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 1649728 | 1991 | VIP(Vasoactive intestinal peptide) | 28 | Free | Amidation | Linear | L | None | Peptide hormone secreted by Intestine | Stimulates the secretion of electrolytes and water | Sample collected at 40-50 minutes | 10pmol min-1 kg -1 peptide infused | 0.50 ±0.11 | Rabbit plasma proteases | Radioimmunoassay | New Zealand White rabbits plasma(have low sodium diet i.e. 29.35 k 4.02 pmol/l) | in vivo | None | None | Not reported | |||
| 1649728 | 1991 | VIP(Vasoactive intestinal peptide) | 28 | Free | Amidation | Linear | L | None | Peptide hormone secreted by Intestine | Stimulates the secretion of electrolytes and water | Sample collected at 40-50 minutes | 10pmol min-1 kg -1 peptide infused | 1.27 ±0.20 | Rabbit plasma proteases | Radioimmunoassay | New Zealand White rabbits plasma(have normal sodium diet i.e. 29.35 k 4.02 pmol/l) | in vivo | None | None | Not reported | |||
| 1723638 | 1991 | Galanin(1-29) | 29 | Free | Amidation | Linear | L | None | Neuropeptide | Neuroendocrine activities, stimulates growth hormone secretion | 37 °C | 1 μM | 100 | Hypothalamic membrane protaeses | HPLC | Hypothalamic membranes of Male Sprague-Dawley rats | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | GRF(1-29)-NH2 (Growth hormone-releasing factor (GRF- Growth regulating factor)) | 29 | Free | Amidation | Linear | L | None | Growth regulating factor (GRF) | Release growth hormone | Not mentioned | 100 µg/ml | 0.25 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [Ala15]GRF(1-29)-NH2 | 29 | Free | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | 0.3 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [DesNH2-Tyr1,Ala15]GRF(1-29)-NH2 | 29 | Chlorpheniramine M | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | 1 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [DesNH2-Tyr1,D-Ala2,Ala15]GRF(1-29)-NH2 | 29 | Chlorpheniramine M | Amidation | Linear | Mix | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | 1 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [Asp8,Ala15]Cyclo(Asp8-Lys12)GRF(1-29)-NH2 | 29 | Free | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | ~ 4 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [D-Ala2,Asp8,Ala15]Cyclo(Asp8-Lys12)GRF(1-29)-NH2 | 29 | Free | Amidation | Linear | Mix | Cyclo-Asp at 8th position, cyclo-Lys at 12 position | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | >4 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [Ala15 ]Cyclo(Lys21 -Asp 25)GRF(1 -29)-NH2 | 29 | Free | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | >4 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [D-Ala2,Ala15]Cyclo(Lys21-Asp25)GRF(1-29)-NH2 | 29 | Free | Amidation | Linear | Mix | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | >4 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 1826667 | 1991 | [Asp8,Ala15]Cyclo(Asp8-Lys12)(Lys21-Asp25)GRF(1-29)-NH2 | 29 | Free | Amidation | Linear | L | None | Synthetic(GRF-1 analogs) | Release growth hormone | Not mentioned | 100 µg/ml | >4 | Porcine plasma proteases | HPLC | Porcine plasma | in vitro | None | None | Not reported | |||
| 2162275 | 1990 | VIP (Vasoactive intestinal peptide) | 28 | Acetylation | Amidation | Linear | L | None | Neuropeptide derived from Prepro-VIP | Vasodilator | Not mentioned | 5 pmol min-1 kg-1 | 0.8 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | It increase heart rate | |||
| 2162275 | 1990 | PHM (Peptide histidine methionine) | 27 | Free | Amidation | Linear | L | None | Peptide derived from Prepro-VIP | Vasodilator | Not mentioned | 5 pmol min-1 kg-1 | 6.5 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | It increase heart rate | |||
| 2896343 | 1988 | GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | L | None | Growth regulating factor | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 6.2 ±0.7 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 100% | |||
| 2896343 | 1988 | [D-Ala2]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 6.6 ±0.4 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 5146% | |||
| 2896343 | 1988 | [D-Asp3]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 5.9 ±0.8 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 670% | |||
| 2896343 | 1988 | lD-Asn8]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 6.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 221% | |||
| 2896343 | 1988 | [D-Tyr10]-GRF(1-29)-NH2 (Growth regulating factor) | 29 | Free | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 4.7 ±0.8 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 230% | |||
| 2896343 | 1988 | Ac-[D-Tyr1,D-AIa2]GRF(1-29)-NH2 (Growth regulating factor) | 29 | Acetylation | Amidation | Linear | Mix | None | GRF-1 analogs | Release growth hormone | Blood collected 1-90 minutes after peptide injection | 20μg/200μl | 7.4 ±0.5 | Rat plasma proteases | Radioimmunoassay | Rat plasma (i/v and s/c route of injection) | in vivo | None | None | Relative potency for GH releasing activity = 2817% | |||
| 2942845 | 1986 | ANF (Ser99-Tyr126) (Atrial natriuretic factor ) | 28 | Free | Free | Cyclic (C7-C23) | L | Radioiodinated peptide at Tyr | Atrial natriuretic factor derivative | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 5second-5 minutes after peptide injected | 60mg/kg | 16.8 ±0.9 | Rat plasma proteases | RP-HPLC | Male Sprague-Dawley rats plasma (Dose i/p injected) | in vivo | None | None | IC50=59pM, Inhibition of aldosterone production | |||
| 2942845 | 1986 | ANF (Arg101-Tyr126) (Atrial natriuretic factor ) | 26 | Free | Free | Cyclic (C5-C21) | L | Radioiodinated peptide at Tyr | Atrial natriuretic factor derivative | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 5second-5 minutes after peptide injected | 60mg/kg | 17.1 ±1.5 | Rat plasma proteases | RP-HPLC | Male Sprague-Dawley rats plasma (Dose i/p injected) | in vivo | None | None | IC50=204pM, Inhibition of aldosterone production | |||
| 2942845 | 1986 | ANF (Ser103-Tyr126) (Atrial natriuretic factor ) | 24 | Free | Free | Cyclic (C3-C19) | L | Radioiodinated peptide at Tyr | Atrial natriuretic factor derivative | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 5second-5 minutes after peptide injected | 60mg/kg | 22.0 ±4.5 | Rat plasma proteases | RP-HPLC | Male Sprague-Dawley rats plasma (Dose i/p injected) | in vivo | None | None | IC50=276pM, Inhibition of aldosterone production | |||
| 2942845 | 1986 | ANF (Ser99-Tyr126) (Atrial natriuretic factor ) | 28 | Free | Free | Cyclic (C7-C23) | L | Radioiodinated peptide at Tyr | Atrial natriuretic factor derivative | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 5second-5 minutes after peptide injected | 60mg/kg | 25.2 ±6.1 | Rat plasma proteases | RP-HPLC | Male Sprague-Dawley rats (nephrectomized rat) plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 2942845 | 1986 | ANF (Ser99-Tyr126) (Atrial natriuretic factor ) | 28 | Free | Free | Cyclic (C7-C23) | L | Radioiodinated peptide at Tyr | Atrial natriuretic factor derivative | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 5second-5 minutes after peptide injected | 60mg/kg | 16.3 ±1.2 | Rat plasma proteases | RP-HPLC | Male Sprague-Dawley rats (hepatectomized rat) plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 2942845 | 1986 | ANF (Ser99-Tyr126) (Atrial natriuretic factor ) | 28 | Free | Free | Cyclic (C7-C23) | L | Radioiodinated peptide at Tyr | Atrial natriuretic factor derivative | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 5second-5 minutes after peptide injected | 60mg/kg | 19.4 ±3.5 | Rat plasma proteases | RP-HPLC | Male Sprague-Dawley rats (both nephrectomized & hepatectomized rat) plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 2953516 | 1987 | rANP (Recombinant Atrial natriuretic peptide ) | 26 | Free | Free | Cyclic (C5-C21) | L | None | Atrial natriuretic factor | Natriuretic, diuretic and vasorelaxant peptide | Blood collected 0.2-2 hours after peptide injection | 1 μg/min dose | 4.5 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | ANP induced dose-related effects on systemic and renal hemodynamic, as well as electrolyte excretion | |||
| 1651738 | 1991 | alpha-ANP (alpha-atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | alpha-atrial natriuretic peptide | Natriuretic and vasodilator | Blood collected 30-60 minutes during and 5-20 minutes after peptide injection | 0.005 - 0.05 µg/kg/min in 25 mL normal saline infused over 1 h | 4.3 ±0.6 | Proteases from Human plasma(younger, 20-39 years old) | Radioimmunoassay | Human plasma(younger, 20-39 years old) | in vivo | None | None | Natriuresis (145 ±36 ν 142 ± 28 µMol/min) and urinary cGMP excretion (40.9 ± 6.7 nmol/h) | |||
| 1651738 | 1991 | alpha-ANP (alpha-atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | alpha-atrial natriuretic peptide | Natriuretic and vasodilator | Blood collected 30-60 minutes during and 5-20 minutes after peptide injection | 0.005 - 0.05 µg/kg/min in 25 mL normal saline infused over 1 h | 7.8 ±0.6 | Proteases from Human plasma(older, 65-83 years old) | Radioimmunoassay | Human plasma(older, 65-83 years old) | in vivo | None | None | Natriuresis 142 ± 28 µMol/min and urinary cGMP excretion 35.3 ± 4.1 | |||
| 1831249 | 1991 | ANP(99-126) (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Blood collected 2-20 minutes after peptide infused | 5pmol/kg | 4.8 ±0.8 | Proteases from Human plasma (Chronic renal diseases) | Radioimmunoassay | Human plasma (Chronic renal diseases) | in vivo | None | None | GFR and ERPF increased by a mean value of 23% and 27% respectively | |||
| 2156886 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 2 pmol/kg peptide infused | 3.1 | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide infused | 1.23 ±0.35 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide+ captoril(ACE inhibitor) infused | 6.99 ±0.34 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide+phosphoramidon, a specific E-24.11 inhibitor infused | 11.8 ±0.49 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 0.17-0.25 Mbeq peptide+phosphoramidon, a specific E-24.11 inhibitor +captoril(ACE inhibitor infused | 14.3 ±0.48 | Rat plasma proteases | HPLC | Rat plasma | in vivo | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide | 4.6 ±0.1 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide+ captoril(ACE inhibitor | 8.3 ±0.3 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide+phosphoramidon, a specific E-24.11 inhibitor infuse | 5.6 ±0.2 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2175178 | 1990 | Porcine 125I-BNP(1-26) | 26 | Free | Free | Cyclic (C4-C20) | L | Tyr is Iodinated (125I) | Porcine brain and heart | Natriuretic and vasodilator | Blood collected 2-270 minutes after peptide injection | 1.5 Kbeq peptide+phosphoramidon, a specific E-24.11 inhibitor +captoril(ACE inhibitor infused | 9.9 ±0.4 | Proteases from Rat serum | HPLC | Rat Serum | in vitro | None | None | PRA and Plasma aldosterone concentrations were suppressed 50 % and 30 % respectively by 2pmol/kg BNP | |||
| 2521208 | 1989 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic | Natriuretic and vasodilator | Not mentioned | Exogenously administered | 1.2 | Proteases from Rabbit plasma | Radioimmunoassay | Rabbit plasma | in vivo | None | None | Not mentioned | |||
| 2521208 | 1989 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic | Natriuretic and vasodilator | Not mentioned | Endoogenously administered | 3.2 | Proteases from Rabbit plasma | Radioimmunoassay | Rabbit plasma | in vivo | None | None | Not mentioned | |||
| 2866222 | 1985 | hGRF-1(1-29) (Human growth hormone-releasing factor) | 29 | Free | Amidation | Linear | L | None | Human growth hormone-releasing factor | Stimulates growth hormone release | Blood collected 2-60 minutes after peptide injection | 10 µg/200μ1 0.9% NaCl/0.5% Human Serum albumin, | 1.9 ±0.2 (alpha half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 2866222 | 1985 | hGRF-1(1-29) (Human growth hormone-releasing factor) | 29 | Free | Amidation | Linear | L | None | Human growth hormone-releasing factor | Stimulates growth hormone release | Blood collected 2-60 minutes after peptide injection | 10 µg/200μ1 0.9% NaCl/0.5% Human Serum albumin, | 10.4 ±0.2 (beta or elimination half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 1664804 | 1991 | Rat alpha-ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic and vasodilator | Blood samples collected at 0.5-10 minutes post peptide injection | 2 µg/150ul saline | 55 (t1/2 alpha or initial phase t1/2) | Proteases from Mice (WKY)plasma | Radioimmunoassay | (Dose i/v injected)Mice (WKY) plasma | in vivo | None | None | Urinary sodi µM excretion (uEq/min per kg)= 0.45 ± 0.10, mean arterial pressure (mmHg) = 129 ± 2, Urinary cGMP excretion (pmol/min) = 28.0 ±2.6 | |||
| 1664804 | 1991 | Rat alpha-ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Atrial natriuretic peptide | Natriuretic and vasodilator | Blood samples collected at 0.5-10 minutes post peptide injection | 2 µg/150ul saline | 4.03 (t 1/2 beta or 2nd phase t1/2) | Proteases from Mice (WKY)plasma | Radioimmunoassay | (Dose i/v injected)Mice (WKY) plasma | in vivo | None | None | Urinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.4 | |||
| 9234336 | 1994 | 131I-VIP (Vasoactive intestinal peptide) | 28 | Free | Amidation | Linear | L | Iodinated at Tyr | Neuropeptide | Anti-inflammatory neuropeptide | Blood sample collected after 2-60 minutes of peptide administeration | 250 µg (6MBq in 0.2mL) | 0.44 ±0.05 (elimination half life) | Proteases from rat blood | HPLC | (Dose i/v injected)Rat blood | in vivo | None | None | Not reported | |||
| 9234336 | 1994 | 131I-VIP (Vasoactive intestinal peptide) | 28 | Free | Amidation | Linear | L | Iodinated at Tyr | Neuropeptide | Anti-inflammatory neuropeptide | Organs are collected at 2-60 minutes after administration of drug (by killing organism) | 250 µg (6MBq in 0.2mL) | 2.3 ±0.8 (elimination half life) | Proteases from rat lung tissues | HPLC | (Dose i/v injected)Rat lung tissues | in vivo | None | None | Not reported | |||
| 8388403 | 1993 | ile 12-ANP (Atrial natriuretic peptide) | 26 | Free | Free | Cyclic (C5-C21) | L | None | Infusions of atrial natriuretic peptide | Natriuretic and vasodilator | Blood sample collected after 15-240 minutes after peptide administration | 1.5pmol/Kg/min dose of peptide | 4.1 ±0.4 | Proteases from Human plasma | Radioimmunoassay | Human plasma(elder men) | in vivo | None | None | It increases the cGMP approx 3 fold | |||
| 2945560 | 1986 | hANP (Human Atrial Natriuretic Peptide) | 28 | Free | Amidation | Cyclic (C7-C23) | L | None | Hormone secreted by heart muscle cells | Natriuretic and vasodilator | Not mentioned | 98.3 ± 44.6pg/ml | 5.65 | Proteases from Human plasma | Radioimmunoassay | Human plasma(bolus injection) | in vivo | None | None | Not reported | |||
| 18424366 | 2008 | GLP(7-34) (Glucagon like peptide) | 28 | Acetylation | Amidation | Linear | L | None | GLP-1 (Glucagon like peptide-1) analogue | Antihyperglycemic or incretin effect (Stimulate Insulin release in glucose dependent manner) | 37C for 2 hours | 200 µg/ml | >2 | DPP IV | MALDI-TOF-MS | Peptide in 0.01 M Na2HPO4 buffer | in vitro | None | None | In the DPP-IV-free rat pancreatic beta cell line RINm5F GLP-1-(7-34)-amide elevated cAMP production with an EC50 of about 40 nM | |||
| 18424366 | 2008 | GLP(7-34) (Glucagon like peptide) | 28 | Acetylation | Amidation | Linear | L | None | GLP-1 (Glucagon like peptide-1) analogue | Antihyperglycemic or incretin effect (Stimulate Insulin release in glucose dependent manner) | 37C for 2 hours | 200 µg/ml | ~34 | DPP IV | MALDI-TOF-MS | Peptide in 0.01 M Na2HPO4 buffer | in vitro | None | None | In the DPP-IV-free rat pancreatic beta cell line RINm5F GLP-1-(7-34)-amide elevated cAMP production with an EC50 of about 40 nM | |||
| 6361234 | 1983 | Porcine gastrin releasing peptide | 27 | Free | Amidation | Linear | L | None | Gastrin releasing peptide | Stimulates the release of Gastrin | Not reported | 5 pmol/kg . min for 30 min and a volume of 1 ml/min. | 3 | Calf blood proteases | Radioimmunoassay | Arterial blood sample of pedigree jersey calves | in vivo | 18185064 | None | Not mentioned | |||
| 10377427 | 1999 | ANP ( Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Cardiac atria | cardiovascular homeostasis | Blood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide | 0.2 µci/mouse of [125I]ANP | 1.44 ±0.05 | Npr3+/+ mice blood proteases | Radioimmunoassay | Npr3+/+ mice blood sample | in vivo | 6230082 | None | Blood pressure=118.7 ±1.9 mmHg | |||
| 10377427 | 2000 | ANP ( Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Cardiac atria | cardiovascular homeostasis | Blood was collected after 0.5, 1.5,2.5, 4, 8, and 16 min after administration of the labeled peptide | 0.2 µci/mouse of [125I]ANP | 2.4 ±0.08 | Npr3-/- mice blood proteases | Radioimmunoassay | Npr3-/- mice blood sample | in vivo | 6230082 | None | Blood pressure=110.4 ±2.3 mmHg | |||
| 2939312 | 1986 | α-hANP (Alpha human atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Human atrial extracts | Natriuretic and hypotensive actions | Venous samples were drawn at 1 mln intervals for 10 mlns after injectlon and then at 15 and 30 mlns. | 100 µg | 2.5 | Human blood proteases | Radioimmunoassay | Intravenous bolus injection of 100μg alpha human atrial natriuretic factor in human | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg | 21.6 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Male rat | in vivo | None | None | Platelet count increased from 1,504×103/mm3 to 2,262×103/mm3,Neutophil count increased from 941/mm3 to 19,802/mm3,Monocyte count increased from 160/mm3 to 7,917/mm3,Eosinophil count increased from 86/mm3 to 1067/mm3,Basophil count increased from 11/mm3 to 653/mm3,Lymphocyte count increased from 4,210/mm3 to 24,759/mm3,RBC count decreased form 7.05×106/mm3 to 5.56×106/mm3,Prothrombin time increased from 13.7 to 16.7 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg | 30.2 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Female rat | in vivo | None | None | Platelet count increased from 1,504×103/mm3 to 2,262×103/mm3,Neutophil count increased from 941/mm3 to 19,802/mm3,Monocyte count increased from 160/mm3 to 7,917/mm3,Eosinophil count increased from 86/mm3 to 1067/mm3,Basophil count increased from 11/mm3 to 653/mm3,Lymphocyte count increased from 4,210/mm3 to 24,759/mm3,RBC count decreased form 7.05×106/mm3 to 5.56×106/mm3,Prothrombin time increased from 13.7 to 16.7 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg | 23 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Male rat | in vivo | None | None | Platelet count increased from 1,504×103/mm3 to 2,243×103/mm3,Neutophil count increased from 941/mm3 to 18,870/mm3,Monocyte count increased from 160/mm3 to 6,790/mm3,Eosinophil count increased from 86/mm3 to 810/mm3,Basophil count increased from 11/mm3 to 329/mm3,Lymphocyte count increased from 4,210/mm3 to 24,874/mm3,RBC count decreased form 7.05×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 13.7 to 17.2 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg | 20.4 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Female rat | in vivo | None | None | Platelet count increased from 1,504×103/mm3 to 2,243×103/mm3,Neutophil count increased from 941/mm3 to 18,870/mm3,Monocyte count increased from 160/mm3 to 6,790/mm3,Eosinophil count increased from 86/mm3 to 810/mm3,Basophil count increased from 11/mm3 to 329/mm3,Lymphocyte count increased from 4,210/mm3 to 24,874/mm3,RBC count decreased form 7.05×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 13.7 to 17.2 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg | 18.2 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Male rat | in vivo | None | None | Platelet count increased from 1,504×103/mm3 to 2,304×103/mm3,Neutophil count increased from 941/mm3 to 27,439/mm3,Monocyte count increased from 160/mm3 to 8,246/mm3,Eosinophil count increased from 86/mm3 to 986/mm3,Basophil count increased from 11/mm3 to 863/mm3,Lymphocyte count increased from 4,210/mm3 to 27,439/mm3,RBC count decreased form 7.05×106/mm3 to 5.52×106/mm3,Prothrombin time increased from 13.7 to 17.5 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg | 19.4 | Rats blood proteases | Radioimmunoassay | Intravenous injection of the peptide in Hans Wistar Female rat | in vivo | None | None | Platelet count increased from 1,504×103/mm3 to 2,304×103/mm3,Neutophil count increased from 941/mm3 to 27,439/mm3,Monocyte count increased from 160/mm3 to 8,246/mm3,Eosinophil count increased from 86/mm3 to 986/mm3,Basophil count increased from 11/mm3 to 863/mm3,Lymphocyte count increased from 4,210/mm3 to 27,439/mm3,RBC count decreased form 7.05×106/mm3 to 5.52×106/mm3,Prothrombin time increased from 13.7 to 17.5 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 10μg/kg | 37 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 2μg/kg | 68 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 10μg/kg | 47 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 25μg/kg | 45 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 100μg/kg | 45 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 2μg/kg | 39 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | Not reported | 10μg/kg | 45 | Monkey blood proteases | Radioimmunoassay | Subcutaneous injection in cynomolgus monkeys | in vivo | None | None | Not mentioned | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 1 | 26.1 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 1 | 25.4 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 1 | 23.4 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 1 | 23.7 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 1 | 33.8 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 1 | 24.2 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 14 | 27.2 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 500μg/kg following dose 14 | 32.7 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 1,811×103/mm3,Neutophil count increased from 4,400/mm3 to 6,900/mm3,Monocyte count increased from 450/mm3 to 1,150/mm3,Eosinophil count increased from 150/mm3 to 450/mm3,Lymphocyte count increased from 5,900/mm3 to 9,400/mm3,RBC count decreased form 5.96×106/mm3 to 5.53×106/mm3,Prothrombin time increased from 19.8 to 21.2 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 14 | 44 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 1000μg/kg following dose 14 | 25.1 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,820×103/mm3,Neutophil count increased from 4,400/mm3 to 7,300/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 800/mm3,Lymphocyte count increased from 5,900/mm3 to 8,100/mm3,RBC count increased form 5.96×106/mm3 to 6.16×106/mm3,Prothrombin time increased from 19.8 to 21.7 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 14 | 39.3 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus male monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds. | |||
| 10606160 | 1999 | GW395058 | 29 | Pegylated with 20,000 mw PEG [CH30(CH2CH2O)nCH@CH2C=O] | Amidation | Linear (branched) | L | Npa-napthylalanine,Sar-sarcosine | AF15705(substituted thrombopoietin mimetic peptide) | Treatment of thrombocytopenia | 48 hours | 2000μg/kg following dose 14 | 31.3 | Monkey blood proteases | Radioimmunoassay | Intravenous injection in cynomolgus female monkey | in vivo | None | None | Platelet count increased from 381×103/mm3 to 2,405×103/mm3,Neutophil count increased from 4,400/mm3 to 5,700/mm3,Monocyte count increased from 450/mm3 to 1,550/mm3,Eosinophil count increased from 150/mm3 to 350/mm3,Lymphocyte count increased from 5,900/mm3 to 11,300/mm3,RBC count decreased form 5.96×106/mm3 to 5.87×106/mm3,Prothrombin time increased from 19.8 to 23.3 seconds. | |||
| 19023544 | 2008 | Tα1 (Thymosin α1) | 28 | Acetylation | Free | Linear | L | None | Component of thymosin fraction | Immunomodulator | Not mentioned | Not mentioned | 127 ±11 | Rabbit plasma proteases | HPLC | Heparinized rabbit plasma | in vitro | http://www.drugbank.ca/drugs/DB00111 | None | IL2 concentration in mouse serum:0.7pg/ml,macrophage clearance index(K value)=0.0165 ±0.0007,phagocytic index(α value=3.73 ±0.56. | |||
| 20382695 | 2010 | hGLP-1[7-36] (Human glucagon like peptide-1) | 30 | Free | Amidation | Linear | L | None | Incretin released by intestinal L cells | Metabolism regulation | 1 hour | 40 nm(1μg/μl upto 500μl) | 50 | Rat blood proteases | HPLC | Rat blood plasma | in vitro | http://www.drugbank.ca/drugs/DB00113 | None | cAMP stimulation,EC50=0.08nM | |||
| 20382695 | 2010 | Taspoglutide | 30 | Free | Amidation | Linear | L | Aib=α-aminoisobutyric acid replacing Ala8 and Gly35 of hGLP-1[7-36] | Novel analog of hGLP1 | Treatment of type 2 diabetes(clinical trials) | 1 hour | 40 nm(1μg/μl upto 500μl) | 9.8 | Rat blood proteases | HPLC | Rat blood plasma | in vitro | http://www.drugbank.ca/drugs/DB00114 | None | cAMP stimulation,EC50=0.06nM | |||
| 20687610 | 2010 | GLP-1 (glucagon like peptide-1) | 30 | Free | Free | Linear | L | None | Incretin released by intestinal L cells | Glucose dependent insulin secretion,promotion of insulin gene transcription,stimulation of β-cell proliferation and neogenesis, inhibition of β-cell apoptosis, and suppression of glucagon secretion. | 24 hours | 100μM | 2.0 ±0.2 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00115 | None | EC50=4.6nM,pEC50=8.3 ±0.08 | |||
| 20687610 | 2010 | c[E16,K20]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16 and K20) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 1.8 ±0.3 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00116 | None | EC50=3.8nM,pEC50=8.4 ±0.06 | |||
| 20687610 | 2010 | c[E18,K22]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E18 and K22) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 2.1 ±0.4 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00117 | None | EC50=0.6nM,pEC50=9.2 ±0.11 | |||
| 20687610 | 2010 | c[E22,K26]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E22 and K26) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 2.9 ±0.8 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00118 | None | EC50=2.8nM,pEC50=8.3 ±0.03 | |||
| 20687610 | 2010 | c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E30 and K34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 3.3 ±0.4 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00119 | None | EC50=5.3nM,pEC50=8.6 ±0.13 | |||
| 20687610 | 2010 | c[E16,K20]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20 and E30-K34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 3.1 ±0.1 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00120 | None | EC50=3.3nM,pEC50=8.5 ±0.04 | |||
| 20687610 | 2010 | c[K16,E20]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between K16-E20 and K30-E34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 2.9 ±0.1 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00121 | None | EC50=7.0nM,pEC50=8.2 ±0.11 | |||
| 20687610 | 2010 | c[E18,K22]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E18-K22 and E30-K34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 3.6 ±0.2 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00122 | None | EC50=1.9nM,pEC50=8.7 ±0.14 | |||
| 20687610 | 2010 | c[K18,E22]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between K18-E22 and K30-E34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 4.1 ±0.2 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00123 | None | EC50=1.0nM,pEC50=9.0 ±0.09 | |||
| 20687610 | 2010 | c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E22-K26 and E30-K34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 6.0 ±1.8 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00124 | None | EC50=1.6nM,pEC50=8.8 ±0.11 | |||
| 20687610 | 2010 | c[K22,E26]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between K22-E26 and K30-E34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 7.3 ±0.4 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00125 | None | EC50=2.2nM,pEC50=8.7 ±0.14 | |||
| 20687610 | 2010 | c[E16,K20]-c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | >24 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00126 | None | EC50=1.8nM,pEC50=8.7 ±0.09 | |||
| 20687610 | 2010 | c[E16,K20]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K35) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 4.6 ±0.7 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00127 | None | EC50=3.8nM,pEC50=8.4 ±0.06 | |||
| 20687610 | 2010 | c[E18,K22]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K36) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 3.2 ±0.4 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00128 | None | EC50=0.6nM,pEC50=9.2 ±0.11 | |||
| 20687610 | 2010 | c[E22,K26]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K37) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 10 ±3.5 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00129 | None | EC50=2.8nM,pEC50=8.3 ±0.03 | |||
| 20687610 | 2010 | c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K38) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 6.9 ±0.5 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00130 | None | EC50=5.3nM,pEC50=8.6 ±0.13 | |||
| 20687610 | 2010 | c[E16,K20]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K39) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 6.9 ±0.1 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00131 | None | EC50=3.3nM,pEC50=8.5 ±0.04 | |||
| 20687610 | 2010 | c[K16,E20]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K40) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 1.7 ±5.0 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00132 | None | EC50=7.0nM,pEC50=8.2 ±0.11 | |||
| 20687610 | 2010 | c[E18,K22]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K41) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | >96 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00133 | None | EC50=1.9nM,pEC50=8.7 ±0.14 | |||
| 20687610 | 2010 | c[K18,E22]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K42) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 18 ±2.2 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00134 | None | EC50=1.0nM,pEC50=9.0 ±0.09 | |||
| 20687610 | 2010 | c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K43) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 3.5 ±0.9 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00135 | None | EC50=1.6nM,pEC50=8.8 ±0.11 | |||
| 20687610 | 2010 | c[K22,E26]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K44) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 1.2 ±0.3 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00136 | None | EC50=2.2nM,pEC50=8.7 ±0.14 | |||
| 20687610 | 2010 | c[E16,K20]-c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K45) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | >96 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00137 | None | EC50=1.8nM,pEC50=8.7 ±0.09 | |||
| 7962302 | 1994 | GHRH | 29 | Free | Amidation | Linear | L | None | Synthetic | Growth hormone-releasing hormone (GHRH) stimulates growth hormone (GH) gene transcription, synthesis, and secretion of growth hormone via growth hormone-releasing hormone receptor (GHRH-R) | Blood samples were obtained at 5 min intervals for measurement of serum GH concentrations and at the | Intravenous dose of 1 µg/kg followed by a 15 min infusion of saline in human subjects. | 18.5 ±0.8 | Human blood proteases | Immunoradiometric assay (IRMA) | Human blood | in vivo | http://www.drugbank.ca/drugs/DB00189 | None | Not reported | |||
| 17204551 | 2007 | Rat Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 0 - 60 minutes | 10 μg | 22 ±2 | Protease from rat plasma | Radioimmunoassay | Intravenous injection of peptide into Sprague Dawley rats | in vivo | None | None | Co-administration of obestatin with ghrelin inhibited food intake. | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 19 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 53 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + P8340 protease inhibitor cocktail | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 39 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + EDTA | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 20.5 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + Soybean trypsin inhibitor | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 20.5 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + APMSF | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 24 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + 1,10-Phenanthrolin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 20 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + Captopril | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 17 | Proteases from Crude brain homogenate of mouse | HPLC | Crude brain homogenate of mouse + Chymostatin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 27 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 75.5 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + P8340 protease inhibitor cocktail | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 62 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + EDTA | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 38.5 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + Soybean trypsin inhibitor | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 16 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate+ APMSF | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 28 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + 1,10-Phenanthrolin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 28 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate + Captopril | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 19422857 | 2009 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 120 minutes | 90 μg | 29.5 | Proteases from Membrane brain Homogenate | HPLC | Membrane brain Homogenate+ Chymostatin | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | No suppressive effects of obestatin on food or water intake were observed | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.4 | 90 μg | 42.2 [40.5, 44.0] | Proteases from mouse plasma | HPLC, LC-UV/MS | Mouse plasma | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.5 | 90 μg | 12.6 [11.4, 14.1] | Proteases from Mouse liver homogenate | HPLC, LC-UV/MS | Mouse liver homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.6 | 90 μg | 30.0 [27.8, 32.6] | Proteases from Mouse stomach homogenate | HPLC, LC-UV/MS | Mouse stomach homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mouse Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin from mouse | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.7 | 90 μg | 138.0 [114.8, 172.9] | Proteases from Mouse kidney membrane homogenate | HPLC, LC-UV/MS | Mouse kidney membrane homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.8 | 90 μg | 65.1 [59.6, 71.7] | Proteases from mouse plasma | HPLC, LC-UV/MS | Mouse plasma | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.9 | 90 μg | 95.8 [89.4, 103.3] | Proteases from mouse plasma + protease inhibitor cocktai | HPLC, LC-UV/MS | Mouse plasma with protease inhibitor cocktail | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.10 | 90 μg | 13.3 [12.7, 14.0] | Proteases from mouse liver homogenate | HPLC, LC-UV/MS | Mouse liver homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.11 | 90 μg | 28.0 [25.8, 30.5] | Proteases from mouse liver homogenate+protease inhibitor cocktai | HPLC, LC-UV/MS | Mouse liver homogenate with protease inhibitor cocktail | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Human Obestatin | 23 | Free | Amidation | Linear | L | None | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.12 | 90 μg | 67.7 [61.7, 75.1] | Proteases from mouse membrane homogenate | HPLC, LC-UV/MS | Mouse kidney membrane homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 18602197 | 2008 | Mono-iodinated human obestatin | 23 | Free | Amidation | Linear | L | Iodination at tyr16 | Proghrelin frpm human | Energy balance, Inhibit Ghrelin-induced Growth Hormone secretion | 37 °C for 0 - 60 minutes, pH 7.12 | 90 μg | 15.1 [9.1, 45.0] | Proteases from Mouse liver homogenate | HPLC, LC-UV/MS | Mouse liver homogenate | in vitro | http://www.sigmaaldrich.com/catalog/product/sigma/ | None | Not reported | |||
| 38613996 | 2024 | PepH3-vCPP2319 5 | 27 | Free | Amidation | Linear | L | Ahx links two peptide | Synthetic chimeric peptide of PepH3 and vCPP2319 | Anticancer | At different time points (0, 1, 5, 10, 30, 60, 120, and 360 min), 120 µL aliquots were collected and incubated with equal volume of 96% ethanol for 30 min at 4⁰C | 1 mM | 125.20 ± 34.21 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | IC50 = 5.20±1.04 for TNBC MDA-MB-231 Monolayer | |||
| 38554247 | 2024 | MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | None | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | 8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38554247 | 2024 | K2-MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | Alkyl chain conjugated with Lys2 side chain | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | Remained intact for 78.68% after 24 Hours | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38554247 | 2024 | K2-K4-MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | Alkyl chain conjugated with Lys2, Lys4 side chain | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | Remained intact for 75.61% after 24 Hours | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 38236561 | 2024 | Cotadutide | 29 | Free | Free | Linear | L | palm-Glu-OH conjugated at Lys9 side chain | Synthetic | Dual GLP-1 and Glucagon (GCG) Receptor agonist | N.A. | 20 to 600 μg | 13.3 | N.A. | N.A. | N.A. | In Vivo | None | None | N.A. | |||
| 37818589 | 2024 | ΔTRTX-Ac1 | 28 | Free | Free | Cyclic (C2-C9-C18-C19-C22-C27 form LCK Loop) | L | None | From venom of the Mexican Blond tarantula spider Aphonopelma chalcodes | Antidiabetes | Blood withdrawn by cardiac puncture at0, 2, 4, 6, 8 and 12 h post-administration | 10 mg/kg | 2.17 | C57Bl/6 Male Mice Plasma Protease | Mass spectrometry | C57BL/6 male mice plasma | In Vivo | https://dom-pubs.pericles-prod.literatumonline.com/doi/10.1111/dom.15319 | None | The activity value of ΔTRTX-Ac1 alone shows minimal influence on reducing circulating glucose levels, with glucose levels remaining at 23.7 ± 3.1 mmol/L in high-fat-fed/streptozotocin (HFF/STZ) mice | |||
| 37818589 | 2024 | ΔTRTX-Ac1 | 28 | Free | Free | Cyclic (C2-C9-C18-C19-C22-C27 form LCK Loop) | L | None | From venom of the Mexican Blond tarantula spider Aphonopelma chalcodes | Antidiabetes | Blood withdrawn by cardiac puncture at 0, 2, 4, 6, 8 and 12 h post-administration | 10 mg/kg | 2.16 | C57Bl/6 Male Mice Pancreas Protease | Mass spectrometry | C57BL/6 male mice pancreas | In Vivo | https://dom-pubs.pericles-prod.literatumonline.com/doi/10.1111/dom.15319 | None | The activity value of ΔTRTX-Ac1 alone shows minimal influence on reducing circulating glucose levels, with glucose levels remaining at 23.7 ± 3.1 mmol/L in high-fat-fed/streptozotocin (HFF/STZ) mice | |||
| 37390979 | 2023 | Stapled secretin | 27 | Free | Amidation | Cyclic (E16-K20 Lactam Bridge) | L | E16, K20 modification | Human secretin modified analog | Secretin receptor agonist | N.A. | 30 nmol/kg | N.A. | Male NMRI mice plasma protease | Mass spectrometry | Male NMRI mice plasma (Non fasted) | In Vivo | None | None | EC50 = 1172 nM for native secretin on murine adipocytes | |||
| 37047588 | 2023 | B7-33 | 27 | Free | Free | Linear | L | None | Derived as a single-chain peptidomimetic of the B-chain of H2 relaxin | Treatment of Acute Cardiac Failure | A total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min) | 400 µg/mL | 6 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | HEK-7BP Binding B.S.A. Free Eu-H2 pKi = 7.28 ± 0.11 | |||
| 37047588 | 2023 | AcK(PalmGlu)-PEG12-B7-33 | 27 | Ac modifed Lysine in Palmitic fatty acid linked with B7-33 using PEG linker | Free | Linear | L | None | B7-33 analog | Treatment of Acute Cardiac Failure | A total of 80 µL of samples was removed at various time points (0 min, 30 min, 60 min, 120 min, 240 min, and 480 min) | 400 µg/mL | 60 | Human serum protease | RP-HPLC | Human serum | In Vitro | None | None | HEK-7BP Binding B.S.A. Free Eu-H2 pKi =7.52 ± 0.13 | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 66 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | (Prodrugs of Onc72) MIC values >50 μmol L−1 on E.coli BW25113 | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 66 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | Prodrugs Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 66 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | 5 kDa thiol-PEG: Reduced cell viability to ≈89% for both HepG2 and HEK293 cell lines | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | (Prodrugs of Onc72) MIC values >50 μmol L−1 on E.coli BW25113 | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | Prodrugs Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | 20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Synthetic | Antimicrobial | 0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates | 31.5 μmol/L | 8 | Mouse serum protease | Serum stability assay | Mouse serum | In Vivo | None | None | 5 kDa thiol-PEG: Reduced cell viability to ≈89% for both HepG2 and HEK293 cell lines | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Synthetic | Antimicrobial | 0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates | 31.5 μmol/L | 14 | Mouse serum protease | Serum stability assay | Mouse serum | In Vivo | None | None | 20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines | |||
| N.A. | 2023 | SEQ ID NO 1 | 28 | Free | Free | Linear | L | None | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 0.2 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 0.83 | |||
| N.A. | 2023 | SEQ ID NO 2 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >19 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 1.9 | |||
| N.A. | 2023 | SEQ ID NO 23 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 103 | |||
| N.A. | 2023 | SEQ ID NO 24 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 54.5 | |||
| N.A. | 2023 | SEQ ID NO 25 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, NMeS = N-Methyl-L-Serine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 17 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 70.5 | |||
| N.A. | 2023 | SEQ ID NO 26 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, Deg = Di-ethyl glycine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 138 | |||
| N.A. | 2023 | SEQ ID NO 27 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, Tie = L-te/t-butyl-glycine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 61.8 | |||
| N.A. | 2023 | SEQ ID NO 28 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, Aib = 2-aminoisobutyric acid at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 72.4 | |||
| N.A. | 2023 | SEQ ID NO 29 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 36.6 | |||
| N.A. | 2023 | SEQ ID NO 30 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 56.5 | |||
| N.A. | 2023 | SEQ ID NO 31 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, NMeS = N- methyl-L-serine at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 12 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 50.3 | |||
| N.A. | 2023 | SEQ ID NO 32 | 28 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 2 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 142 | |||
| N.A. | 2023 | SEQ ID NO 33 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3, 1Nal = 3-(l-naphthyl)-L-alanine at position 4 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 61 | |||
| N.A. | 2023 | SEQ ID NO 34 | 29 | Free | Free | Linear | L | NMeS = N- methyl-L-serineat position 2,X = Octanoyl-Dpr at position 3, Nal = 3-(l-naphthyl)-L-alanine at position 4 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 25 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 27.2 | |||
| N.A. | 2023 | SEQ ID NO 35 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | 63 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 76.7 | |||
| N.A. | 2023 | SEQ ID NO 36 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 44.5 | |||
| N.A. | 2023 | SEQ ID NO 37 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 27.5 | |||
| N.A. | 2023 | SEQ ID NO 38 | 29 | Free | Free | Linear | L | X = Octanoyl-Dpr at position 3 | Human Ghrelin Analog | Ghrelin Receptor Agonist | Solutions were incubated at 37 C for 60, 120 and 180 Minutes | 1 mg/ml | >58 | Plasma protease | LC-MS | Diluted plasma | In Vitro | None | EP 2023054305 W | EC50(nM) = 56.1 | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration | 260 μg/kg | 54.5 | Mouse serum protease | Modified ELISA | Mouse serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration | 260 μg/kg | 32.3 | Mouse serum protease | Modified ELISA | Mouse serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration | 260 μg/kg | 66.4 ± 33.0 | Rats serum protease | Modified ELISA | Rats serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration | 260 μg/kg | 40.9 ± 17.7 | Rats serum protease | Modified ELISA | Rats serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 0.25, 0.5, 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after IV administration | 52 μg/kg | 24.9 ± 2.2 | Dogs serum protease | Modified ELISA | Dogs serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36997003 | 2023 | HM15136 | 30 | IgG Fc linked at N terminus through MAL-PEG-ALD linker | Free | Cyclic (lactam bridge between E16-K20) | L | Aib2 modification | Synthetic | Treatment of Hyperinsulinemic Hypoglycemia | Blood (0.3 mL) was collected from the retro-orbital plexus at 1, 4, 8, 24, 48, 72, 96, 120, 144, 168, 192, 216, 240, 264, 288, 312, and 336 h after SC administration | 52 μg/kg | 26.6 ± 1.5 | Dogs serum protease | Modified ELISA | Dogs serum | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | EC50 of HM15136 was 0.024 ± 0.006 nM while that of native glucagon was 0.003 ± 0.001 nM for hGCGR | |||
| 36443381 | 2022 | SA10SC-RLX | 25 | Acetylation | Amidation | Linear | L | Attachment of a lipid moiety (C18-γ-Glu-PEG2) at K25 position, Aib, Nle,acetylation of Lys10 | Synthetic | Treatment for Chronic Fibrotic and Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48 and 72 h (IV route) and 0.25, 0.5, 1, 2, 4, 8, 12, 24, 48 and 72 h (SC route) | 1 mg/kg | 4 (Terminal Half Life) | Rats plasma protease | LC-HRMS | Rats plasma | In Vivo | None | None | EC50 (nM) = 0.8 for EA.hy926_hRXFP1 | |||
| 36443381 | 2022 | SA10SC-RLX | 25 | Acetylation | Amidation | Linear | L | Attachment of a lipid moiety (C18-γ-Glu-PEG2) at K34 position, Aib, Nle | Synthetic | Treatment for Chronic Fibrotic and Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 2, 4, 6, 8, 24, 48, 72, 96 and 168 h (IV route) and 0.25, 0.5, 2, 4, 6, 8, 24, 48, 72, 96 and 168 h (SC route) | 1 mg/kg | 7 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50 (nM) = 0.8 for EA.hy926_hRXFP1 | |||
| 35414877 | 2022 | B_3.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 347 | |||
| 35414877 | 2022 | B_3.2 | 25 | Acetylation | Amidation, FLAG tag | Linear | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | ~2 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 7890 | |||
| 35414877 | 2022 | B_1275 | 25 | Acetylation | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | ~3.5 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 2076 | |||
| 35414877 | 2022 | B_1275.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 1209 | |||
| 35414877 | 2022 | B_1275.2 | 25 | Acetylation | Amidation, FLAG tag | Linear | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | ~2 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 8336 | |||
| 35414877 | 2022 | B_1275.4 | 25 | Acetylation | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | Stable | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | None | None | IC50(nM) = 826 | |||
| 35414877 | 2022 | B_3.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 585 (Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 347 | |||
| 35414877 | 2022 | B_1275.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 643(Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 1209 | |||
| 35414877 | 2022 | B_1275.4 | 25 | Acetylation | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 3.767 (Elimination half life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 826 | |||
| 35113575 | 2022 | TT1-IP peptide | 27 | Free | Amidation | Cyclic (C-C Disulfide Bond) | L | Conjugation of TT1 and IP proteins which is linked by Ahx | TT1 and IP fusion protein | Antitumor (Effect on TPP-IPs on Cll xenograft models) | periods of time (0, 1, 6, and 24 h) | 5 mg/kg | 40% of the peptide was recovered after 6 hours incubation | Human serum protease | MS using MALDI-TOF | Human serum | In Vitro | None | None | The average survival for TT1-IP and LinTT1-IP treated groups was 19 days (the survival range for TT1-IP group was 17-23 days and for LinTT1-IP group was 13-25 days) and for the control group 16 days (range of 14-20 days) | |||
| 35113575 | 2022 | TT1-IP peptide | 27 | Free | Amidation | Cyclic (C-C Disulfide Bond) | L | Conjugation of TT1 and IP proteins which is linked by Ahx | TT1 and IP fusion protein | Antitumor (Effect on TPP-IPs on Cll xenograft models) | plasma collected at 10, 20, 30, 45, 60, 120 and 360 min | 5 mg/kg | 28 (Terminal Half Life) | BALB/c mice plasma protease | HPLC-MS | Balb/c mice plasma | In Vivo | None | None | The average survival for TT1-IP and LinTT1-IP treated groups was 19 days (the survival range for TT1-IP group was 17-23 days and for LinTT1-IP group was 13-25 days) and for the control group 16 days (range of 14-20 days) | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 1 mg | 0.25 ± 0.02 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 4 mg | 0.36 ± 0.04 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 10 mg | 0.45 ± 0.05 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment of Ischemic Stroke | Blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 20 mg | 0.55 ± 0.07 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 30 mg | 0.70 ± 0.08 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 45 mg | 0.73 ± 0.05 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34954052 | 2022 | SY-007 | 24 | Free | Free | Linear | L | None | Neuropeptide | Treatment Of Ischemic Stroke | blood samples were collected for determinationsof SY-007 at pre-dose (within 0.5 h prior to dosing) and at 5, 10, 15, 20,30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of the intravenous infusion | 60 mg | 0.78 ± 0.06 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.05 mg/kg | 7.37 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.125 mg/kg | 10.5 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.25 mg/kg | 19.94 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.25 mg/kg | 13.16 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.5 mg/kg | 16.2 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 1 mg/kg | 19.97 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| 34217775 | 2022 | FE 992326 | 30 | Free | Amidation | Linear | L | None | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 2, 6, 10, 15, 20, 30, 45, 60, 90, 120 min | 0.3 mg/kg | 6.5 ± 1.8 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| 34217775 | 2022 | FE 992326 | 30 | Free | Amidation | Linear | L | None | Derived from CGRP | Treatment of Acute Episodic Migraine | Blood sample was collected at 5, 10, 20, 30, 45, 60, 90, 120, 180, 240, 300 min | 1 mg/kg | 11 ± 8.4 | Male SD rats plasma protease | LC-MS/MS | Male SD rats plasma | In Vivo | None | None | Rat (%Plasma Protein Binding) = 9 ± 3, Human(%Plasma Protein Binding) = 17 ± 2 for FE 205030 | |||
| N.A. | 2022 | 12kD-PEG-e9-XPLGLAG-r9-k(cy5) | 25 | 12 KDa PEG | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 6 nmol | 20 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Alb-e9-XPLGLAG-r9-k(cy5) | 25 | Alb=albumin | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Alb=albumin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 4.8 nmol | 3 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Dex-e9-XPLGLAG-r9-k(cy5) | 25 | Dextran | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Dex=Dextran, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 5 nmol | 6 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| 34122400 | 2021 | CATH2 | 27 | Free | Free | Linear | L | None | Cationic chicken heterophil-derived peptide | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 302 ± 34.5 | Human serum protease | HPLC | Human serum | In Vitro | None | None | The cytotoxicity of CbTP was lower than that of parental peptide CATH2 | |||
| 36133017 | 2021 | Fab–CKP-NLP | 30 | Free | Free | Linear | L | Fab conjugation, Lys1 fatty acid conjugation (Palm) | Synthetic | Platform for potential delivery of peptide like drug candidates | 37 °C for 24 hour | N.A. | 75% Remained Intact | N.A. | SEC | N.A. | In Vitro | None | None | N.A. | |||
| 36133017 | 2021 | CKP-NLP | 30 | Free | Free | Linear | L | AF488 labeled , Lys1 fatty acid conjugation (Palm) | Synthetic | Platform for potential delivery of peptide like drug candidates | 37 °C | N.A. | 1 | N.A. | SEC | N.A. | In Vitro | None | None | N.A. | |||
| 33813091 | 2021 | FITC-TPP1 | 21 | FITC labelled | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding | 4 mg/kg | <10 (Blood Clearance Half Life) | Mice blood plasma protease | Fluorescence spectrometry | Mice blood plasma | In Vivo | None | None | N.A. | |||
| 33813091 | 2021 | TPP1 (SPIO NP@M-P) | 21 | FITC labelled | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding | 4 mg/kg | 6 (Blood Clearance Half Life) | Mice blood plasma protease | Fluorescence spectrometry | Mice blood plasma | In Vivo | None | None | N.A. | |||
| 33706686 | 2021 | TB59-2 | 30 | GLP-1 7–36 peptide is linked to the light chain N-terminal of the TB01-2 antibody via a (G4S)x3 linker | Free | Linear | L | None | Synthetic | Antidiabetes | 250 ul blood samples were collected via jugular vein cannula at these time points: pre-dose, 0.0833, 0.25, 0.5, 1, 2, 4, 8, 24, 48, 72, 96, 168, 240 and 336 hours post dose. | 10 mg/kg | >2 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | TB59-2 binds specifically to the GLP-1 R with an EC50 of 15.5 nM, TB-59-2 is a potent agonist in the cAMP assay with a similar EC50 as the GLP-1 7–36 peptide, TB59-2 can also induce the β-arrestin recruitment in GLP-1 R expression cells | |||
| 33672039 | 2021 | GLP1_8A37C-HSA | 30 | Free | HSA | Linear | L | Substituition of amino acid A at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 3.3 (T1/2a) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50=185 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33672039 | 2021 | GLP1_8A37C-HSA | 30 | Free | HSA | Linear | L | Substituition of amino acid A at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 7.1 (T1/2b) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50=185 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 1 mg | 0.26 ± 0.02 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 4 mg | 0.36 ± 0.04 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 10 mg | 0.45 ± 0.05 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 20 mg | 0.55 ± 0.07 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | Plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 30 mg | 0.70 ± 0.08 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 45 mg | 0.73 ± 0.05 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33607700 | 2021 | Tat-K13 | 24 | Free | Free | Linear | L | None | Synthetic | Treatment of Ischemic Stroke | plasma samples were taken at pre-dose, 5, 10, 15, 20, 30, 45 min, and 1, 1.5, 2, 3, 4, 5, 6 h after the beginning of intravenous infusion | 60 mg | 0.78 ± 0.06 | Human plasma protease | UPLC–MS/MS | Human plasma | In Vivo | None | None | N.A. | |||
| 33555858 | 2021 | B10-33 (Cpd 58) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with(-(γE)3-C16), Aib | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 4.3 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 17.6 ± 8.1(97%) in OVCAR5 cells | |||
| 33555858 | 2021 | B10-33 (Cpd 59) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C16), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 8.9 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 3.6 ± 2.0 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 60(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C16), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 6.4 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 3.2 ± 2.1 (74%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 61(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 4.8 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 1.0 ± 0.9 (79%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 62(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 4.3 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.6 ± 0.4 (95%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 63(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C16), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 5.7 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 1.0 ± 0.6 (80%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 64(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 3.9 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.2 ± 0.1 (89%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 65(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 3.4 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.1 ± 0.1 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 66(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C18), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 3.96 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 0.4 ± 0.2 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 67(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C16-OH), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | N.A. | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 809 ± 20 (70%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 68(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C18-OH), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | N.A. | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 368 ± 76 (75%) in OVCAR5 cells | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 4.01 ± 1.19 | Human male blood protease | Two site ELISA | Human male blood sample | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 3.94 ± 1.10 | Human female blood protease | Two site ELISA | Human female blood sample | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 33135460 | 2021 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | 1 day | 0.65 ng/kg/min from 1100 (120 min) till the end of the study at 1400 (300 min) | 3.96 ± 1.12 | Human blood protease (All) | Two site ELISA | Human blood sample (All) | In Vivo | pdb id: 1GCN | None | N.A. | |||
| 32778037 | 2021 | [14C]-WLBU2 | 24 | C14 labeling | Free | Linear | L | None | Synthetic | Antimicrobial | N.A. | 15 mg/kg | 22 (Radioactivity Half Life) | CD1 female mice plasma protease | Radiochromatography | CD1 female mice plasma | In Vivo | None | None | N.A. | |||
| 33374407 | 2020 | Tα1-PAS | 28 | Free | PAS#1(600) | Linear | L | None | Synthetic | Antiviral, Anticancer | Blood samples (100 µL) were taken from 5 animals each at various time points | 3.4 mg/kg | 15.7 ± 0.8 (Τ1/2a) | Rats plasma protease | sandwich ELISA | Rats plasma | In Vivo | UniprotKb ID: P06454 | None | N.A. | |||
| 33374407 | 2020 | Tα1-PAS | 28 | Free | PAS#1(600) | Linear | L | None | Synthetic | Antiviral, Anticancer | Blood samples (100 µL) were taken from 5 animals each at various time points | 3.4 mg/kg | 15.9 ± 0.9 (Τ1/2b ) | Rats plasma protease | sandwich ELISA | Rats plasma | In Vivo | UniprotKb ID: P06454 | None | N.A. | |||
| 33310780 | 2020 | NYBSP-C | 30 | Acetylation | Amidation | Linear | L | None | Derived from ACE2 | Antiviral | 0, 10, 30, 60, and 120 min | 1 mM | >289 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | IC50 >27.7 μM in HT1080/ACE2 cells | |||
| 32808659 | 2020 | ELA-21 | 21 | Free | Free | Linear | L | None | produced endogenously in the body | Anti-Heart Failure Activity | Blood was collected at time points of 0, 3, 10, 30 and 90 mins, and 4.5, 12 and 24 h | 100 mg/kg | ∼13 | Mice plasma protease | Western blotting | Mice plasma | In Vivo | https://sci-hub.se/10.1016/j.ijcard.2019.04.089 | None | EC50 = 0.6 nM (cAMP supression) | |||
| 32608185 | 2020 | 125I-M-E5 | 22 | Free | Tyrosine (Y) residue was added to E5 sequence and 125I was added | Linear | L | None | Synthetic | Anticancer (Treatment of Acute Myeloid Leukemia) | N.A. | 50 µg/g | 14.53 ± 6.04 | Rats plasma protease | Gamma counter | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4196105/#sec10 | None | The cells that were pretreated with M-E5 showed significantly reduced migration compared with the CXCL12 group, and the inhibitory rate was 82.9% for the leukemic cells separated from the spleen and 59.1% for those separated from the BM | |||
| 32506501 | 2020 | gamma3-MSH | 26 | Free | Free | Linear | L | None | Derived from POMC | Antiinflammatory and Cardiovascular function | 37 °C | 2 µM | 2.62 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 9.37E-10 for MC1R-g3-MSH | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(16,23) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifications include (R-octenyl alanine) and (Bis-pentenyl glycine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 120 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(23,30) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifications include (S-octenyl alanine) and (Bis-pentenyl glycine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 30 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | stitched GLP-1 | 30 | Free | Free | Cyclic (I, I+7 Stitched GLP) | L | None | Stitched GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | 220 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | GLP-1 | 30 | Free | Free | Linear | L | None | Unstapled GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 1 mM | <10 | Proteinase K | LC-MS/MS | DMSO + buffer consisting of 50 mM Tris HCl, pH 7.4 | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | GLP-1 | 30 | Free | Free | Linear | L | None | Unstapled GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 14 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(16,23,30) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifcations include (R-octenyl alanine) and (bis-pentenyl glycine) and (S-octenyl alanine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 320 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32235388 | 2020 | cTxIB-5 | 21 | Linker (GGAAG) | Free | Cyclic (C2-C8, C3-C16 Disulfide Bond And Linker-C16 Bond) | L | None | α-conotoxin TxIB analogue | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Slightly lower stability than TXIB | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | Inhibition of cTxIB-5 is 42% | |||
| 32235388 | 2020 | cTxIB-6 | 22 | Linker (GAGAAG) | Free | Cyclic (C2-C8, C3-C16 Disulfide Bond And Linker-C16 Bond) | L | None | α-conotoxin TxIB analogue | Blocks the Α6/Α3Β2Β3 Nicotinic Acetylcholine Receptors | Aliquots of each peptide were taken out at 0, 12, 24, 36, and 48 h. | 100 μM | Slightly lower stability than TXIB | Male AB human serum protease | RP-UPLC | Male AB human serum | In Vitro | None | None | Inhibition of cTxIB-6 is 48% | |||
| 32133341 | 2020 | Apamin based analogs 3 | 25 | Free | Free | Cyclic (C1-C11, C3-C15) | L | None | Apamin based analogs | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 12.8 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.65 ± 0.18 | |||
| 32133341 | 2020 | Apamin based analogs 9 | 21 | Free | Amidation | Cyclic(C1-C11, C3-C15 ) | L | None | Apamin based analogs | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 6.6 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.76 ± 0.03 | |||
| 32133341 | 2020 | R3 B1-27 | 27 | Free | Free | Linear | L | None | Native relaxin-3 | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 3.1 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 5.91 ± 0.21 | |||
| 32133341 | 2020 | R3 B1-22R | 23 | Free | Amidation | Linear | L | None | Synthetic | Relaxin-3 antagonist | N.A. | 0.05 μg/μl | 4 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.76 ± 0.03 | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hour after sHDL administration | 50 mg/kg | 2.1 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A-P | 23 | Free | Proline addition at C terminal | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hour after sHDL administration | 50 mg/kg | 4.2 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3.3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3.3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31776208 | 2020 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected at pre-dose and 0.25, 0.5, 1, 2, 4, 8, and 24 hours after sHDL administration | 50 mg/kg | 3.3 | Rats serum protease | LC-MS | SD rats serum | In Vivo | None | None | The binding of a peptide to phospholipid was also confirmed by increased helicity of 22A, 21A, and 22A-P in sHDL particles (94%, 91%, and 82%) relative to the free peptide (77%, 79%, and 77%) as measured by CD | |||
| 31805154 | 2019 | CP24 | 24 | Free | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 Fusion Inhibitory Peptide) | Serial blood samples were collected from monkeys that received CP24 or IBP-CP24 before injection and at 2, 4, 6, 24, 72 and 144 h post-injection | 10 mg/kg | 1.69 | Rhesus monkeys plasma protease | Sandwich ELISA | Rhesus monkeys plasma | In Vivo | None | None | IC50(nM) = 0.8±0.2 for CP24 in virus subtype A (92UG029) | |||
| 31341417 | 2019 | PSG4R | 25 | hIgG4 Fc conjugation through linker AEAAAKEAAAKEAAAKEAAAKA | Free | Cyclic (Two Disulfide Bonds Arranged As Cys2-Cys10 And Cys4-Cys8 In Ap25) | L | None | RGD-4C and endostatin fragment ES-2 fusion protein derived | Antitumor | 100 to 200 µL orbital blood samples were taken at 5 min before drug administration or 0 min, 5 min, 10 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 18 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, 216 h after drug administration | 5 mg/kg | 56.27 (Elimination Half Life) | Rats plasma protease | Indirect competitive ELISA | Rats plasma | In Vivo | None | None | IC50 = 1.82 ± 0.25 μmol/L for PSG4R on HUVEC proliferation | |||
| 31341417 | 2019 | AP25 | 25 | Free | Free | Cyclic (Two Disulfide Bonds Arranged As Cys2-Cys10 And Cys4-Cys8) | L | None | Synthetic | Antitumor | 100 to 200 µL orbital blood samples were taken at 5 min before drug administration or 0 min, 5 min, 10 min, 30 min, 1 h, 2 h, 4 h, 6 h, 8 h, 12 h, 18 h, 24 h, 36 h, 48 h, 72 h, 96 h, 120 h, 144 h, 168 h, 192 h, 216 h after drug administration | 5 mg/kg | 50 (Elimination Half Life) | Rats plasma protease | ELISA | rats plasma | In Vivo | None | None | IC50 = 1.60 ± 0.15μmol/L for AP25 on HUVEC proliferation | |||
| 31443263 | 2019 | LTP | 29 | Free | TP5 conjugated with LTP(13-36) at C terminus | Linear | L | None | Synthetic | Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions) | 37 °C | N.A. | 240.03 ± 55.14 | Rats plasma proteaes | HPLC | 10 μg/mL rats plasma | In Vitro | None | None | Among the peptides, LTP exhibited a lower cytotoxicity than LL-37 and TP5. In addition, LTP exhibited no significant cytotoxicity towards RAW264.7 cells, even at the highest concentration of 60 µg/mL | |||
| 31040673 | 2019 | ES2-AF | 21 | Free | VEGFR1-selective hexapeptide (GNQWFI, AF) ,amidation | Linear | L | FITC labeled | Synthetic | Antiangiogenic | Blood samples were collected through the fundus venous plexus, 0.5–24 hours after administration | 20 mg/kg | 2.34 ± 0.43 | Mice plasma protease | Fluorescence spectrometry | Mice plasma | In Vivo | None | None | The inhibitory rates of ES2-AF and CS-ES2-AF were similar (5 μg/mL–100 μg/mL), which indicated that the activity of ES2-AF was similar to CS-ES2-AF at relatively low concentrations | |||
| 31040673 | 2019 | CS-ES2-AF | 21 | CS (chondroitin sulfate) | VEGFR1-selective hexapeptide (GNQWFI, AF) ,amidation | Linear | L | FITC labeled | Synthetic | Antiangiogenic | Blood samples were collected through the fundus venous plexus, 0.5–24 hours after administration | 20 mg/kg | 7.57 ± 2.65 | Mice plasma protease | Fluorescence spectrometry | Mice plasma | In Vivo | None | None | The inhibitory rates of ES2-AF and CS-ES2-AF were similar (5 μg/mL–100 μg/mL), which indicated that the activity of ES2-AF was similar to CS-ES2-AF at relatively low concentrations | |||
| 30938069 | 2019 | ESA-CJC-1295 | 30 | Free | (DAC) maleimidopropionic acid conjugated with Equine serum albumin | Cyclic | Mix | None | Synthetic | Stimulates The Production Of Growth Hormone (Gh) From The Pituitary Gland | One mL aliquots were removed for analysis at 0, 24, 48, 72 and 96 hours at 4°C | 700 pg/mL | 20 | Equine plasma protease | Mass spectrometry | Equine plasma | In Vivo | None | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes | 200 pmol/kg | 4.3 ± 1.2 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection | 200 pmol/kg | 92 ± 21 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 1, 2, 5, 15, 30, 60, 90, and 120 minutes | 2000 pmol/kg | 6.9 ± 2.5 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30817059 | 2019 | Porcine C‐Peptide | 29 | Free | Free | Linear | L | None | Released from the pancreatic beta cells when proinsulin is processed into insulin and C-peptide | Used as marker of insulin production | Blood samples (200 μL each) were collected through the catheter at 5, 15, 30, 60, 90 and 120 minutes after intraperitoneal injection | 2000 pmol/kg | 53 ± 14 (Terminal Elimination Half Life) | Rats plasma protease | ELISA | Rats plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)41064-8/pdf | None | N.A. | |||
| 30794654 | 2019 | CNP(1–22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | CNP C terminal cleavage | Improved endochondral ossification and accelerated bone growth in mice | N.A. | 20 nmol/kg | 1.42 ± 0.45 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | CNP(1–22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | CNP C terminal cleavage | Improved Endochondral Ossification And Accelerated Bone Growth In Mice | N.A. | 50 nmol/kg | 10.0 ± 5.0 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30521347 | 2019 | cot-APTEDB-SN38 | 26 | Free | Free | Cyclic (2 Trp-Trp Bond) | L | Lys15 linked with (Cot-Mal-PEG4-Ala-SN38) | Linker is Mal-PEG4 | Anticancer | Those mice were sacrificed at 0.08, 0.5, 1, 3, 6, 12, 24, and 48 h post injection | 1 mg/kg | 1.36 | ICR mice plasma protease | HPLC | ICR mice plasma | In Vivo | https://sci-hub.st/10.1016/j.jconrel.2012.08.029 | None | HC[cot-APTEDB−SN38/Abcot] at an SN38/kg dose-equivalent of 2 mg effectively suppressed tumor growth and showed much greater antitumor activity (49.8% inhibition) than both cotAPTEDB-SN38 alone (23.9% inhibition) and CPT-11 (10.6% inhibition) | |||
| 33224505 | 2019 | AR-Bi@SiO2-Gd/DOX NPs | 23 | Free | C-Terminal End Of The Ar Peptide Was Added With An Nh2-Rich Linker (GGGGKKKK) | Linear | L | None | Synthetic | Antitumor (Tumor homing ) | N.A. | N.A. | 104.5 (Tumor Retention Half Life) | N.A. | ICP-MS | N.A. | In Vivo | None | None | N.A. | |||
| 30165332 | 2018 | DV1 | 21 | Free | Amidation | Linear | D | All D-amino acids | Synthetic | CXCR4 antagonist | Blood samples were collected into heparin-coated polypropylene centrifuge tubes at 0, 5, 10, 15, 30 min and 1, 2, 4, 6, 8, 12, 24, 36 and 48 h after the dose | 10 mg/kg | 8.7 ± 2.4 | Rats plasma protease | HPLC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30161002 | 2018 | P16 | 21 | Free | Free | Linear | L | None | TNF-a cleaved fragment | Antitumor | Orbital blood samples were collected from 3 mice at different time points (0, 0.25, 0.5, 1, 2, 4, 8, 12, 16, 24, and 48 h) | 5 mg/kg | 0.07 | BALB/c mice plasma protease | LC-MS | BALB/c mice plasma | In Vivo | None | None | N.A. | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 1.7 (T1/2 Initial Phase) | Rats plasma protease | LC-MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 0.97 (T1/2 Initial Phase) | Rats plasma protease | LC-MS | Rats plasma volume reduced to 12.5 ml | In Vitro | None | None | N.A. | |||
| 29958697 | 2018 | 125I-TLQP-21 | 21 | 125I labelled | Free | Linear | L | None | Derived from the proteolytic cleavage of the 617-aa VGF | Isoproterenol stimulated lipolysis | At the time points of 0 min, 10 min, 30 min, and 60 min, aliquots of the incubated solutions were withdrawn (15uL) | 1 mM | 110 (T1/2 Terminal Phase) | Rats plasma protease | LC-MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 30 μg | 11.43 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 100 μg | 12.07 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 150 μg | 10.97 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 300 μg | 9.54 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29799205 | 2018 | 4a | 29 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 17.4 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.29 ± 0.04 | |||
| 29799205 | 2018 | 4b | 29 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 27.7 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.97 ± 0.11 | |||
| 29799205 | 2018 | 4c | 29 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 37.7 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 1.49 ± 0.13 | |||
| 29799205 | 2018 | 4d | 29 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 20.2 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.49 ± 0.07 | |||
| 29799205 | 2018 | 4e | 29 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 29.4 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 1.68 ± 0.18 | |||
| 29799205 | 2018 | 4f | 29 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 37.3 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) =6.35 ± 0.39 | |||
| 29673717 | 2018 | I-1 | 30 | Free | Amidation | Linear | L | Cys17-Gly8-GLP-1(7-36) modification and fatty acid modification through Mal referred to as X1 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50(pM) = 5.6 ± 1.1 | |||
| 29673717 | 2018 | I-2 | 30 | Free | Amidation | Linear | L | Cys17-Gly8-GLP-1(7-36) modification and fatty acid modification through Mal referred to as X2 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50(pM) = 14.3 ± 2.0 | |||
| 29673717 | 2018 | I-3 | 30 | Free | Amidation | Linear | L | Cys17-Gly8-GLP-1(7-36) modification and fatty acid modification through Mal referred to as X3 | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | More Stable Than Ex-4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50(pM) = 26.3 ± 2.5 | |||
| 29617109 | 2018 | RNP-DFO | 30 | Free | PLGA linked through mPEG | Linear | L | None | Synthetic | Treatment of Parkinson in mice | Blood samples were harvested from the tail vein at 0.08, 0.5, 1, 2, 4, 6, 12, and 24 h post-dosing | 50 mg/kg | More Stable | Rats plasma protease | HPLC | Rats plasma | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 4.588 | Rats serum protease | LC-MS | Rats serum after 50 mg/kg sHDL | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 4.25 | Rats serum protease | LC-MS | Rats serum after 2.5 mg/kg sHDL-PEG2k | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 7.14 | Rats serum protease | LC-MS | Rats serum after 5 mg/kg sHDL-PEG2k | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 5.05 | Rats serum protease | LC-MS | Rats serum after 2.5 mg/kg sHDL-PEG5k | In Vivo | None | None | N.A. | |||
| 28948296 | 2018 | GIP(3-30)NH2 | 27 | Free | Amidation | Linear | L | None | GIP analogue | GIP receptor antagonist | Blood samples were drawn 30, 15 and 0 min before and 20, 25, 30, 40, 50, 60, 67, 70, 75, 80, 95 and 125 min after the start of the GIP(3-30)NH2 infusion | 800 pmol/kg/min | 7.6 ± 1.4 (Elimination Half Life) | Human plasma protease | RIA | Human plasma | In Vivo | None | None | IC50 value of 87.6 nmol/l | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local muscle relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.25 mg/kg | 0.3 (Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local muscle relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.5 mg/kg | 0.68 (Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local Muscle Relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.25 mg/kg | 0.26(Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29316656 | 2018 | [125I]-Az | 21 | Free | Free | Linear | L | 125I labeld at His9 | Derived from Azemiops feae (Fea's viper) | Local muscle relaxant | Animal blood samples were taken from the orbital sinus 5, 15, 30, 60 min and 1, 2, 4 and 24 h after [125I]-Az administration | 0.5 mg/kg | 0.29(Excretion Half Life) | ICR mice blood protease | Radioactivity assay | ICR mice blood | In Vivo | None | None | LD50 of Az (0.51 mg/kg) | |||
| 29263923 | 2017 | FITC-conjugated E5 | 22 | FITC conjugation | Free | Linear | L | None | Synthetic | Inhibit Breast Tumor Progression | N.A. | 40 mg/kg | ~10 | Mouse serum protease | Fluorescence assay | Mouse serum | In Vivo | None | None | E5 (0.1 μM) had high affinity towards 4T1 cells and HUVECs | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 1.96 ± 0.05 | Rats plasma protease | RIA | Rats plasma without NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 9.94 ± 1.40 | Rats plasma protease | RIA | Rats plasma with NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28899838 | 2017 | CNP(1-22) | 22 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | Produced from recombinant DNA in Escherichia coli | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 10 nmol/kg | 4.34 ± 0.20 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28714475 | 2017 | tagPK128 | 22 | tag | Free | Bicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit plasma kallikrein | N.A. | 0.5 mg/kg | 0.9 ± 0.2 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin | |||
| 28714475 | 2017 | tagPK128 | 22 | tag | Free | Bicyclic(C9-C15,C15-C21 Disulfide Bond In Pk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit plasma kallikrein | N.A. | 0.5 mg/kg | 2.9 ± 0.7 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin | |||
| 28714475 | 2017 | tagUK18 | 24 | tag | Free | Bicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit urokinase | N.A. | 0.5 mg/kg | 1.0 ± 0.1 (T1/2a) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 780±110 for rat albumin | |||
| 28714475 | 2017 | tagUK18 | 24 | tag | Free | Bicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit urokinase | N.A. | 0.5 mg/kg | 7.4 ± 0.2 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 780±110 for rat albumin | |||
| 28668697 | 2017 | 7b | 29 | Free | Free | Linear | L | X2 = Structure given in paper, n= 40 | Derived from Xenopus GLP-1 | Antidiabetes | Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h | 50 nmol | 2.78 ± 0.14 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 1.4 ± 0.2 for peptide 7 (potency on the cloned human GLP-1 receptor) | |||
| 28668697 | 2017 | 7c | 29 | Free | Free | Linear | L | X3= Structure given in paper, n = 108 | Derived from Xenopus GLP-1 | Antidiabetes | Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h | 50 nmol | 5.67 ± 0.30 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 1.4 ± 0.2 for peptide 7 (potency on the cloned human GLP-1 receptor) | |||
| 28619366 | 2017 | BPI-3016 | 30 | Free | Free | Linear | L | substituting –NHCO– amide bond of Ala2 with –CH(CF3)NH– to form (A'), Lys20 conjugation with C18, K34R modification | hGLP-1 analogs | Antidiabetes | Blood samples collected at −2 (pre-administration), 2, 8, 22, 46, 94, 118, 142, and 166 h after administration | 0.2 mg/kg | 95 ± 20 | Diabetic cynomoglus monkeys plasma protease | electrospray ionization LC–MS/MS | Diabetic cynomoglus monkeys plasma | In Vivo | None | None | Single subcutaneous injection of 0.4 mg/kg BPI-3016 significantly lowered the fasting glucose level at 46 h after administration | |||
| 28606508 | 2017 | SAPSP-Dox | 21 | Dox = Doxorubicin, Cys incorporation for linking | Amidation | Linear | L | None | SAPSP peptide | Anticancer | 37 °C | 0.1 mM | 9.58 | Fetal Bovine Serum protease | RP-HPLC | Fetal Bovine Serum | In Vitro | None | None | IC50 (microM) = 1.19±0.13 against MCF-7 cells | |||
| 28575099 | 2017 | AAYR-Onc112 | 23 | AAYR | Amidation | Linear | Mix | None | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Low Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28575099 | 2017 | LVPR-Onc112 | 23 | LVPR | Amidation | Linear | Mix | None | Analog of Oncopeltus | Antibacterial | Aliquots (20 or 40 μL) taken after 0 and 60 min (0, 10 and 30 min for Api88) | 31.5 μmol/L | Low Stable | Mouse blood/plasma/serum protease | RP-HPLC | Mouse blood/plasma/serum | In Vitro | None | None | N.A. | |||
| 28494253 | 2017 | Peptide 23 | 21 | 111In-DTPA-Gly = diethylenetriaminepentaacetic acid | Free | Linear | L | X1=Asn, X2=Leu, X3=Lys,X4 = Thr, Biotinylated Lysine | A20FMDV2 analogue | Antitumor | After 24 hrs at 37 ◦C | 7.5 MBq | 60% Stable | Human blood plasma protease | Radio-HPLC | Human blood plasma | In Vitro | None | None | Affinity for peptide 23 = 1.28 ± 0.23 | |||
| 28097629 | 2017 | TP508 | 23 | Free | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 13.7 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG5k-TP508 | 23 | PEG5K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 11.5 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG20k-Cys14-TP508 | 23 | Free | Amidation | Linear | L | PEGylation at Cys14 through Mal-modified PEG20K, TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | Molar equivalent of 5 mg/mL TP508 | 70 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG20k-TP508 | 23 | PEG20K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | 2.16 mM | 93 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 28097629 | 2017 | PEG30k-TP508 | 23 | PEG30K | Amidation | Linear | L | TAMRA-labeled | Synthetic | Treatment of Diabetic Foot Ulcers | N.A. | Molar equivalent of 1 mg/mL TP508 | 258 | Male CD1 mice plasma protease | Fluorescence assay | Male CD1 mice plasma | In Vivo | None | None | N.A. | |||
| 27881716 | 2017 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 3.81 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 142.81 | |||
| 27881716 | 2017 | 22A | 22 | Free | Free | Linear | L | None | Synthetic | Treatment of Cardiovascular Diseases | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 4.43 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 142.81 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 6.27 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 53.77 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 4.14 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL)= 47.63 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 150 mg/kg | 2.57 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 53.77 | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 150 mg/kg | 2.74 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL)= 47.63 | |||
| 27689406 | 2017 | Glucagon | 29 | Free | Free | Linear | L | None | Produced by the alpha cells of the pancreas | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 3.2 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | None | None | N.A. | |||
| 27539157 | 2017 | Anti‐VEGF PCCs Bi‐LV | 23 | X1 = biotin-PEG3 label | lfreW = D and L -amino acids | Cyclic | Mix | Tz4 = triazole linker | Synthetic | In vivo imaging probe and an Anti‐PA peptide | Blood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min | 1 mg/kg | 7 (Elimination Half Life) | Mice plasma protease | LC‐MS/MS assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 27539157 | 2017 | Anti‐VEGF PCCs Tri‐LV | 28 | X1 = biotin-PEG3 label | eeird = D-amino acids | Cyclic | Mix | Tz4 = triazole linker | Synthetic | In vivo imaging probe and an Anti‐PA peptide | Blood was drawn from each of three animals at the following time points: 3, 10, 30, 60, 120, 240, 360, 1,440 min | 1 mg/kg | 36 (Elimination Half Life) | Mice plasma protease | LC‐MS/MS assay | Mice plasma | In Vivo | None | None | IC50 = 2.6 ± 0.5 nM | |||
| 28714475 | 2017 | tagPK128 | 22 | Tag | Free | Bicyclic (C2-C8,C8-C14 Disulfide Bond In Pk128) | L | Lys4 conjugated with Palm | Synthetic | Inhibit plasma kallikrein | Probes were taken at different time points (5 min, 0.5, 1, 2, 4, 8, 24 and 48 h) at 37 C , diluted to 3 mM (urokinase inhibitor) or 0.75 mM (plasma kallikrein inhibitor) with assay buffer (10 mM TrisCl, pH 7.4, 150 mM NaCl, 10 mM MgCl2, 1 mM CaCl2, 0.01% v/v Tween-20, and 0.1% (w/v) casein) | 20 microM | >48 (Activity Half Life) | Human plasma protease | N.A. | Human plasma | In Vitro | None | None | Albumin binding (Kd) (nM) = 720±90 for rat albumin for tagPK128 | |||
| 27804918 | 2016 | APTEDB–SN38 | 26 | Free | Free | Cyclic (2 Trp-Trp Bond) | L | Ala-modified SN38 (Cys-Mal-PEG4-Ala-SN38) linked with Cys-modified APT EDB through Lys15 | Linker is Mal-PEG4 | Anticancer | At different times (0.08, 0.5, 1, 3, 6, 12 h) after injection | 1 mg/kg | 1.77 | Mice plasma protease | HPLC | Mice plasma | In Vivo | https://sci-hub.st/10.1016/j.jconrel.2012.08.029 | None | IC50 = 472.6 nM | |||
| 27364558 | 2016 | Biotinylated SSTN(IGF1R) | 28 | Free | Free | Linear | L | Biotinylation | Mouse derived | Dually Attack MM Tumor Cell Survival And Tumor Angiogenesis | terminally bled at 0, 0.1, 0.3, 1, 3, 6, 12 and 24 hr post-injection | 0.365 mg/kg | 27 | Female BALB/c mice serum | IR scanning using anti-biotin antibody | Female BALB/c mice serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3651771/ | None | The growth of human CAG, RPMI-8226, KMS-12, U266, MM.1R and the mouse P3X63Ag8 myeloma cells was significantly reduced by a three-day treatment with 30 μM SSTNIGF1R | |||
| 27243004 | 2016 | Api794 | 22 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (WO)3 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 311 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) = 0.28 ± 0.03 in HEK293 | |||
| 27243004 | 2016 | Api796 | 22 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (IO)3 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 249 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) > 0.6 in HEK293 | |||
| 26673564 | 2016 | H3 | 30 | Free | Free | Linear | L | None | Histone 3 | Structural role | preincubated for 1 h | 3.0 μM | 9.63 (Activity Half Life) | N.A. | Resorufin-derived absorbance assay | Assay buffer containing 25 μM peptide substrate, 50 μM Amplex Red, and 1 unit/mL HRP and H3 | In Vitro | None | None | IC50(nM) =153 | |||
| 106-160-175-860-210 | 2016 | P28 | 28 | acetylate | amidated | Cyclic | L | enzymatically cyclized | P. aeruginosa azurin | Therapeutic | 72 hours | 10 μl | Increased | NA | MTT | Human Cancer Cells | in vivo | https://lens.org/106-160-175-860-210 | US 9,434,770 B2 | N.A. | |||
| 030-841-916-119-277 | 2017 | GLP-1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 20 | NA | cAMP assay | rabbits | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP-1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 24 | NA | cAMP assay | rabbits | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 12.9 | NA | cAMP assay | rats | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 030-841-916-119-277 | 2017 | GLP1 | 30 | Free | Fusion with ELP | Linear | L | None | synthetic | agonists | 15-60 min | 300-500 mg/dl | 8.6 | NA | cAMP assay | rats | in vivo | https://lens.org/030-841-916-119-277 | US 9821036 B2 | NA | |||
| 179-033-965-606-598 | 2017 | insulin | 21 | Free | Free | Linear | L | None | Human | NA | 0.02 mg/kg | Less than 20K-PEG-insulin | NA | enzyme immunoassay | Rat Blood | in vivo | https://lens.org/179-033-965-606-598 | US 9616109 B2 | EC50 = 7.9ng/ml | ||||
| 025-814-764-427-267 | 2017 | PB1120 | 28 | VIP with a Met | ELP(1-120) | linear | L | None | Synthetic | NA | 30 min | 3 mg/kg | 45.8 | NA | cell-based bioassay | Monkeys | in vivo/vitro | https://www.lens.org/lens/patent/025-814-764-427-267 | US 9,700,598 B2 | NA | |||
| 092-334-515-289-964 | 2017 | PB1120 | 29 | VIP | ELP (1-120) | Linear | L | None | NA | anti-hypertensive | NA | NA | 45.8 | NA | NA | Monkeys | in vitro | https://lens.org/092-334-515-289-964 | US 9561262 B2 | NA |