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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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 15322125 | 2004 | Aβ(1 €“ 40) | 40 | Free | Free | Linear | L | None | Derivative of human A precursor protein APP770 | Neurodegenerative | 120 minutes | 2x107 cpm of 125I-Aβ42 peptide | 2.4 | Mouse plasma proteases | Radioactivity measured by scintillation counter | Intravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samples | in vivo | None | None | Neurodegeneration caused by oligomerization | |||
| 12859428 | 2003 | BNP-32 | 32 | Free | Free | Linear | L | None | Canine B-type natriuretic peptide | Diuretic, natriuretic, hypotensive and smooth muscle relaxant activities | Not reported | Not mentioned | 1.57 ± 0.14 | Dog plasma proteases | Radioimmunoassay | Injected intravenously into dogs | in vivo | None | None | 44.7 ±0.3% RBC during BNP-32 infusion | |||
| 11054637 | 2000 | Human brain natriuretic peptide (hBNP) | 32 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 12.7 | Sheep blood proteases | HPLC | Infused in pulmonary artery of sheep | in vivo | 2136732 | None | Kd=8pM for receptor binding | |||
| 11054637 | 2000 | Human brain natriuretic peptide (hBNP) | 32 | Free | Free | Linear | L | None | Cardiac origin | Regulation of extracellular fluid and blood pressure homeostasis | Not mentioned | Not mentioned | 3.1 | Human blood proteases | HPLC | Injected in humans | in vivo | 2136732 | None | Kd=8pM for receptor binding | |||
| 21244372 | 2010 | Exenatide | 39 | Free | Amidation | Linear | L | None | Synthetic version of the 39-amino-acid peptide originally isolated from the saliva of the gila monster lizard | Regulate blood glucose | Not mentioned | 5 µg ·mL-1 ·kg-1 | 1.5 to 4 | Rat plasma proteases | ELISA | Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1 | in vivo | None | None | EC50 of 2.3nM for stimulation of intracellular cAMP in PC12 cells | |||
| 21244372 | 2010 | PB-105 (ExC39) | 39 | Free | Amidation | Linear | L | None | Analogue of exenatide | Regulate blood glucose | Not mentioned | 5 µg ·mL-1 ·kg-1 | 2.9 ±0.1 | Rat plasma proteases | ELISA | Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1 | in vivo | None | None | EC50 of 1.4nM for stimulation of intracellular cAMP in PC12 cells | |||
| 21244372 | 2010 | PB-110 (ExC39PEG5kDa) | 39 | Free | Amidation | Linear | L | 5 kDa PEG at Cys at 39th position | Analogue of exenatide | Regulate blood glucose | Not mentioned | 5 µg ·mL-1 ·kg-1 | 6.1 ±0.8 | Rat plasma proteases | ELISA | Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1 | in vivo | None | None | EC50 of 1.3nM for stimulation of intracellular cAMP in PC12 cells | |||
| 21244372 | 2010 | PB-106 (ExC39PEG20kDa) | 39 | Free | Amidation | Linear | L | 20 kDa PEG at Cys at 39th position | Analogue of exenatide | Regulate blood glucose | Not mentioned | 5 µg ·mL-1 ·kg-1 | 49.4 ±7.7 | Rat plasma proteases | ELISA | Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1 | in vivo | None | None | EC50 of 1.2nM for stimulation of intracellular cAMP in PC12 cells | |||
| 21244372 | 2010 | PB-107 (ExC39PEG30kDa) | 39 | Free | Amidation | Linear | L | 30 kDa PEG at Cys at 39th position | Analogue of exenatide | Regulate blood glucose | Not mentioned | 5 µg ·mL-1 ·kg-1 | 70.5 ±2.6 | Rat plasma proteases | ELISA | Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1 | in vivo | None | None | EC50 of 14.2nM for stimulation of intracellular cAMP in PC12 cells | |||
| 21244372 | 2010 | PB-108 (ExC39PEG40kDa) | 39 | Free | Amidation | Linear | L | 40 kDa PEG at Cys at 39th position | Analogue of exenatide | Regulate blood glucose | Not mentioned | 5 µg ·mL-1 ·kg-1 | 76.4 ±7.4 | Rat plasma proteases | ELISA | Intravenously injected into Sprague-Dawley rats at a dose of 5 µg ·mL-1 ·kg-1 | in vivo | None | None | EC50 of 114.1nM for stimulation of intracellular cAMP in PC12 cells | |||
| 12047915 | 2002 | LY315902 | 35 | 2-indolyl-propionyl | Free | Linear | L | Oct-octanoic moiety | Glucagon-like peptide-1 analogue | Insulinotropic and glucagonostatic | Not mentioned | Not mentioned | 1.1 | Canine plasma protease | Radioimmunoassay | Canine plasma after subcutaneous injection of 100 µg/kg | in vivo | 9232514 | None | Plasma insulin 255 pmol/l on intravenous infusion of 20 pmol/kg/min of LY315902 | |||
| 17292977 | 2007 | AC3174 | 39 | Free | Amidation | Linear | L | None | Analog of exendin-4 | Regulates blood glucose | 5 hours | Not mentioned | >5 | Human plasma proteases | LC/MS | Human plasma | in vitro | None | None | IC50=0.66 ±0.13nM for binding to GLP-1 receptor | |||
| 17292977 | 2007 | AC3174 | 39 | Free | Amidation | Linear | L | None | Analog of exendin-4 | Regulates blood glucose | Not mentioned | Not mentioned | 42 ±3.4 | Rat plasma proteases | ELISA | Subcutaneously administion of 10 µg/kg dose to Sprague Dawley rats | in vivo | None | None | ED50=1.2 µg/kg for glucose lowering in db/db mice | |||
| 17292977 | 2007 | AC3174 | 39 | Free | Amidation | Linear | L | None | Analog of exendin-4 | Regulates blood glucose | Not mentioned | Not mentioned | 43 ±4.0 | Rat plasma proteases | ELISA | Subcutaneously administion of 100 µg/kg dose to Sprague Dawley rats | in vivo | None | None | ED50=1.3 µg/kg for glucose lowering in C57BL/6 mice | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(6 €“28) | 35 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 11.7 ±3.4 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.5x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(8 €“28) | 33 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 11.1 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.4x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(10 €“28) | 31 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.6x10-10nM for GPR38 agonist activity | |||
| 17107718 | 2006 | Glucagon-like peptide-2 (GLP-2) | 33 | Free | Free | Linear | L | None | Posttranslational processing of proglucagon | Stimulate intestinal growth | Not mentioned | Not mentioned | 6.8 ±0.8 | Pig plasma proteases | ELISA | Infused into blood of pigs | in vivo | None | None | Not reported | |||
| 17107718 | 2006 | Glucagon-like peptide-2 (GLP-2) | 33 | Free | Free | Linear | L | None | Posttranslational processing of proglucagon | Stimulate intestinal growth | Not mentioned | Not mentioned | 9.9 ±0.8 | Pig plasma proteases with valine-pyrrolidide (DPP-IV inhibitor) | ELISA | Infused into blood of pigs | in vivo | None | None | Not reported | |||
| 659633 | 1978 | C-peptide | 31 | Free | Free | Linear | L | None | Proinsulin | Not mentioned | Not reported | 0.75pmol/ml | 33.5(mean) | Not mentioned | Single-dose injection technique | 6 Normal human male blood plasma sample | in vivo | None | None | Not mentioned | |||
| 659633 | 1978 | C-peptide | 31 | Free | Free | Linear | L | None | Proinsulin | Not mentioned | Not reported | 0.9pmol/ml | 42.5(mean) | Not mentioned | Single-dose injection technique | 7 Diabetic human male blood plasma sample | in vivo | None | None | Not mentioned | |||
| 15882144 | 2005 | Ucn1 (urocortin 1) | 40 | Free | Free | Linear | L | None | Urocortin 1 | Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetite | Not reported | 50 μg | 54 ±3 | Human blood proteases | Not mentioned | Human blood plasma(Male patients with stable congestive heart failure) (Intravenous injection) | in vivo | None | None | Not given | |||
| 15882144 | 2005 | Ucn1 (urocortin 1) | 40 | Free | Free | Linear | L | None | Urocortin 1 | Coronary and peripheral vasodilatation, stimulation of cardiac natriuretic peptide secretion,stress and inflammatory responses, suppression of appetite | Not reported | 50 μg | 52 ±3 | Human blood proteases | Not mentioned | Human blood plasma (Normal humans) (Intravenous) | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 5.6 ±0.45 | Human blood proteases | Not mentioned | Human plasma of patients with mild, stable heart failure | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 11 ±1.3 | Human blood proteases | Not mentioned | Human plasma of patients with mild, stable heart failure given infusion of metoprolol | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 5.7 ±0.8 | Human blood proteases | Not mentioned | Human plasma (Normal humans) | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 6.6 ±1.3 | Human blood proteases | Not mentioned | Human plasma (Normal humans given infusion of metoprolol) | in vivo | None | None | Not given | |||
| 17266646 | 2007 | Exendin-4 | 39 | Free | Free | Linear | L | None | Salivary secretions of the lizard Heloderma suspectum | Exhibits potent anti-diabetic or glucoregulatory activities | Not reported | 100μg/ml | 9.57 | Not mentioned | RP-HPLC and MS-TOF | Human blood plasma | in vitro | None | None | Not given | |||
| 17479256 | 2007 | BNP | 32 | Free | Free | Linear | L | None | Synthetic peptide | Vasodilator | Not reported | 0.01 μg/kg per minute | 12.1 ±3.0 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not given | |||
| 17537541 | 2007 | IK312532 | 31 | Free | Free | Linear | L | None | Synthetic peptide | VIP analogue | Not reported | Ki=1.36 ±0.29 nM | 4.73 | Not mentioned | Not mentioned | Rat lung alveolar L2 cells | in vitro | None | None | Not given | |||
| 17640899 | 2007 | ENF (T-20) | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.006 µg/ml against IIIB virus virus | |||
| 17640899 | 2007 | ENF (T-20) | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.050 µg/ml against 098 virus virus | |||
| 17640899 | 2007 | ENF (T-20) | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.526 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | ENF (T-20) | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=54.958 µg/ml against 098-T1249 virus virus | |||
| 17640899 | 2007 | ENF (T-20) | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=47.822 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-1249 | 39 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.003 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-1249 | 39 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.013 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-1249 | 39 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.022 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-1249 | 39 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.363 µg/ml against 098-T1249 virus virus | |||
| 17640899 | 2007 | T-1249 | 39 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=8.140 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.008 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.033 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.060 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.151 µg/ml against 098-T1249 virus virus | |||
| 17640899 | 2007 | T-651 | 36 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 0.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=7.599 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-2410 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.008 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-2410 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.032 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-2410 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.039 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-2410 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.137 µg/ml against 098-T1249 virus virus | |||
| 17640899 | 2007 | T-2410 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=4.975 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-290676 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.006 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-290676 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.013 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-290676 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.022 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-290676 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.072 µg/ml against 098-T1249 virus virus | |||
| 17640899 | 2007 | T-290676 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 1.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=1.314 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-2635 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 16.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.007 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-2635 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 16.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.018 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-2635 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 16.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.025 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-2635 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 16.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.015 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-2635 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 16.3 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.021 µg/ml against 098-T651 virus virus | |||
| 17640899 | 2007 | T-2544 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.1 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.007 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-2544 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.1 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.026 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-2544 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.1 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.033 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | T-2544 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.1 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.014 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-2544 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 5.1 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.021 µg/ml against 098-T651 virus virus | |||
| 17640899 | 2007 | T-267209 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 3.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.007 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267209 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 3.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.021 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267209 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 3.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.034 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | T-267209 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 3.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.024 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267209 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 3.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.039 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-267221 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 15.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.011 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267221 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 15.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.035 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267221 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 15.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.028 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | T-267221 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 15.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.035 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267221 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 15.2 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.050 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-267226 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 7.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.007 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267226 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 7.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.021 µg/ml against 098 | |||
| 17640899 | 2007 | T-267226 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 7.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.035 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | T-267226 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 7.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.030 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267226 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 7.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.020 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.019 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.043 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.079 µg/ml against 098-T20 virus virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.038 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267225 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 12.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.196 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-267227 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 17.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.012 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267227 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 17.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.045 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267227 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 17.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.028 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-267227 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 17.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.025 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267227 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 17.9 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.044 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-291022 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 28.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.022 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-291022 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 28.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.049 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-291022 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 28.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.093 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-291022 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 28.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.046 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-291022 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 28.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.242 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-290822 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.030 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-290822 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.054 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-290822 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.084 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-290822 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.147 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-290822 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 8.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.242 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-290821 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 9.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.065 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-290821 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 9.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.118 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-290821 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 9.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.154 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-290821 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 9.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.192 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-290821 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 9.6 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50>20 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-267228 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 30.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.172 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267228 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 30.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.600 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267228 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 30.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.416 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-267228 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 30.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.555 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267228 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 30.8 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=0.987 µg/ml against 098-T651 virus | |||
| 17640899 | 2007 | T-267229 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 35.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50=3.162 µg/ml against IIIB virus | |||
| 17640899 | 2007 | T-267229 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 35.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50>20 µg/ml against 098 virus | |||
| 17640899 | 2007 | T-267229 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 35.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50>20 µg/ml against 098-T20 virus | |||
| 17640899 | 2007 | T-267229 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 35.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50>20 µg/ml against 098-T1249 virus | |||
| 17640899 | 2007 | T-267229 | 38 | Free | Free | Linear | L | None | Synthetic peptide | Antiviral peptide | Not reported | ~1 €“2mg/kg | 35.4 | Monkey blood proteases | RP-HPLC and ESI-MS | Male cynomolgus monkey blood plasma (Intravenous) | in vivo | None | None | IC50>20 µg/ml against 098-T651 virus | |||
| 17994612 | 2007 | Exendin-4 (Ex-4) | 39 | Free | Free | Linear | L | None | Salivary gland of the lizard Heloderma suspectum | Glucose-dependent insulin secretion, suppresses inappropriately elevated glucagon secretion, and slows down gastric emptying | Not reported | 4.0 mg/kg | 56.7 | Not mentioned | Radioimmunoassay | Monkey (Intravenous injection) | in vivo | None | None | Not given | |||
| 17994612 | 2007 | Exendin-4 (Ex-4) | 39 | Free | Free | Linear | L | None | Salivary gland of the lizard Heloderma suspectum | Glucose-dependent insulin secretion, suppresses inappropriately elevated glucagon secretion, and slows down gastric emptying | Not reported | 4.0 mg/kg | 77.4 | Not mentioned | Radioimmunoassay | Monkey (Subcutaneous injection) | in vivo | None | None | CL/F =2.0 ml/h/kg | |||
| 18413862 | 2008 | A3-APO (Dimer) | 38 | Chex =Cyclohexane carboxylic acid | Free | Linear | L | Dab =2,4-diamino-butyric acid | Synthetic peptide | Antibacterial | Not reported | 5 mg/kg | 100 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC= 16 mg/mL | |||
| 18413862 | 2008 | A3-APO (Dimer) | 38 | Chex =Cyclohexane carboxylic acid | Free | Linear | L | Dab =2,4-diamino-butyric acid | Synthetic peptide | Antibacterial | Not reported | 5 mg/kg | 230 | Mouse serum proteases | RP-HPLC | Mouse serum | in vitro | None | None | MIC= 16 mg/mL | |||
| 18553094 | 2008 | BNP | 32 | Free | Free | Linear | L | None | Pro-Brain natriuretic peptide | Vasodilator | Not reported | Not mentioned | ~22 | Human blood proteases | ELISA | Human plasma | in vitro | None | None | Not available | |||
| 19458086 | 2009 | fsANP | 40 | Free | Free | Cyclic (C7-C23) | L | None | C terminus of atrial natriuretic peptide | Natriuretic, diuretic and vasorelaxant | Not reported | 1 µM | 4.5 | Human kidney membrane proteases | Radioimmunoassay | Human kidney membranes | in vitro | None | None | IC50=3.2nM | |||
| 19602537 | 2009 | GLPAG | 37 | Free | Cholesterol moiety | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | 3mg/kg | Stable | Mouse blood proteases | RP-HPLC and ESI-MS | Mouse plasma (Subcutaneous injection) | in vivo | None | None | EC 50, cAMP=180nM for mGCGR | |||
| 19602537 | 2009 | DualAG | 37 | Free | Cholesterol moiety | Linear | L | None | Proglucagon molecule | Protease-resistant dual GLP1R/GCGR agonist | Not reported | 3mg/kg | 1.7 | Mouse blood proteases | RP-HPLC and ESI-MS | Mouse plasma (Subcutaneous injection) | in vivo | None | None | EC 50, cAMP=1.5nM for mGCGR | |||
| 19602537 | 2009 | Oxm | 37 | Free | Free | Linear | L | None | Proglucagon molecule | Antidiabetic | Not reported | 3mg/kg | ~8-12 | Mouse blood proteases | RP-HPLC and ESI-MS | Mouse plasma (Subcutaneous injection) | in vivo | None | None | EC 50, cAMP=6.2nM for mGCGR | |||
| 11976797 | 2002 | Exendin 3 | 39 | Free | Free | Linear | L | Radiolabelling of exendin 3 at position 1 (histidine) | Heloderma horridum venom | GLP-1 agonist | Not reported | 10 MBq of the radiolabelled peptides | 13 ±3.2 | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 11976797 | 2002 | Exendin 3 | 39 | Free | Free | Linear | L | Radiolabelling of exendin 3 at position 1 (histidine) | Heloderma horridum venom | GLP-1 agonist | Not reported | 10 MBq of the radiolabelled peptides | 108 ±16 | Rat blood proteases | Scintigraphy | NEDH Rats (rat tumour model) | in vivo | None | None | Not mentioned | |||
| 15587934 | 2004 | Human BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 3.1 | Not mentioned | EIA | Mice plasma (Intravenous injection) | in vivo | None | None | EC50 =0.46 ± 1.1 nM | |||
| 15587934 | 2004 | AlbuBNP | 32 | Human serum albumin | Free | Linear | L | None | B-type cardiac natriuretic peptides fused to HAS at N-terminal | Vasodilator | Not reported | 2.19 mg/kg | 11.2 | Mouse blood proteases | EIA | Mice plasma (Intravenous injection) | in vivo | None | None | EC50 =28.4 ± 1.2 nM | |||
| 15587934 | 2004 | AlbuBNP | 32 | Human serum albumin | Free | Linear | L | None | B-type cardiac natriuretic peptides fused to HAS at N-terminal | Vasodilator | Not reported | 2.19 mg/kg | 19.3 | Mouse blood proteases | EIA | Mice plasma (Subcutaneous injection) | in vivo | None | None | EC50 =28.4 ± 1.2 nM | |||
| 18353507 | 2008 | PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | 23 ±6 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 7.7 ±1.4 nM | |||
| 18353507 | 2008 | PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetically synthesised pituitary adenylate cyclase-activating polypeptide | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 4.3 ±0.3 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 7.7 ±1.4 nM | |||
| 18353507 | 2008 | Acetyl-PACAP38 | 38 | Acetylation | Amidation | Linear | L | None | Synthetic analog of PACAP38 | 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 ±1.5 nM | |||
| 18353507 | 2008 | Hexanoyl-PACAP38 | 38 | Hexanoylation | Amidation | Linear | L | None | Synthetic analog of PACAP38 | 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 = 8.3 ±1.8 nM | |||
| 18353507 | 2008 | [Aib2]PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | 65 ±8 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 7.1 ±1.4 nM | |||
| 18353507 | 2008 | [D-Ser2]PACAP38 | 38 | Free | Amidation | Linear | Mix | None | Synthetic analog of PACAP38 | 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 = 9.7 ±2.5 nM | |||
| 18353507 | 2008 | [ψCH2-NH21-22]PACAP38 | 38 | Free | Amidation | Linear | L | [ψCH2-NH21-22] | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 18 ±2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 59 ±17 nM | |||
| 18353507 | 2008 | [Ala20]PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 8.3 ±1.2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 1.2 ±0.4 nM | |||
| 18353507 | 2008 | [Ala21]PACAP38 | 38 | Free | Amidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 6.6 ±0.5 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 2.0 ±0.5 nM | |||
| 18353507 | 2008 | Acetyl-PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | 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 = 2.9 ±0.9 nM | |||
| 18353507 | 2008 | Acetyl-PACAP38-hexylamide | 38 | Acetylation | Hexylamidation | Linear | L | None | Synthetic analog of PACAP38 | 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 = 3.5 ±0.7 nM | |||
| 18353507 | 2008 | Acetyl-[Ala14, Ala20]PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 5.3 ±1.7 nM | |||
| 18353507 | 2008 | Acetyl-[Ala14, Ala20]PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 15 ±2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 5.3 ±1.7 nM | |||
| 18353507 | 2008 | Acetyl-[Ala15, Ala20]PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-5 M | >240 | DPP IV | RP-HPLC and MS-MALDI-TOF | DPP IV | in vitro | None | None | IC50 = 1.8 ±0.7 nM | |||
| 18353507 | 2008 | Acetyl-[Ala15, Ala20]PACAP38-propylamide | 38 | Acetylation | Propylamidation | Linear | L | None | Synthetic analog of PACAP38 | Therapeutic Neuropeptide for neurodegenerative diseases. | Not reported | 10-4 M | 25 ±2 | Human plasma proteases | RP-HPLC and MS-MALDI-TOF | Human plasma | in vitro | None | None | IC50 = 1.8 ±0.7 nM | |||
| 19836183 | 2010 | BNP | 32 | Free | Free | Linear | L | None | Porcine brain | Vasodilator | Not reported | 31.2ng/ml | 3.1 | Mouse plasma proteases | ELISA | Mouse plasma | in vivo | None | None | Not mentioned | |||
| 21334413 | 2011 | Exendin-4 | 39 | Free | Free | Linear | L | None | Venom of the lizard Heloderma suspectum | Binds and activates the GLP-1 receptor | Not reported | 500 μg/kg | 2.4 | Rat blood proteases | Radioimmunoassay | Rat plasma | in vitro | None | None | Not mentioned | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 0.1 mg/kg | 19.0 ± 2.0 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.67 106/ µl 21 days after the administration | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 0.5 mg/kg | 34.0 ± 5.9 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.67 106/ µl 21 days after the administration | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 5 mg/kg | 99.0 ± 37.1 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.67 106/ µl 21 days after the administration | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 5[C14] mg/kg | 84.0 ± 9.56 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.73 106/ µl 21 days after the administration | |||
| 24378440 | 2013 | EGFR2R-lytic peptide | 32 | Free | Free | Linear | Mix | None | Synthetic peptide | Cytotoxic and antitumor | Not reported | Not mentioned | 9.4 ± 1.5 | Not mentioned | Not mentioned | Bovine serum | in vivo | None | None | Not available | |||
| 24378440 | 2013 | EGFR2R-lytic peptide-gelatin complex | 32 | Free | Free | Linear | Mix | None | Synthetic peptide | Cytotoxic and antitumor | Not reported | Not mentioned | 19.3 ±2.9 | Not mentioned | Not mentioned | Bovine serum | in vivo | None | None | Not available | |||
| N.A. | 2011 | Chimeric Motilin A | 35 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.74 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin B | 34 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin C | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.9 ±0.53 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin D | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.9 ±0.50 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin E | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin F | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.37 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin G | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.25 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-ii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.5 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-iii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.65 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-vi | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.94 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-vii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 12.78 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-viii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.56 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xii | 33 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 13.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xiii | 34 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 13.09 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-A | 39 | Free | Free | Cyclic (C1-C17) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 24 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-B | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 40 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-C | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 27.2 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-A | 39 | Free | Free | Cyclic (C1-C17) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 46.4 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-B | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 57.3 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-C | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 37.8 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-A | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 20.7 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-B | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 24 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-A | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 21.7 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-B | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 362 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-C | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 15.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-D | 37 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 20.3 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-G | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 17.75 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-H | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 14.86 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-I | 34 | Free | Amidation | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 14.5 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-J | 39 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 20 nm/ Kg | 31.24 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-K | 35 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 20 nm/ Kg | 18.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2012 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | 520 micro g/Kg | 0.8 | Not mentioned | EIA | Rat plasma (Subcutaneous) | in vivo | None | EP2423233A2 | Blood glucose after 24 hour >25 mM | |||
| N.A. | 2012 | Exendin-4-α1AT(P357N) | 39 | Free | Fusion of Alpha-1 Antitrypsin Monovariant [α1AT(P357N)] | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | 520 micro g/Kg | 19.1 | Not mentioned | EIA | Rat plasma (Subcutaneous) | in vivo | None | EP2423233A2 | Blood glucose after 24 hour ~10 mM | |||
| N.A. | 2006 | Derivative of Glucagon Like Peptide-2 (GLP-2) | 33 | Free | Amidation | Linear | L | None | GLP-2 | Intestine function modulator | N.A. | 500 nM/ Kg | 1.5 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | US7112567B2 | Increase in wet-weight of small intestine >0.5 g | |||
| N.A. | 2006 | Derivative of Glucagon Like Peptide-2 (GLP-2) | 33 | Free | Amidation | Linear | L | None | GLP-2 | Intestine function modulator | N.A. | 500 nM/ Kg | 0.9 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | US7112567B2 | Not mentioned | |||
| N.A. | 2006 | Derivative of Glucagon Like Peptide-2 (GLP-2) | 34 | Free | Addition of maleimidopropionic acid (MPA) and amidation | Linear | L | None | GLP-2 | Intestine function modulator | N.A. | 500 nM/ Kg | 16.2 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | US7112567B2 | Increase in wet-weight of small intestine ~0.3 g | |||
| N.A. | 2006 | Derivative of Glucagon Like Peptide-2 (GLP-2) | 34 | Free | Addition of maleimidopropionic acid (MPA) and amidation | Linear | L | None | GLP-2 | Intestine function modulator | N.A. | 500 nM/ Kg | 23.8 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | US7112567B2 | Not mentioned | |||
| N.A. | 2012 | Intermedin or adrenomedullin peptide | 39 | Free | Free | Linear | L | None | Preproadrenomedullin | Calcium homeostasis | N.A. | Not mentioned | 1.5 | Rat blood proteases | ELISA | Rat plasma (Intravenous) | in vivo | None | WO2012138867A2 | Not mentioned | |||
| 20503261 | 2001 | Val8-GLP-1-Fc | 31 | Free | Addition of Fc | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 5.6 nM/ Kg | 45 | Monkey blood proteases | Radioimmunoassay | Monkey plasma (Intravenous) | in vivo | None | EP1355942B1 | Activation of GLP1 receptor (with respect to Val8-GLP-1(7-37)OH) 1.00% | |||
| 20503261 | 2001 | Val8-GLP-1-Human serum albumin (HSA) | 31 | Free | Human serum albumin | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 5.6 nM/ Kg | 87 | Monkey blood proteases | Radioimmunoassay | Monkey plasma (Intravenous) | in vivo | None | EP1355942B1 | Not mentioned | |||
| 20503261 | 2001 | Gly8-Glu22-GLP-1-CEx-Linker-IgG1 | 31 | Free | Linking IgG1 using CEx-Linker (SSGAPPPS-GGGGSGGGGSGGGGS) | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 55 | Dog blood proteases | Radioimmunoassay | Dog plasma (Intravenous) | in vivo | None | EP1355942B1 | Activation of GLP1 receptor (with respect to Val8-GLP-1(7-37)OH) 150.00% | |||
| 20503261 | 2001 | Gly8-Glu22-GLP-1-CEx-Linker-IgG1 | 31 | Free | Linking IgG1 using CEx-Linker (SSGAPPPS-GGGGSGGGGSGGGGS) | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 38 | Not mentioned | Radioimmunoassay | Dog plasma (Subcutaneous) | in vivo | None | EP1355942B1 | Not mentioned | |||
| 20503261 | 2010 | GLP-1-PEG | 40 | Free | Addition of NH2-PEG at Cys40 | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 25.8 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP1881850B1 | EC50= 0.36 nM | |||
| 20503261 | 2010 | GLP-1-PEG | 40 | Free | Addition of NH2-PEG at Cys40 | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 28.3 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP1881850B1 | Not mentioned | |||
| 20503261 | 2010 | GLP-1-PEG | 40 | Free | Addition of NH2-PEG at Cys40 | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.01 mg/ Kg | 75.69 | Not mentioned | Radioimmunoassay | Monkey plasma (Subcutaneous) | in vivo | None | EP1881850B1 | Not mentioned | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ kg | 1.5 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 1.3 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | Val8-GLP-1-OH | 31 | Free | Addition of hydroxyl group | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 10 micro g/ kg | 0.05 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 100% (as reference) | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 59.5 | Monkey blood proteases | Radioimmunoassay | Monkey plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 61.6 | Not mentioned | Radioimmunoassay | Monkey plasma (Subcutaneous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | Exendin-4 | 39 | Free | Free | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 0.7 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 100% (as reference) | |||
| N.A. | 2012 | Exendin-4(N)-PEG-Fc | 39 | Pegylation | Addition of Fc | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 62 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= <0.2 % with respect to Exendin-4 | |||
| N.A. | 2012 | Exendin-4(Lys27)-PEG-Fc | 39 | Free | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 61 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 13.2 % with respect to Exendin-4 | |||
| N.A. | 2012 | DM exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into dimethylhistidyl (DM) group | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 69 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 2.6 % with respect to Exendin-4 | |||
| N.A. | 2012 | DA exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into desaminohistidyl (DA) group | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 54 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 13.2 % with respect to Exendin-4 | |||
| N.A. | 2012 | HY exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into betahydroxylamidazolpropionyl (HY) | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 52 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 7.6 % with respect to Exendin-4 | |||
| N.A. | 2012 | CA exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into imidazoacetyl (CA) group | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 52 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 8.5 % with respect to Exendin-4 | |||
| N.A. | 2012 | DA GLP-1 (Lys20,28)-PEG-Fc | 39 | Modification of His1 of Exendin-4 into desaminohistidyl (DA) group | Addition of Fc | Linear | L | Pegylation at K20 and K28 | Glucagon like peptide1 | Insulinotropic peptide | N.A. | Not mentioned | 27 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 2 % with respect to Exendin-4 | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 1.2 mg/ Kg | 2.02 | Not mentioned | HPLC | Rat plasma (Subcutaneous) | in vivo | None | US6656906 | Fold fusion-inhibition (CEM cells and Molt-4 cells) with respect to T20 (DP-178) against HIV2-NIH-Z strain 840 Fold | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 1.5 mg/ Kg | 2.46 | Rat blood proteases | HPLC | Rat plasma (Intravenous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.8 mg/ kg | 4.83 | Not mentioned | HPLC | Monkey plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.8 mg/ kg | 5.57 | Not mentioned | HPLC | Monkey plasma (Intramuscular) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.8 mg/ kg | 5.35 | Monkey blood proteases | HPLC | Primate plasma (Intravenous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 15 mg/ Kg | 2 | Not mentioned | HPLC | Rat plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 5 mg/ Kg | 1.86 | Rat blood proteases | HPLC | Rat plasma (Intravenous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 0.4 mg/ kg | 6.23 | Monkey blood proteases | HPLC | Monkey plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| N.A. | 2003 | T1249 | 39 | Acetylation | Amidation | Linear | L | None | Hybrid of anti-HIV peptide and peptide derived from virus glycoproteins | Anti-HIV peptide | N.A. | 1.6 mg/ kg | 5.55 | Monkey blood proteases | HPLC | Monkey plasma (Subcutaneous) | in vivo | None | US6656906 | Not mentioned | |||
| 3922013 | 1984 | Calcitonin gene related peptide | 37 | Free | Free | Linear | L | None | Human non-thyroidal tissue | Vasoactive neuropeptide | Not given | 0.32 pmol/kg | 6.9 ±0.9 (first phase) | Human blood plasma proteases | Radioimmunoassay | Intravenous injection into human | in vivo | http://physrev.physiology.org/content/94/4/1099 | None | CGRP infusion reduces gastric acid output as measured by plasma concentration of CGRP against time data obtained during infusion. | |||
| 3922013 | 1984 | Calcitonin gene related peptide | 37 | Free | Free | Linear | L | None | Human non-thyroidal tissue | Vasoactive neuropeptide | Not given | 2.56 pmol/kg | 26.4 ±4.7 (first phase) | Human blood plasma proteases | Radioimmunoassay | Intravenous injection into human | in vivo | http://physrev.physiology.org/content/94/4/1099 | None | CGRP infusion reduces gastric acid output as measured by plasma concentration of CGRP against time data obtained during infusion. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-36)) | 36 | Free | Amidation | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 2.1 ±0.1 (for first phase) | Dog plasma proteases | Radioimmunoassay and HPLC | Intravenous injection to dogs plasma | in vitro | None | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-37)) | 37 | Free | Free | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 2.4 ±0.3 (for first phase) | Dog plasma proteases | Radioimmunoassay and HPLC | Intravenous injection to dogs plasma | in vitro | http://www.anaspec.com/products/product.asp?id=324 | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-36)) | 36 | Free | Amidation | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 68 ±6 (for final phase) | Dog plasma proteases | Radioimmunoassay and HPLC | Intravenous injection to dogs plasma | in vitro | None | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-37)) | 37 | Free | Free | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 81 ±3 (for final phase) | Dog plasma proteases | Radioimmunoassay and HPLC | Intravenous injection to dogs plasma | in vitro | http://www.anaspec.com/products/product.asp?id=324 | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-36)) | 36 | Free | Amidation | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 132 ±16 | Dog plasma proteases | Radioimmunoassay and HPLC | Subcutaneous injection into dog plasma | in vitro | None | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-37)) | 37 | Free | Free | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 61 ±9 | Dog plasma proteases | Radioimmunoassay and HPLC | Subcutaneous injection into dog plasma | in vitro | http://www.anaspec.com/products/product.asp?id=324 | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-36)) | 36 | Free | Amidation | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 449 ±17 | Dog plasma proteases | Radioimmunoassay and HPLC | Subcutaneous injection into dog plasma in presence of bacitracin | in vitro | None | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 8839678 | 1995 | Glucagon like peptide 1 (GLP( 7-37)) | 37 | Free | Free | Linear | L | None | Human intestinal epithelium | Gastric motility | 5, 10, 20, 40, 60, 90, 120, 240, 300 and 360 min | 400 pmol/l | 238 ±35 | Dog plasma proteases | Radioimmunoassay and HPLC | Subcutaneous injection into dog plasma in presence of bacitracin | in vitro | http://www.anaspec.com/products/product.asp?id=324 | None | Bacitracin proteolytoic assay. When plasma sample incubated with 0.1% of bacitracin half life is increased. | |||
| 7529108 | 1994 | Human big endothelin-1 (Human big-ET-1) | 38 | Free | Free | Linear | L | None | Human Endothelin-1 | Vasoconstricting peptide | 180 minute | 3 nmol of peptide with 200 ng of enzyme | 24 (t1/2 of hydrolysis) | Endopeptidase-24.11(E-24.11) | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 7529108 | 1994 | Porcine big endothelin-1 (Porcine big-ET-1) | 39 | Free | Free | Linear | L | None | Porcine Endothelin-1 | Vasoconstricting peptide | 80 minute | 3 nmol of peptide with 50 ng of enzyme | 25 (t1/2 of hydrolysis) | Thermolysin | Radioimmunoassay and RP-HPLC | Purified ET-1 protein sample | in vitro | 8269939 | None | Not reported | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 32 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 20.7 (slow component) | None | Not mentioned | None | in vitro | 2136732 | None | Not reported | |||
| 8076909 | 1994 | Human BNP (Brain natriuretic Peptide) | 32 | Free | Free | Linear | L | None | Human BNP (Brain Natriuretic Peptide) | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 3.9 (fast component) | None | Not mentioned | None | in vitro | 2136732 | None | Not reported | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 1.25 μg/kg | 14 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 32 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 2.5 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 33 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 5.0 μg/kg | 8.1 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Intravenously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 34 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 5.0 μg/kg | 15 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 35 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 10 μg/kg | 14 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 36 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 12.5 μg/kg | 12 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 37 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 15 μg/kg | 13 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 38 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 17.5 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 12145241 | 2002 | NN2211 (Glucagon- Like Peptide 1 Derivative) | 39 | Free | Free | Linear | L | γ-Glu-palmitoyl residue at position 21 | Glucagon-like peptide 1 (GLP-1) derivative | Anti-diabetic peptide | 48 hours | 20 μg/kg | 11 | Dipeptidyl peptidase IV (DPP-IV), human blood proteases | Not mentioned | Subcutaneously injected in Humans | in vivo | https://www.bachem.com/api-products/generic-apis/l | None | Significant increase in insulin secretion (P = 0.0002), but there was no significant effect on glucagon levels. | |||
| 19805567 | 2010 | Enfuvirtide | 36 | Acetylation | Free | Linear | L | 19 residue is N15 labelled, also have 13C carbon | Enfuvirtide | Antiretroviral fusion inhibitor | 5, 15, and 30 min and 1, 2, 4, 8, 24, and 48 h after drug injection | dose, 4 mg/kg of body weight | 2.8 | Wistar rats blood protease | LC-MS/MS | Female Wistar rats | in vivo | None | None | Showed an EC50 of about 275 nM | |||
| 19805567 | 2010 | Enfuvirtide-PEG12-CP | 37 | Acetylation | Free | Linear | L | Mal-PEG12-CP was conjugated to Cys-enfuvirtide | Enfuvirtide conjugate | Antiretroviral fusion inhibitor | 5, 15, and 30 min and 1, 2, 4, 8, 24, and 48 h after drug injection | dose, 4 mg/kg of body weight | 10.4 | Wistar rats blood protease | LC-MS/MS | Female Wistar rats | in vivo | None | None | The enfuvirtide-CP conjugates displayed similar EC50s that ranged from 51 nM to 72 nM | |||
| 17065394 | 2006 | Porcine PYY (Peptide YY) | 34 | Free | Amidation | Linear | L | None | Porcine intestine | Neuropeptide | 120 minutes | 25 mg/kg BW per min | 15 | Pigs blood proteases | Double-antibody Radioimmunoassay | Intravenously administred to Crossbred (Large White!Landrace!Duroc) castrated male pigs | in vivo | http://www.genscript.com/peptide/RP10354-Peptide_Y | None | Plasma GH levels significantly increased 30 min after PYY3 €“36 injection compared with the saline-injected group (7.8 ± 2.1 vs 3.0 ± 0.6 ng/ml, P<0.05) | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 15 mg/kg | 0.40 ±0.05 (t1/2 α) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 30 mg/kg | 0.63 ±0.02 (t1/2 α) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 150 mg/kg | 1.56 ±0.10 (t1/2 α) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 15 mg/kg | 5.04 ±0.06 (t1/2 β) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 30 mg/kg | 5.83 ±0.86 (t1/2 β) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 17583927 | 2007 | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers (CPP-PMO) | 34 | Free | PMO (5'-ACGTTGAIIIGCATCGTCGC-3') | Linear | L | X = 6-aminohexanoic acid, B = beta-alanine, I = inosine | Cell penetrating peptides-Phosphorodiamidate morpholino oligomers | Cell penetrating peptide | 24 hours | 150 mg/kg | 8.23 ±0.07 (t1/2 β) | Rat plasma proteases | MALDI-TOF-MS | Intravenous administration in Rat | in vitro | None | None | LD50 of the conjugate administered iv in rats was between 210 and 250 mg/kg | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | 2U | 7.32 (steriodigenic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Shows activity of 80~180USP Units/mg | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1/2, 1, 2, 4, 8, and 16min | Not mentioned | 4.43 (lipolytic activity t1/2) | Rat blood proteases | Not mentioned | Intravenously injected to rat | in vivo | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Shows activity of 80~180USP Units/mg | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1,2,3 and 4 hours | 200 mU | 59.22 (lipolytic activity t1/2) | Rat plasma proteases | Not mentioned | Rat plasma | in vitro | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Not mentionedtive ACTH shows similar activity to rat and rabbit fats when compared in terms of the minimal effective dose (rat = 6*10-6mg/50mg tissue and rabbit = 5*10-6mg/50mg tissue) | |||
| 4327730 | 1971 | Purified Sheep Adrenocorticotropic Hormone (ACTH) | 39 | Free | Free | Linear | L | None | Sheep Adrenocorticotropic Hormone (ACTH) | Steroidogenic peptides | 1,2,3 and 4 hours | 200 mU | 250.87 (lipolytic activity t1/2) | Rat muscle proteases | Not mentioned | Rat muscle slices | in vitro | http://www.genscript.com/peptide/RP11304-ACTH_1-39 | None | Not mentionedtive ACTH shows similar activity to rat and rabbit fats when compared in terms of the minimal effective dose (rat = 6*10-6mg/50mg tissue and rabbit = 5*10-6mg/50mg tissue) | |||
| 17283237 | 2007 | Glucagon like peptide-1 (GLP-1) | 37 | Free | Free | Linear | L | None | Human GLP-1 | Growth Hormone | 3 hours | 100 μg/kg peptide in mice | <5 | Mice blood proteases | Radioimmunoassay | Subcutaneously injected in mice | in vivo | http://www.uniprot.org/blast/?about=P01275[92-128] | None | Promotes glucose-depen- dent insulin secretion from the pancreas | |||
| 8403527 | 1993 | Calcitonin gene-related peptide (CGRP) | 37 | Free | Free | Linear | L | None | Human Vasopressin | Vasoactive peptide | 2,4,6,8, 10, 15,20,25,30,40,50,60 and 90 min. | Not mentioned | 63.9 ±4.5 | Rat kidney proteases | Not mentioned | Isolated perfused rat kidney | in vivo | http://www.uniprot.org/blast/?about=P06881[83-119] | None | Not reported | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 3.2mg/kg | 8.15 ±1.97 ( alpha or distribution half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 6.4mg/kg | 9.69 ±1.5 ( alpha or distribution half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 12.8mg/kg | 8.56 ±2.01 ( alpha or distribution half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 3.2mg/kg | 24.74 ±8.30 ( beta or elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 6.4mg/kg | 27.38 ±11.52 ( beta or elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 12.8mg/kg | 30.49 ±10.24 ( beta or elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 3.2mg/kg | 1.45 ±0.53(gamma or termination elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 6.4mg/kg | 1.30 ±0.27 (gamma or termination elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18049308 | 2007 | HLP(Hirulog-like peptide) | 32 | Free | Free | Linear | L | I125 labeling | Synthetic | Thrombin inhibitor | Blood collected after 2-120 minutes after i/v injection of peptide | 12.8mg/kg | 1.24 ±0.44 (gamma or termination elimination half life) | Rat plasma proteases | Radioisotopic tracing method | Rat plasma | in vivo | None | None | Platelet aggregation %age = 24.33 ± 8.12, 25.67 ± 10.01 , 30.17 ± 1.13 for 3.2mg/kg/h . 2.3mg/kg/h 1.6 mg/kg/h respectively as compre to control which 36.67 ± 3.44 %; Therefore, bleeding time was significantly longer in rats received 1.6, 2.3, or 3.2 mg/kg/h of HLP compared to control | |||
| 18972837 | 2008 | sCT (Salmon calcitonin) | 32 | Free | Free | Cyclic (C1-C7) | L | None | Hormone secreted by the parafollicular cells of thethyroid gland | Calcitropic Hormone, reduce blood calcium | 5-360minutes | 10 µM | 13.18 | Rat kidney homogenates proteases | LC-ESI-MS | Rat kidney homogenates | in vitro | None | None | Not reported | |||
| 18972837 | 2008 | sCT (Salmon calcitonin) | 32 | Free | Free | Cyclic (C1-C7) | L | None | Hormone secreted by the parafollicular cells of thethyroid gland | Calcitropic Hormone, reduce blood calcium | 5-360minutes | 10 µM | 43.07 | Rat kidney homogenates proteases | LC-ESI-MS | Rat Liver homogenates | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | β-Endorphin | 31 | Free | Free | Linear | L | None | Endogenous opioid neuropeptide in neurons of both the central and peripheral nervous system. | Agonist of the opioid receptors | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22263969 | 2012 | 2m (monomer Atrial natriuretic peptide- Fc ) | 39 | Free | Fc region | Cyclic (C7-C23 & C-residues of Fc region) | 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 | 3.9 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | Ex-4 (Exendin-4) | 39 | Free | Free | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | Blood sample collected after 50-130 minutes after the infusion of peptide | 10 pmol/kg | 32.8 ±4.1 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | GLP-1Arg34(7 €“36), Ex(31 €“39) or [GLP-Ex] | 39 | Free | Free | Linear | L | None | Synthetic | GLP-1 receptor agonist | Blood sample collected after 42-130 minutes after the infusion of peptide | 20 pmol/kg | 19.5 ±3.3 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 25039358 | 2014 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 4.8 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =1.6 ± 0.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist, Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 17.1 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 12 | 31 | 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 | 5.4 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 11.3 ± 0.6 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 13 | 31 | 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 | 18.4 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 16.8 ± 0.7 pM in HEK-293 cells | |||
| 25039358 | 2014 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 2.5 ±1.2 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 =1.6 ± 0.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 14 .9 ±0.9 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells | |||
| 25243635 | 2014 | VGLP1 (Glucagon like peptide 1 derivative) | 31 | Free | Free | Cyclic (C18-C26) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | <5 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | VGLP1K3 (Glucagon like peptide 1 derivative) | 34 | Free | Free | Cyclic (C18-C26) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | <80 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | VGLP1K6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | ~ 70 | DPP IV | ELISA | DPP IV | in vitro | None | None | The insulin levels were increased dramatically to 906.53b ± 22.18pmol/L within 60 min after GLP-1 administration | |||
| 25243635 | 2014 | VGLP1S6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | ~ 7.5 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | VGLP1V6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | ~ 5 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | GLP-1(Glucagon Like protein-1) | 31 | Free | Free | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 5-90 hours | 500μg | <2 | DPP IV | ELISA | DPP IV | in vitro | None | None | The insulin levels were increased dramatically to 806.74 ± 30.60 pmol/L within 15 min after GLP-1 administration | |||
| 25243635 | 2014 | VGLP1K6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 5-90 hours | 300μg/Kg body weight of rats | ~ 70 | Rat serum proteases | ELISA | Subcutaneously injected in Sprague ˆ’Dawley (SD) rats | in vivo | None | None | The insulin levels were increased dramatically to 906.53b ± 22.18pmol/L within 60 min after GLP-1 administration | |||
| 25594223 | 2015 | ENF(Enfuvirtide) | 36 | Acetylation | Amidation | Linear | L | None | Enfuvirtide | Anti-viral (Anti-HIV activity) | 0.5-24 hours | 1.7μM/Kg | 1.5 | Rat plasma proteases | HPLC | Sprague-Dawey (SD) rats Plasma | in vivo | None | None | EC50 = 3nM for Anti-viral potency | |||
| 25594223 | 2015 | SL-ENF(Sialic acid Enfuvirtide) | 37 | Sialic acid | Amidation | Linear | L | None | Synthetic derived from glycosylated ENFs | Anti-viral | 0.5-24 hours | 1.7μM/Kg | 23.1 | Rat plasma proteases | HPLC | Sprague-Dawey (SD) rats Plasma | in vivo | None | None | EC50 = 2nM for Anti-viral potency | |||
| 25594223 | 2015 | Lac-ENF (Lactic acid Enfuvirtide) | 37 | Lactic acid | Amidation | Linear | L | None | Synthetic derived from glycosylated ENFs | Anti-viral | 0.5-24 hours | 1.7μM/Kg | 4.2 | Rat plasma proteases | HPLC | Sprague-Dawey (SD) rats Plasma | in vivo | None | None | EC50 = 2nM for Anti-viral potency | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 37 C, 48 Hours | 10 µM | 4.18 | Fxa(Facor Xa) and DPP-IV | HPLC-ESI/MS/MS | Protein Sample +HAS + Fxa +DPP IV | in vitro | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | ~ 5 | db/db mice plasma proteases | LC-MS/MS | db/db Mice plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | ~ 5 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | Exendin-4 | 39 | Free | Free | Linear | L | None | GLP-1 derived peptide | Regulate blood glucose | 0.5-24 hours | 0.5 mg/kg | 3.03 | db/db mice plasma proteases | LC-MS/MS | db/db Mice plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in Exendin-4 -treated mice (20nmol/kg) is 1.62 fold higher than control | |||
| 25771000 | 2015 | Exendin-4 | 39 | Free | Free | Linear | L | None | GLP-1 derived peptide | Regulate blood glucose | 0.5-24 hours | 0.5 mg/kg | >3 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in Exendin-4 -treated mice (20nmol/kg) is 1.62 fold higher than control | |||
| 25900863 | 2015 | TRI-1144 | 38 | Acetylation | Amidation | Linear | L | None | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 4.2 | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG-TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with PEG(40KDa) thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 34 | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG-TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with PEG(40KDa) thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Not mentioned | Not mentioned | 70 | Human plasma proteases | LC-MS/MS | Human Plasma | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG40kDa[ClPhSO2]TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with ClPhSO2 conjugate thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Not mentioned | Not mentioned | 150 (t1/2β) | Human plasma proteases | LC-MS/MS | Human Plasma | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG40kDa[ClPhSO2]TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with ClPhSO2 conjugate thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 150 (t1/2 linker cleavage) | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG40kDa[MorphSO2]TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with MorphSO2 conjugate thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 44 (t1/2β of releasable PEG-TRI-1144 conjugate) | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 3.4 ±0.2 | Pig blood proteases | Radioimmunoassay and HPLC | Female pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 10.8 ±0.8 | Pig blood proteases | Radioimmunoassay and HPLC | Female pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotinin | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 6.2 ±0.2 | Pig plasma proteases | Radioimmunoassay and HPLC | Female pigs plasma+ Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 11.9 ±0.7 | Pig plasma proteases | Radioimmunoassay and HPLC | Female pigs plasma+ Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotinin | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | PYY(3-34) [Peptide YY] | 34 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Blood sample collected after 15minutes of the infusion of peptide | 100 pmol/kg | 3.6 ±0.5 | Pig blood proteases | Radioimmunoassay | Female pigs blood | in vivo | None | None | Porcine PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.9nmol/L | |||
| 26197931 | 2015 | PYY(1-36) [Peptide YY] | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Blood sample collected after 15minutes of the infusion of peptide | 100 pmol/kg | 7.3 ±0.8 | Pig blood proteases | Radioimmunoassay | Female pigs blood | in vivo | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 04 to 18 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P700 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P800 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 1 ±0.3 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 5 ±1.0 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 12 ±1.0 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 41 ±5.0 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | OXM(1-37) (Oxyntomodulin) | 37 | Free | Free | Linear | L | None | Peptide Hormone of colon | Anti-apetizer | Room Temp | 0.4 µM | <24 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | OXM(1-37) (Oxyntomodulin) | 37 | Free | Free | Linear | L | None | Peptide Hormone of colon | Anti-apetizer | Room Temp | 0.4 µM | >72 | Human plasma proteases + DPP IV | MS | P800 plasma | in vitro | None | None | Not reported | |||
| 26308095 | 2015 | Exenatide | 39 | Free | Amidation | Linear | L | None | Saliva of Gila monster | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after7-288 hours after the injection of peptide | 5nmol/Kg | 02-Mar | Proteases from mini-pig plasma | ELISA, LC/MS | Mini-pigs plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | Exenatide | 39 | Free | Amidation | Linear | L | None | Saliva of Gila monster | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 30 | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | Acylation of peptide at K-26 with C-18(palmitic acid) fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Upregulates intracellular cAMP resulting in the release of insulin | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 8-10 hours | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | Acylation of peptide at K-26 with C-18(palmitic acid) fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Upregulates intracellular cAMP resulting in the release of insulin | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 14.4 hours | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | semaglutide | 36 | Free | Amidation | Linear | L | Alpha-aminoisobutyric acid at 8th position, Acylation of peptide at K-26 with C-18 fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after7-288 hours after the injection of peptide | 1 -2 nmol/Kg | 165 | Human plasma proteases | ELISA, LC/MS | Human plasma (Dose s/c injected) | in vivo | 25475122 | None | Semaglutide was the most potent with an ED50 of < 2 nmol/kg | |||
| 26308095 | 2015 | semaglutide | 36 | Free | Amidation | Linear | L | Acylation of peptide at K-26 with C-18 fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 46 | Mini-pig plasma proteases | ELISA, LC/MS | Mini-pigs plasma (Dose s/c injected) | in vivo | 25475122 | None | Semaglutide was the most potent with an ED50 of < 2 nmol/kg | |||
| 26337231 | 2015 | RMP-16 (Recombinant slow-release TNF α-derived peptide) | 32 | Free | Free | Linear | L | None | Recombinant slow-release TNF α-derived peptide | Tumor growth inhibitor and anti-angiogenic | Blood sample collected after0.5-24 hours after the injection of peptide | 5mg/kg | 13.11 ±1.49 | BALB/c mice plasma proteases | LC/MS | BALB/c mice plasma (Dose i/v injected) | in vivo | None | None | Growth inhibition effect of RMP16 was observed in DU145 cells (IC50 = 17.20 ± 1.95 nM, the tumor inhibition rates of RMP16-treated mice was 78.11% | |||
| 21459096 | 2011 | BNP(B-type natriuretic peptide) | 32 | Free | Free | Cyclic (C10-C26) | L | None | Brain natriuretic peptide | Cardiac fibrosis Inhibitor | 37 °C for 0-125 minutes | Not mentioned | 8 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 21459096 | 2011 | DNP (Dendroaspis natriuretic peptide) | 39 | Free | Free | Cyclic (C7-C23) | L | None | Dendroaspis natriuretic peptide | Natriuretic and hypotensive activities | 37 °C for 0-125 minutes | Not mentioned | 159 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | 19395584 | None | Not reported | |||
| 21459096 | 2011 | CD-NP (C-terminal tail of DNP) | 37 | Free | Free | Cyclic (C6-C22) | L | None | Chimeric peptide derived from CNP and DNP | Natriuretic and aldosterone suppressor | 37 °C for 0-125 minutes | Not mentioned | 17-22.9 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 25625650 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist | 0.25-84 hours | 0.6mg s/c injected | 12 ±2.8 | Cat blood proteases | ELISA | Healthy cat blood (Dose s/c injected) | in vivo | None | None | Insulin secretion increased 760.8 ± 350.7 (449 €“1,493) ng/L on Liraglutide administration as compared to normal 455.5 ±115.8 (411 €“660) in hyperglycemic patients | |||
| 5092290 | 2014 | LL-37 (Antimicrobial Peptide) | 37 | Free | Free | Linear | L | None | Human epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein) | Antimicrobial | 15-720 minutes hour | 3 µM | ~1 | Cathepsin | Proteolysis assay, (confirmed by Western blotting) | Western Blotting | in vitro | 16716248 | None | Not reported | |||
| 5092290 | 2014 | LL-37 (Antimicrobial Peptide) | 37 | Free | Free | Linear | L | None | Human epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein) | Antimicrobial | 15-720 minutes hour | 3 µM | >12 | Cathepsin | Proteolysis assay, (confirmed by Western blotting) | Western Blotting | in vitro | 16716248 | None | Not reported | |||
| 1904406 | 1991 | [Leu27] hGRF( 1-32)NH2 (Growth hormone releasing factor analog) | 32 | Free | Amidation | Linear | L | None | Human growth hormone releasing factor analog | Growth hormone(GH) release | 37 °C, phosphate buffer pH 7.4 | 0.2mM | 202 | Collagenase pancreatin | HPLC | Cultured bovine anterior pituitary cells | in vitro | None | None | EC50=0.24 ± 0.045(GH release) | |||
| 1904406 | 1991 | [Leu27, Asn28]hGRF(I-32)NH2 (Growth hormone releasing factor analog) | 32 | Free | Amidation | Linear | L | None | Human growth hormone releasing factor analog | Growth hormone(GH) release | 37 °C, phosphate buffer pH 7.4 | 0.2mM | 150 | Collagenase pancreatin | HPLC | Cultured bovine anterior pituitary cells | in vitro | None | None | EC50=0.32 ± 0.059(GH release) | |||
| 1904406 | 1991 | [Ser8, Leu27, Asn28]hGRF(I-32)NH2 (Growth hormone releasing factor analog) | 32 | Free | Amidation | Linear | L | None | Human growth hormone releasing factor analog | Growth hormone(GH) release | 37 °C, phosphate buffer pH 7.4 | 0.2mM | 746 | Collagenase pancreatin | HPLC | Cultured bovine anterior pituitary cells | in vitro | None | None | EC50=0.26 ± 0.040(GH release) | |||
| 1904406 | 1991 | [Ser8, Leu27]hGRF(I-32)NH2 (Growth hormone releasing factor analog) | 32 | Free | Amidation | Linear | L | None | Human growth hormone releasing factor analog | Growth hormone(GH) release | 37 °C, phosphate buffer pH 7.4 | 0.2mM | 1550 | Collagenase pancreatin | HPLC | Cultured bovine anterior pituitary cells | in vitro | None | None | EC50=0.44 ± 0.014(GH release) | |||
| 3147901 | 1988 | Oxyntomodulin | 37 | Free | Free | Linear | L | None | Synthetic derived from proglucagon, identified in extracts from porcine small intestinal mucosa | GLP-1-GCGR (glucagon) agonist | Blood samples collected at 1-5 hourss after peptide injection | 100- 400ng/kg/h | 12 ±1 | Human plasma proteases | Radioimmunoassay | Human plasma (Dose i/v injected) | in vivo | http://www.glucagon.com/oxyntomodulin.html | None | The acid secretion increased during the first 90 rnin of pentagastrin infusion from 1 - 2 meq H+/15 rnin to a plateau of 5-6 meq H+/15 min | |||
| 3261772 | 1988 | hCGRP(Human Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Blood collected-10 to 90 minutes after peptide infusion | 5pmol/kg | 3.6 ±0.3 (Half life of 1st phase) | Sheep plasma proteases | Radioimmunoassay, RP-HPLC | Merino-Corriedale cross ewes (sheep) plasma | in vivo | None | None | Not reported | |||
| 3261772 | 1988 | hCGRP(Human Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Blood collected-10 to 90 minutes after peptide infusion | 5pmol/kg | 13.6 ±1.0(Half life of 1st phase) | Sheep plasma proteases | Radioimmunoassay, RP-HPLC | Merino-Corriedale cross ewes (sheep) plasma | in vivo | None | None | Not reported | |||
| 3601235 | 1987 | Porcine NPY (Neuropeptide Y) | 36 | Free | Amidation | Linear | L | None | Neuropeptide | Acts as a neurotransmitter | Blood collected 1 to 90 minutes after peptide infusion | 06-10nM/kg | ~ 20 (20-28) | Dog plasma proteases | Radioimmunoassay | Six mongrel dogs plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 3924685 | 1985 | hGRF-1(1-40) (Human growth regulating factor) | 40 | Free | Amidation | Linear | L | None | Human growth regulating factor | Release growth hormone | Blood collected 60-240 minutes after peptide injection | 5 µg/200ul | 57.3 ±1.5 (beta or elimination half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 3924685 | 1985 | hGRF-1(1-40) (Human growth regulating factor) | 40 | Free | Amidation | Linear | L | None | Human growth regulating factor | Release growth hormone | Blood collected 60-240 minutes after peptide injection | 5 µg/200ul | 3.2 ±0.2 (alpha or distribution half life) | Rat plasma proteases | Radioimmunoassay | (Dose i/v injected)Rat plasma | in vivo | None | None | Not reported | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 4.95 ±1.04(short half life or initial decay) | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 32.4 ±5(long half life) | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 4.55 ±1.23 (short half life or initial decay) | Proteases from Human(obese) plasma | Radioimmunoassay | Human(obese) plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 1551497 | 1992 | C-peptide (Connecting peptide) | 31 | Free | Free | Linear | L | None | Pro-insulin derivative | Connect A- and B-chains of insulin and regulates Ca-dependent cell signaling | Blood collected 2-180 minutes after peptide injection | 150 µg of peptide injected | 32.4 ±5(long half life) | Proteases from Human(obese) plasma | Radioimmunoassay | Human(obese) plasma | in vivo | None | None | Insulin secretion rates can be accurately estimated from plasma levels of C-peptide | |||
| 2714145 | 1989 | GLP-1(72-107) (Glucagon-like peptide-1) | 36 | Free | Amidation | Linear | L | None | Glucagon-like peptide-1 derivative | Regulates glycemic index, inhibits gastric acid secretion | Not mentioned | 14.4ng/kg peptide infused from 45 min as priming dose, followed by 100 - 400 ng/kg/h dose for 45 m | 17.2 ±2 | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | 200pmol/L and 600pmol/L cause 16% and 23% Inhibition of pentagastrin-stimulated acid secretion respectively | |||
| 2714145 | 1989 | Truncated GLP-1(78-107) | 31 | Free | Amidation | Linear | L | None | Glucagon-like peptide-1 derivative | Regulates glycemic index, inhibits gastric acid secretion | Not mentioned | 4.8 -14.4ng/kg peptide infused from 45 min as priming dose, followed by 12.5 - 50 ng/kg/h dose for | 11.4 ±2.1 | Proteases from Human plasma | Radioimmunoassay | Human plasma | in vivo | None | None | 200pmol/L of peptide causes 36% Inhibition of pentagastrin-stimulated acid secretion respectively | |||
| 8147781 | 1994 | CGRP(Calcitonin gene related peptide) | 37 | Free | Free | Linear | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | 37 °C for 5-60 minutes | 60 µL of 1 nmol/L CGRP | 4.3 ±0.2 | Proteases from sheep plasma | Radioimmunoassay | Sheep plasma before nephrectomy | in vitro | None | None | Not reported | |||
| 8147781 | 1994 | CGRP(Calcitonin gene related peptide) | 37 | Free | Free | Linear | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | 37 °C for 5-60 minutes | 60 µL of 1 nmol/L CGRP | 7.6 ±0.8 | Proteases from sheep plasma | Radioimmunoassay | Sheep plasma after 2 days nephrectomy | in vitro | None | None | Not reported | |||
| 8147781 | 1994 | CGRP(Calcitonin gene related peptide) | 37 | Free | Free | Linear | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | 37 °C for 5-60 minutes | 60 µL of 1 nmol/L CGRP | 7.3 ±0.4 | Proteases from sheep plasma | Radioimmunoassay | Sheep plasma after 5 days nephrectomy | in vitro | None | None | Not reported | |||
| 8403527 | 1993 | CGRP(Calcitonin gene related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Neuropeptide and alernative spliced product of calcitonon produced by thyroid gland | Vasodilator | Blood sample collected after 2-90 minutes | 1.0 pmol/ml of peptide | 63.9 ±4.5 | Rat plasma proteases and isolated perfused rat kidney | Not mentioned | Rat plasma (+IPRK (isolated perfused rat kidney)filtering) | in vitro | None | None | Not reported | |||
| 8403527 | 1993 | CGRP(Calcitonin gene related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Neuropeptide and alernative spliced product of calcitonon produced by thyroid gland | Vasodilator | Blood sample collected after 2-90 minutes | 1.0 pmol/ml of peptide | >10 | Rat plasma proteases and isolated perfused rat kidney | Not mentioned | Rat plasma (+IPRK (isolated perfused rat kidney)filtering) | in vitro | None | None | Not reported | |||
| 26308095 | 2015 | Semaglutide | 31 | Free | Free | Linear | L | Aib =2-Aminoisobutyric acid; Acylation of peptide at K-26 with fatty acid side chain i.e. N6-[N-(17-carboxy-1-oxoheptadecyl-L-c-glutamyl[2- (2-aminoethoxy)ethoxy]acetyl[2-(2 aminoethoxy)ethoxy]acetyl | GLP-1 (Glucagon like peptide-1) analogue | Regulate blood glucose level | Blood samples collected upto 96 hous | 1 -2 nmol/Kg | 165 | Proteases from Human plasma | ELISA, LC/MS | (Dose s/c injected)Human plasma | in vivo | 23743288 | None | Semaglutide was the most potent to lower blood glucose with an ED50 of < 2 nmol/kg | |||
| 26308095 | 2015 | Semaglutide | 31 | Free | Free | Linear | L | Aib =2-Aminoisobutyric acid; Acylation of peptide at K-26 with fatty acid side chain i.e. N6-[N-(17-carboxy-1-oxoheptadecyl-L-c-glutamyl[2- (2-aminoethoxy)ethoxy]acetyl[2-(2 aminoethoxy)ethoxy]acetyl | GLP-1 (Glucagon like peptide-1) analogue | Regulate blood glucose level | Blood samples collected upto 96 hous | 5nmol/Kg | 46 | Proteases from mini-pig plasma | ELISA, LC/MS | (Dose i/v injected)Mini-pigs plasma | in vivo | 23743288 | None | Semaglutide was the most potent to lower blood glucose with an ED50 of < 2 nmol/kg | |||
| 1911217 | 1991 | CGRP (Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Not mentioned | 300-600pmol | 9.00 (plasma half-life) | Proteases from Human plasma | Not mentioned | Human Plasma | in vivo | None | None | Not reported | |||
| 1911217 | 1991 | CGRP (Calcitonin gene-related peptide) | 37 | Free | Amidation | Cyclic (C2-C7) | L | None | Alernative spliced product of calcitonon produced by thyroid gland | Vasodilator and cause tumor hypoxia | Not mentioned | 300-600pmol | 30 (biological half-life) | Not mentioned | Not mentioned | Human Plasma | in vivo | None | None | Not reported | |||
| 24361089 | 2014 | Teriparatide | 34 | Free | Free | Linear | L | None | Parathyroid Hormone derivative | Increase the concentration of ionic calcium (Ca2+) in the blood | Not mentioned | Not available | 5 (Elimination half life) | Proteases from human plasma(Severe renal impairment patients) | Not mentioned | Human plasma (Severe renal impairment patients) | in vivo | None | None | Not reported | |||
| 24361089 | 2014 | Teriparatide | 34 | Free | Free | Linear | L | None | Parathyroid Hormone derivative | Increase the concentration of ionic calcium (Ca2+) in the blood | Not mentioned | Not available | 1.5 (Elimination half life) | Proteases from human plasma(Normal) | Not mentioned | Human plasma (Normal) | in vivo | None | None | Not reported | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 90mg | 3.16(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Intravenous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 45mg | 3.46(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Subcutaneous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 90mg | 3.8(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Subcutaneous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 15656696 | 2005 | Enfuvirtide | 36 | Acetylation | Amidation | Linear | L | None | Synthetic peptide derived from the naturally occurring motif (residues 643 €“678) within the second heptad repeat (HR2) domain of the HIV- 1HXB2 gp41 transmembrane glycoprotein. | Inhibits de novo infection and cell-to-cell HIV-1 virus transmission | Not mentioned | 180mg | 4.35(t1/2β) | Human blood proteases | liquid chromatography-tandem mass spectrometry method | Subcutaneous injection in 12 HIV patients,blood samples | in vivo | http://www.drugbank.ca/drugs/DB00109 | None | Not mentioned | |||
| 19023544 | 2008 | Tα1-TP5 (Thymosin α1-thymopentin) | 33 | Acetylation | Free | Linear | L | None | Synthetic | Immunoregulatory | Not mentioned | Not mentioned | 140 ±14 | Rabbit plasma proteases | HPLC | Heparinized rabbit plasma | in vitro | http://www.drugbank.ca/drugs/DB00110 | None | IL2 concentration in mouse serum:0.75pg/ml,macrophage clearance index(K value)=0.0206 ±0.0010,phagocytic index(α value=3.95 ±0.19(compared to TP5). | |||
| 21210710 | 2011 | Linear chlorotoxin(CTX) | 36 | Free | Free | Linear | L | N-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 27 | Scorpion venom | Identify tumor foci with high sensitivity | 24 hours | 50μl of 40μM | 14 | Mice serum proteases | Imaging system to measure fluorescent intensity | Intravenous injection in two month old wild-type C57BL/6 mice | in vivo | http://www.drugbank.ca/drugs/DB00140 | None | Fluorescent efficiency (cm2) in the tumor compared with control mice=2.49 ±1 | |||
| 24133142 | 2013 | GLP2-2G-XTEN (Glucagon like peptide-2-2G-XTEN) | 34 | Free | Ahx-6-aminohexanoic acid, Mpa-3-maleimidopropionic acid conjugated to the amino group of Ahx,XTEN protein | Linear | L | None | Glucagon-like peptide 2 variant | Treatment of short bowel syndrome | Aliquots were collected at 0.08, 4, 8, 24, 48, 72, 96, 120 and 168 h | 2mg/kg of rats | 38.5 ±7.4 | Rats blood proteases | ELISA,RP-HPLC | Subcutaneous injection in female Sprague €“ Dawley strain rats | in vivo | http://www.drugbank.ca/drugs/DB00185 | None | GPCR Ca2+ flux mobilization assay, relative activity=1.43% | |||
| 1213660 | 1975 | Procine C-Peptide | 34 | Free | Free | Linear | L | None | Proinsulin | Not mentioned | Not reported | 5-8.6 µg/kg were injected. | 9.9 ±0.5 | Porcine blood proteases | Radioimmunoassay | Porcine blood | in vivo | http://www.drugbank.ca/drugs/DB00187 | None | Not reported | |||
| 8100840 | 1993 | Neuropeptide Y | 36 | Free | Amidation | Linear | L | None | Neuropeptide | Stimulation of the right cardiac sympathetic nerve | Not reported | Not reported | 21 | Dogs blood proteases | Not mentioned | Dogs plasma | in vivo | http://www.drugbank.ca/drugs/DB00195 | None | Not reported | |||
| 38917331 | 2024 | Aptamer-split peptide conjugate | 34 | DBCO modified S10 at C terminus | DBCO modified S11 peptide at N terminus | Linear | L | Azide-modified aptamer fragments (5 SSA and 3 SSA) "TTAATTCTGGGGGAGCCTTTTGTGGGTAGGGTTTTGTGGGTAGGGCGGGTTGGTTTTCGGGTTGGTTTTGCCCCGGAGGAGGAATT" are conjugated with DBCO-modified peptides (S10 and S11) , DBCO = Dibenzocyclooctyne | Aptamer-peptide complex | Hetero modulator for split GFP in response to ATP | Samples were collected every 24 h for 7 days | 1 μM | 4 | C57Bl/6N Mice serum protease | Serum stability assay | C57BL/6N Mice serum | In Vitro | None | None | A shorter antisense DNA of 11 nucleotides (aptamer) showed an EC50 value of 238 μM | |||
| 38789061 | 2024 | Liraglutide | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 5.3 ± 1.5 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 0.5 ± 0.1 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38789061 | 2024 | Liraglutide | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Blood samples (250 μL) were collected at predetermined time points. For SC-dosed rats, time points included pre-dose, 15 min, 30 min, 1 hr, 2 hr, 3 hr, 4 hr, 8 hr, 10 hr, 24 hr, and 30 hr | 1 mg/kg | 9.1 ± 2.9 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood sample was collected for IV-dosed rats, time points were pre-dose, 1 min, 5 min, 15 min, 30 min, 1 hr, 2 hr, 4 hr, 8 hr, 10 hr, and 24 hr | 1 mg/kg | 1.03 ± 0.10 | Male SD rats plasma protease | UHPLC | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38789061 | 2024 | Liraglutide (Lymph cannulated) | 31 | Free | Free | Linear | L | Lys-30 is replaced by Arg and Lys-20 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Lymph was collected continuously into tubes at specified time intervals: predose, 0–15 min, 15–30 min, 30 45 min, 45–60 min, 1–1.5 hr, 1.5–2 hr, 2–3 hr, 3–4 hr, 4–6 hr, 6–8 hr, 8–10 hr, 10–24 hr, and 24–30 hr | 2 mg/kg | 12.61 ± 5.45 | Male SD rats lymph protease | UHPLC | Male SD rats thoraic lymph | In Vivo | None | None | N.A. | |||
| 38789061 | 2024 | Exenatide (Lymph cannulated) | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | Lymph was collected continuously into tubes at specified time intervals: predose, 0–15 min, 15–30 min, 30 45 min, 45–60 min, 1–1.5 hr, 1.5–2 hr, 2–3 hr, 3–4 hr, 4–6 hr, 6–8 hr, 8–10 hr, 10–24 hr, and 24–30 hr | 1 mg/kg | 10.26 ± 6.51 | Male SD rats lymph protease | UHPLC | Male SD rats thoraic lymph | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 100 µg/kg | 8.43 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 30 µg/kg | 15.4 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 100 µg/kg | 7.36 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 300 µg/kg | 9.21 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.02 mg/kg | 32.3 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.007 mg/kg | 24 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.02 mg/kg | 24.3 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38721043 | 2024 | EXT607 (R=OH) | 35 | Free | Cys modified PTH-1 linked with VitD3 through (PEG)36 | Linear | L | R= OH for Cys35 | PTH-1 derivative | Treatment of Hypoparathyroidism | Blood samples were collected at 0 (pre-dose), 0.083 (IV only), 0.25, 0.5, 1, 2, 4, 6, 12, 24, 36, 48, 60, and 72 h post-dose | 0.07 mg/kg | 27.7 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 23.7 (Calcium responses of EXT607 in mammalian cells overexpressing human PTHR1) | |||
| 38601038 | 2024 | DR10627 | 39 | Free | Amidation | Linear | L | A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position | GLP-1 analogs | Antiobesity, Antidiabetes | Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration | 1 nmol/kg | 5.80 ± 1.26 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action | |||
| 38601038 | 2024 | DR10627 | 39 | Free | Amidation | Linear | L | A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position | GLP-1 analogs | Antiobesity, Antidiabetes | Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration | 5 nmol/kg | 5.05 ± 0.405 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action | |||
| 38601038 | 2024 | DR10627 | 39 | Free | Amidation | Linear | L | A palmitoyl group is conjugated to DR10627 via a -γ-glutamyl-linker connected to the Lys10 position | GLP-1 analogs | Antiobesity, Antidiabetes | Blood samples were collected at 0 (pre-dose), 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 30, 38 and 48 h after administration | 26 nmol/kg | 4.19 ± 0.957 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | The glucose-lowering effect of 12 nmol/kg DR10627 reached its lowest point at 2 hours post-administration, and the effect lasted for 24 hours, indicating a long-lasting action | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼16.8 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38486997 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys20 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Attenuates Renal Fibrosis | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼8 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼20.5 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38486997 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys20 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Attenuates Renal Fibrosis | Blood samples were collected at 0 min (before peptides administration) and 10, 20, 30 min, 1, 2, 4, 6, 8, 24, 36, 48, 72 h, 4, 5, 6 and 7 day after peptides administration | 0.05 mg/kg | ∼7.95 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | N.A. | 25.0 μg/kg | 84 | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38486997 | 2024 | 1907-B | 40 | Free | Replacing the amide bond with a C-terminal acid | Cyclic (Lactam Bridge K17 & D21) | Mix | At position 10 of the peptide sequence, modifications involving octadecanedioic acid (C18) and a glycine/serine-based linker "GGSGSG" were introduced, Aib modification,D-serine | GLP-1 analogs | Antidiabetes | N.A. | 25.0 μg/kg | N.A. | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | GLP-1R EC50 (nmol/L) = 0.088 (for 1907-B) | |||
| 38356317 | 2024 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety conjugated with Lys20, Aib modification at position 2,13 | GLP-1 analogs | Antidiabetes | PK samples were collected after single and multiple doses, up to 109 weeks of continuous tirzepatide treatment | 2–500 ng/mL. | 5.4 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | N.A. | |||
| N.A. | 2024 | Compound 2 | 40 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, aMeL13, Ornl6, K17, Aib20, D-Glu24, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.06 nmol/kg | 105 | Dogs plasma protease | LC-MS | Dogs plasma after food is provided 30 min post dose | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 2 | 40 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, aMeL13, Ornl6, K17, Aib20, D-Glu24, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 389 nmol/kg | 96 | Dogs plasma protease | LC-MS | Dogs plasma after treatment with Sodium Caprate (C10, 280Mg) | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 3 | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.01 nmol/kg | 104 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 3 | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 20 mg | 111 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 3 | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 and 1-Nal22 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 20 mg | 104 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | TZP | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.15 nmol/kg | 70 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | TZP | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 4.15 nmol/kg | 159 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | TZP | 40 | Free | Amidation | Linear | L | Aib2, Aibl3 substituitions, Lys20 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)1-CO-(CH2)18-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 336 Hours | 20 mg | 97 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 4 μg/kg | 144 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 8 μg/kg | 147 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 14 μg/kg | 135 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 20 μg/kg | 147 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 40 μg/kg | 141 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 60 μg/kg | 154 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | Blood samples were taken for PK measures pre-dose and at 1, 2, 4, 8, and 12 h post-dose on day 1, and once on days 2, 4, 7, 10, 14, 21, 28, 35, 42, and 49 | 100 μg/kg | 180 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 1 mg | 155.03 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 2 mg | 151.53 ( terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Trough samples were taken immediately before dosing on days 8, 22, 36, and 50. Samples were taken again after the last (eighth) dose at 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 4 mg | 155.85 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 8 mg | 159.95 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 12 mg | 170.62 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38288338 | 2024 | Efpeglenatide | 39 | N terminal amine group of His replaced by imidazo-acetyl | Amidation | Linear | L | Conjugate in which LYS27 side chain linked to PEG-Fc | Exendin-4 analogs | Antidiabetes | blood samples were taken for PK assessments pre-dose on the first dosing day (day 1) and 8, 24, 48, 72, 96, 120, and 144 h after the first dose. Samples were also taken 7, 10, 14, and 21 days after dosing. Trough samples were taken immediately before dosing on days 29 and 57. Finally, after the last (third) dose, samples were taken 8, 24, 48, 72, 96, 120, and 144 h after dosing and 7, 10, 14, 21, 28, and 35 days after dosing | 16 mg | 161.76 (terminal elimination half life) | Human serum protease | Sandwich ELISA | Human serum | In Vivo | https://pubmed.ncbi.nlm.nih.gov/32175655/ | None | N.A. | |||
| 38952487 | 2024 | [3H]-semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H) | GLP-1 analogs | GLP-1 receptor agonist | Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose | 1 mg/ml | 168.3 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Intact [3H]-semaglutide-related material | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H), other metabolite may be attached | GLP-1 analogs | GLP-1 receptor agonist | Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose | 1 mg/ml | 201.2 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Dry [3H]-semaglutide-related material | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18(3H), other metabolite may be attached | GLP-1 analogs | GLP-1 receptor agonist | Blood sample were collected at predose, 8, 16, 24,32,40,48,56,64,72,96,120,144,168,240,336,504,672 and 840 hours post dose | 1 mg/ml | 180.5 | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for PK assessment of semaglutide were taken at the following time points after the first dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144 and 168 h and at the following time points after the last dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h. Additional PK samples were taken before dosing in weeks 4, 8 and 11 | 0.5 mg | 156 | Human blood sample protease | LC-MS/MS | Human blood sample with once weekly dosage (at steady state) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for PK assessment of semaglutide were taken at the following time points after the first dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144 and 168 h and at the following time points after the last dose: 0, 6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h. Additional PK samples were taken before dosing in weeks 4, 8 and 11 | 1 mg | 159 | Human blood sample protease | LC-MS/MS | Human blood sample with once weekly dosage (at steady state) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 183 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Normal Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 169 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Mild Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 201 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Moderate Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | blood samples were taken 15 min prior to administration of semaglutide and 2, 8, 14, 16, 18, 20, 22, 24, 26, 28, 30, 32, 34, 38, 42, 48, 54, 60, 66, 72, 96, 144, 192, 240, 360, and 480 h after administration of semaglutide | 0.5 mg | 221 (elimination half life) | Human serum protease | LC-MS/MS | Human serum (Severe Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | For ESRD subjects on hemodialysis, hourly blood samples were drawn during each of the first two hemodialysis sessions post-administration (each hemodialysis session lasted for ~2–4 h). | 0.5 mg | 243 (elimination half life) | Human serum protease | LC-MS/MS | Human serum dosage 1–24 H after hemodialysis, With No Hemodialysis For 48 H Post-Dose (End Stage Renal Disease Renal Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 150 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Normal Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 155 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Mild Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 151 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Moderate Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were taken to determine the plasma concentration profiles of semaglutide 15 minutes prior to dosing, at time zero, and at 6, 12, 18, 24, 30, 36, 42, 48, 54, 60, 72, 96, 120, 144, 168, 336, 504, 672 and 840 hours (up to 35 days) after administration of semaglutide | 0.5 mg | 163 (Terminal elimination half life) | Human plasma protease | LC-MS/MS | Human plasma (Severe Hepatic Function Group) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | N.A. | 20 mg | 153 | Human plasma protease | Luminescence oxygen channelling immunoassay (LOCI) | Human plasma dosed at steady state (Healthy) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | N.A. | 40 mg | 161 | Human plasma protease | Luminescence oxygen channelling immunoassay (LOCI) | Human plasma dosed at steady state (Healthy) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | N.A. | 40 mg | 158 | Human plasma protease | Luminescence oxygen channelling immunoassay (LOCI) | Human plasma dosed at steady state (Type 2 Diabetic) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | 10 days | 10 mg | 160 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 mg Once Daily Semaglutide (Subjects In The Fasting Arm Were Fasting Overnight For At Least 10 H Before Each Dosing) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | 10 days | 10 mg | 152 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 Mg Once Daily Semaglutide (Subjects In The Reference Arm Were Fasting Overnight For At Least 6 H Before Each Dosing) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for semaglutide PK assessment were drawn onday 1 (pre- and post-dose), then pre-dose on days 6 to 10 | 7 mg | 141 | Human plasma protease | N.A. | Human plasma (Type 2 Diabetic Patient With Upper Gastrointestinal Disease) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples for semaglutide PK assessment were drawn onday 1 (pre- and post-dose), then pre-dose on days 6 to 10 | 7 mg | 142 | Human plasma protease | N.A. | Human plasma (Type 2 Diabetic Patient Without Upper Gastrointestinal Disease) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were drawn into K3EDTA tubes pre-dose on day 1, and at set time points on days 9 and 10 | 10 mg | 150 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 mg Semaglutide Once Daily For 5 Days | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 38952487 | 2024 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples were drawn into K3EDTA tubes pre-dose on day 1, and at set time points on days 9 and 10 | 10 mg | 156 | Human plasma protease | LC-MS/MS | Human plasma dosed with 10 mg Semaglutide Once Daily For 5 Days And With Omeprazole 40 Mg | In Vivo | https://pubmed.ncbi.nlm.nih.gov/28323117/, https://pubmed.ncbi.nlm.nih.gov/29205786/, https://pubmed.ncbi.nlm.nih.gov/33159658/ | None | N.A. | |||
| 37759683 | 2023 | IBP-EK1 | 32 | Conjugation with human immunoglobulin G Fc-binding peptide (IBP) at n terminus | Free | Linear | L | None | Fusion protein | Antiviral | Serial blood samples were collected from monkeys that received IBP-EK1 or EK1 before injection and at 2, 4, 6, 24, 72, and 144 h post injection | 10 mg/kg | 37.67 | Rhesus monkeys serum protease | HPLC-MS/MS | Rhesus monkeys serum | In Vivo | None | None | IC50 = 788 nM for IBP-EK1 ( against Pseudotyped SARS-CoV-2 Variants on Caco-2 Cells) | |||
| 37759683 | 2023 | IBP-EK1 | 32 | Conjugation with human immunoglobulin G Fc-binding peptide (IBP) at n terminus | Free | Linear | L | None | Fusion protein | Antiviral | Serial blood samples were collected from monkeys that received IBP-EK1 or EK1 before injection and at 2, 4, 6, 24, 72, and 144 h post injection | 10 mg/kg | 39.72 | Rhesus monkeys serum protease | HPLC-MS/MS | Rhesus monkeys serum | In Vivo | None | None | IC50 = 788 nM for IBP-EK1 ( against Pseudotyped SARS-CoV-2 Variants on Caco-2 Cells) | |||
| 37390979 | 2023 | BI-3434 | 33 | Free | Amidation | Linear | L | Lys33 conjuagted with HLE (fatty acid based half life extension group),Substituting Ser with 2-aminoisobutyric acid (Aib) at position 2 | Lipidated secretin analog | Secretin receptor agonist | N.A. | 30 nmol/kg | <15 | Male NMRI mice plasma protease | Mass spectrometry | Male NMRI mice plasma (Non fasted) | In Vivo | None | None | EC50 =15.5 pM for BI-3434 | |||
| 36989942 | 2023 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys20 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes, Antiobesity | N.A. | N.A. | 7.22 - 9.26 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | PubChem CID: 56843331 | None | N.A. | |||
| 36780786 | 2023 | hGLP-2 (variant 6) | 33 | Free | Free | Linear | L | Addition of a C16 monoacid at position 20 of the hGLP-2 peptide | Proglucagon-derived intestinal hormone | Antiapoptosis, Antiinflammatory | Blood samples were drawn from the tail at t = 0.5, 1, 2, 4, 8, 12, 24, 36, and 48 h | 400 µg/kg | 9.5 | Female SD rats plasma protease | RIA | Female SD rats plasma | In Vivo | None | None | EC50 = 0.44 nM for hGLP-2R in the presence of 1% HSA | |||
| 36630826 | 2023 | Exendin-4 | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 2.12 ± 0.3 (T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36630826 | 2023 | Ex-PEGRh(4.4 ± 1.1nm) | 39 | Free | PEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 23.14 ± 3.2(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-PEGMw(46.3KDa) | 39 | Free | PEGylation (Mw(46.3KDa)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 34.91 ± 4.5(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 = 2.7 ± 0.5 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 97.3 ± 3.2(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Exendin-4 | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 1.88 ± 0.2(T1/2 Elimination) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36630826 | 2023 | Ex-PEGRh(4.4 ± 1.1nm) | 39 | Free | PEGylation (Rh(4.4 ± 1.1nm)) and linked via DBCO | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 11.9 ± 2.7 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 12.1 ± 1.0 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt(54.7KDa) | 39 | Free | POEGMA (poly[oligo(ethylene glycol) methyl ether methacrylate]) conjugation (MW opt = 54.7KDa) | Linear | L | Fluorescently labeled | Exendin-4 analogs | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol kg−1 | 105.7 ± 6 (T1/2 Elimination) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 = 2.8 ± 0.7 nM | |||
| 36410792 | 2023 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Small Bowel Hypertrophic Effect | Blood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912 | 670 nmol/kg | 0.6 ± 0.1 | SD rats serum protease | GLP-2 ELISA | SD rats serum | In Vivo | None | None | EC50 = 0.12 ± 0.056 nM for teduglutide peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP) | |||
| 36410792 | 2023 | HM15912 | 34 | [(1H-imidazol-4-yl)-acetyl 1] | Conjugation of GT15912 and hIgG4 Fc was carried out through the formation of amine bonds between the bi functional PEG and Lys34 in GT15912 or the N-terminal amino acid in hIgG4 Fc | Linear | L | None | GLP-2 analogue | Small Bowel Hypertrophic Effect | Blood (0.3 ml) was then collected from the jugularvein at 0.25, 0.5, 1, 1.5, 2, 3, 4, 6, and 8 hours for teduglutide and 1, 4, 8, 24, 48, 72, 96, 230, 244, 268, 192, 216, 240, 264, 288, 312, and 336 hours for HM15912 | 13 nmol/kg | 42.3 ± 3.4 | SD rats serum protease | GLP-2 ELISA | SD rats serum | In Vivo | None | None | EC50 = 0.327 ± 0.096 nM for HM15912 peptide (In vitro potency of GLP-2 analogs on human GLP-2 receptor in cell-based functional assays of dose-response cAMP) | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 2.12 ± 0.3 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 23.14 ± 3.2 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-PEGMw | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(46.3 KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 34.91 ± 4.5 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 (nM) = 2.7 ± 0.5 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional POEGMA(54.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 97.3 ± 3.2 (T1/2 Elimination) | Naïve mice plasma protease | fluorescence assay | Naïve mice plasma | In Vivo | None | None | EC50 (nM) = 2.8 ± 0.7 | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 1.88 ± 0.2 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional PEG(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 11.9 ± 2.7 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | Exendin-DBCO was conjugated to azide-functional POEGMA(54.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 105.7 ± 6 (T1/2 Elimination) | Immunized mice plasma protease | fluorescence assay | Immunized mice plasma | In Vivo | None | None | EC50 (nM) = 2.8 ± 0.7 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, And 48 H post I.V. application | 0.25 mg/kg | 7.9 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 8.21 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 7.33 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 5.69 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 8.68 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2.0 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 10.3 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2.0 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 6.19 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 6.97 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 11.2 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 6 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 9.7 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.5 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 11.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 16 | 31 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid, Iva = Isovaline | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 10.8 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.1 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 19.6 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 20.1 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | SEQ ID NO 21 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 12.9 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.8 | |||
| N.A. | 2023 | SEQ ID NO 21 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 12.1 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.8 | |||
| N.A. | 2023 | SEQ ID NO 22 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 13.6 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 1 | |||
| N.A. | 2023 | SEQ ID NO 22 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 15.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 1 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.08, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post I.V. application | 0.25 mg/kg | 14.5 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 35 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, and 48 H post S.C. application | 0.5 mg/kg | 14.3 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 0.6 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0 H and after 0.083, 0.25, 0.5, 1 , 2, 4, 8, 24, 32, 48, 56, 72, 80, and 96 H post I.V. application | 0.05 mg/kg | 64.1 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | SEQ ID NO 19 | 39 | Free | Amidation | Linear | L | Aib = α-aminoisobutyric acid | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0 H and after 0.25, 0.5, 1 , 2, 4, 8, 24, 32, 48, 56, 72, 80, and 96 H post S.C. application | 0.1 mg/kg | N.A. | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2022074607 W | IC50 hGIPR (nM) = 2 | |||
| N.A. | 2023 | Parent compound 1 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 8 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 104 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 2.1 | |||
| N.A. | 2023 | Parent compound 3 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 131 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4 | |||
| N.A. | 2023 | Parent compound 4 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 56 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4.2 | |||
| N.A. | 2023 | Parent compound 5 | 39 | Free | Amidation | Linear | L | Aib at position 2 and 13, Chem.16[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19- carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 134 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 9.7 | |||
| N.A. | 2023 | Parent compound 1 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 8 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 nmol/kg | 121 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 2.1 | |||
| N.A. | 2023 | Parent compound 2 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 1 nmol/kg | 104 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 1.5 | |||
| N.A. | 2023 | Parent compound 4 | 39 | Free | Free | Linear | L | Aib at position 2, Chem. 7 [(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 1 nmol/kg | 106 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | hGLP-1R, CRE Luc 0% HSA EC50(pM) = 4.2 | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 0.65 ± 0.04 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | PEG Rh(27.7Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 6.59 ± 0.27 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-PEGMw | 39 | Fluorescently labelled | PEG MW(46.3 Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 6.6 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 2.7 ± 0.5 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | PEGMAopt(54.7Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 9.1 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 2.8 ± 0.7 | |||
| 36630826 | 2023 | Exendin | 39 | Fluorescently labelled | Amidation | Linear | L | None | Derived from Gila monster | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 0.77 ± 0.07 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 0.04 ± 0.01 | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Fluorescently labelled | PEG RH(27.7KDa) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | N.A. | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 1.3 ± 0.2 | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Fluorescently labelled | POEGMAopt(54.7Kda) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Ten μl of blood was collected from a tiny incision on the tail vein into tubes containing 90 μl of 1,000 U ml-1 heparin (Sigma) at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h. | 1000 nmol/kg | 12.1 ± 1.0 (T1/2 Absorption) | Immunized mice plasma protease | Fluorescence assay | Immunized mice plasma | In Vivo | PDB id: 7MLL | None | EC50 (nM) = 2.8 ± 0.7 | |||
| 36630826 | 2023 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 0.65 ± 0.04 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36630826 | 2023 | Ex-PEGRh | 39 | Free | PEGylation | Linear | L | Fluorescently labeled | Synthetic | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 6.59 ± 0.27 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 1.3 ± 0.2 nM | |||
| 36630826 | 2023 | Ex-PEGMw | 39 | Free | PEGylation | Linear | L | Fluorescently labeled | Synthetic | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 6.6 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 2.7 ± 0.5 nM | |||
| 36630826 | 2023 | Ex-POEGMAopt | 39 | Free | POEGMA conjugation | N.A. | L | Fluorescently labeled | Synthetic | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 9.1 ± 0.9 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 2.8 ± 0.7 nM | |||
| 36630826 | 2023 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | Blood collection at 5-min, 1-, 2-, 4-, 8-, 24-, 48-, 72-, 96-, 120-, 144- and 168-h | 1000 nmol/kg | 0.77 ± 0.07 (T1/2 Absorption) | Naïve mice plasma protease | Fluorescence assay | Naïve mice plasma | In Vivo | PDB id: 1JRJ | None | EC50 = 0.04 ± 0.01 nM for exendin | |||
| 36997003 | 2023 | Compound 14 | 40 | Free | Amidation | Linear | Mix | D-Ser2 substiuition, Lys14 side chain linked to C16 fatty acid via linker yE-C16 | GLP-1 analogs | Dual GLP-1/Glucagon receptor agonist | The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application | 1 mg/kg | 3.2 | C57/B16 female mice plasma protease | LC−MS/MS | C57/B16 female mice plasma | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | GLP-1 receptor : EC50 = 3.9 pM | |||
| 36997003 | 2023 | Liraglutide | 32 | Free | Free | Linear | L | Lys20 side chain linked to C16 fatty acid via linker yE-C16 | GLP-1 analogs | Dual GLP-1/Glucagon receptor agonist | The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application | 1 mg/kg | 3.6 | C57/B16 female mice plasma protease | LC−MS/MS | C57/B16 female mice plasma | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | GLP-1 receptor : EC50 = 6.4 pM | |||
| 37242650 | 2023 | ELA | 32 | pGlu = Pyroglutamate | Free | Cyclic (C17-C22 disulfide bond) | L | None | Human derived | Endogenous Ligand of APJ | Incubated at 37°C for 2, 5 and 10 min | 1 mM | Almost completely degraded after 2 min | Rats plasma protease | HPLC-MS | Rats plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/26986036/ | None | Gαi1 EC50 (nM) = 5.3 ± 2.5 | |||
| 36380917 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | 37 °C | 0.3 nmol | 10.2 ± 0.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | PDB id: 5VAI | None | BGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | 37 °C | 6 nmol | 55.7 ± 12.1 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | PDB id: 5VAI | None | BGLmax (mmol L−1) = 19.27 ± 1.41 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glc-GLP-1-1 | 31 | Free | Free | Linear | L | Glucosylation at Asn15 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 30.2 ± 2.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-1 | 31 | Free | Free | Linear | L | Glucosylation at Asn15 | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 94.1 ± 7.6 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-3 | 31 | Free | Free | Linear | L | Glucosylation at Asn26 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 46.1 ± 3.5 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-3 | 31 | Free | Free | Linear | L | Glucosylation at Asn26 | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 138.8 ± 14.5 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-5 | 31 | Free | Free | Linear | L | Glucosylation at Asn34 | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 32.5 ± 1.4 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glc-GLP-1-5 | 31 | Free | Free | Linear | L | Glucosylation at Asn34 | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 113.3 ± 11.8 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | N.A. | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn15 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 49.1 ± 5.7 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 24.44 ± 2.37 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn15 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 355.5 ± 9.3 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 24.44 ± 2.37 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 145.7 ± 4.3 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-1(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn15 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 736.6 ± 12.3 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 28.71 ± 2.63 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 185.3 ± 1.1 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn26 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 738.6 ± 9.7 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 24.07 ± 3.79 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn26 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 374.7 ± 1.8 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 25.71 ± 3.19 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-3(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn26(G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 1393.1 ± 8.9 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 25.71 ± 3.19 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn34 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 182.0 ± 0.1 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 14.50 ± 1.62 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2) | 31 | Free | Free | Linear | L | N-glycosylation with biantennary complex-type N-glycan at Asn34 (G2 glycoform = glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 390.4 ± 13.5 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 14.50 ± 1.62 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 0.3 nmol | 245.3 ± 1.3 | DPP-IV | RP-HPLC | 50 mM Tris–HCl (pH 7.4) buffer + 10 ng μL−1 DPPIV | In Vitro | None | None | BGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability) | |||
| 36380917 | 2022 | Glycan-GLP-1-5(G2S2) | 31 | Free | Free | Linear | L | N-glycosylation with sialylated biantennary complex-type N-glycan at Asn34 (G2S2 glycoform = sialylated glycan) | GLP-1 analogs | Antidiabetes | 37 °C | 6 nmol | 777.0 ± 10.2 | Mouse serum protease | RP-HPLC | Mouse serum | In Vitro | None | None | BGLmax (mmol L−1) = 15.50 ± 3.74 (In vivo glucose stabilizing capability) | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 228 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 3.8 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M1 | 35 | Free | Two lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 17 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.068 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M2 | 34 | Free | 1 lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 5 mg | 231 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 254 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal , Amidation | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 2.8 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M1 | 35 | Free | Two lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 37.7 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.068 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M2 | 34 | Free | 1 lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 255 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | blood sampling in subjects receiving 5 and 10 mg of glepaglutide once weekly occurred at the day 1 visit (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 60, 72, 96 and 120 h post-dose); pre-dose on days 8, 15, 22 and 29; and in connection with the last dosing visit on day 36 (pre-dose and 0.5, 1, 2, 4, 8, 12, 16, 20, 24, 36, 48, 72, 120, 168, 336, 504, 672 and 840 h post-dose) | 10 mg | 88.3 | Human plasma protease | LC-MS | Human plasma after SC glepaglutide 5 mg after 6 once-weekly doses | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 10.4 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide parent | 39 | Free | Six lysines has been added at C terminal , Amidation | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 11.7 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.12 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M1 | 35 | Free | Two lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 1.2 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.068 nM In vitro potency | |||
| 36323988 | 2022 | Glepaglutide M2 | 34 | Free | 1 lysines has been added at C terminal | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood sampling for a pharmacokineticanalysis in these subjects was conducted pre-dose and at 5,10, 15, 20, 25, 35, 45, 60, 75 and 90 min and 2, 3, 4, 8, 12,16, 20, 24, 36 and 48 h after the start of the IV infusion, and again on day 22 | 1 mg | 2.6 | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | EC50 = 0.044 nM In vitro potency | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 20 nmol/kg | 10.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18059 pmol/kg | 12.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18058 pmol/kg | 10.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17872 pmol/kg | 18.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 1 | 31 | desH indicates the non-natural amino acid deamino-histidine | Free | Linear | L | X = R1, R2 = H (R2 group present in R1) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18052 pmol/kg | 12.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17838 pmol/kg | 8.5 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17881 pmol/kg | 8 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17833 pmol/kg | 8.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17941 pmol/kg | 7.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18000 pmol/kg | 7.9 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 17890 pmol/kg | 8.7 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35990007 | 2022 | Peptides 2 | 35 | desH indicates the non-natural amino acid deamino-histidine at position 1 | Free | Linear | L | X = R1, R2 = H (R2 group present in R1), Y = R3, R4 = Zr (R4 group present within R3) | GLP-1R agonist | Antidiabetes, Antiobesity | 200 µL blood samples were taken at 2, 6, 10, 24, 30 and 48 h | 18117 pmol/kg | 8.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 35971165 | 2022 | Au‐AR pep‐PROTAC | 33 | Free | Free | Linear | L | None | Synthetic | Anticancer (Prostate Cancer Therapy) | N.A. | N.A. | 26.3 | Mouse serum protease | ICP‐MS | mouse serum | In Vivo | None | None | N.A. | |||
| 35971165 | 2022 | Au‐AR pep‐PROTAC | 33 | Free | Free | Linear | L | None | Synthetic | Anticancer (Prostate Cancer Therapy) | N.A. | N.A. | 25.1 | PBS containing 10% serum protease | HPLC | PBS containing 10% serum | In Vitro | None | None | IC50 of Au‐AR pep‐PROTAC on AML 12 cells is 2.41 µM | |||
| 35971165 | 2022 | AR pep‐PROTAC | 33 | Free | Free | Linear | L | None | Synthetic | Anticancer (Prostate Cancer Therapy) | N.A. | N.A. | 1.9 | PBS containing 10% serum protease | HPLC | PBS containing 10% serum | In Vitro | None | None | IC50 of Au‐AR pep‐PROTAC on AML 12 cells is 2.41 µM | |||
| 35858423 | 2022 | 4A | 38 | 3A coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2CHSO2-, N3-linker N-hydroxysuccinymidocarbonates containing isopropyl sulfone (1A) and N,N-dimethyl-sulfonamide (1B) modulators | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600 and 672 h on a staggered schedule from 12 mice to give 4 replicates at each time-point | 20 nmol | 40 (T1/2,a -Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | QWk 50 nmol of 4A caused significantly increased growth, with mice becoming about 25% longer than the vehicle control over the study period | |||
| 35858423 | 2022 | 4B | 38 | 3B coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2CHSO2-, N3-linker N-hydroxysuccinymidocarbonates containing N,N-dimethyl-sulfonamide (1B) modulators | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 24, 96, 168, 240, 336, 408, 504, 576, 672, 840, 1008, 1176, 1344, and 1512 h from 8 mice on a staggered schedule to give 4 replicates at each time-point | 700 nmol | 60 ( T1/2,a - Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | Single dose of 85 nmol of 4B showed similar growth stimulation as QD administration of [Gln6,14]CNP-38 for 3 weeks, but growth plateaued afterward | |||
| 35858423 | 2022 | 4A | 38 | 3A coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2CHSO2- | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600 and 672 h on a staggered schedule from 12 mice to give 4 replicates at each time-point | 20 nmol | 212 (T1/2,b-Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | QWk 50 nmol of 4A caused significantly increased growth, with mice becoming about 25% longer than the vehicle control over the study period | |||
| 35858423 | 2022 | 4B | 38 | 3B coupled to bicyclononyne-modified MSs (MS-N-hydroxysuccinymidocarbonates) | Free | Linear | L | Gln 6,14 modification, Mod = (CH3)2NSO2- | MS-[Gln6,14]CNP-38 conjugate | Treatment of Achondroplasia | Blood samples (~100 μL) were drawn from the tail vein at 8, 24, 24, 96, 168, 240, 336, 408, 504, 576, 672, 840, 1008, 1176, 1344, and 1512 h from 8 mice on a staggered schedule to give 4 replicates at each time-point | 700 nmol | 610 ( T1/2,b-Elimination Half Life) | CD1 mice plasma protease | ELISA, LC-MS/MS | CD1 mice plasma | In Vivo | None | None | Single dose of 85 nmol of 4B showed similar growth stimulation as QD administration of [Gln6,14]CNP-38 for 3 weeks, but growth plateaued afterward | |||
| 35710141 | 2022 | mGIPAnt‐1 | 37 | Free | Free | Linear | L | C16-diacid acylation at Lysine16 | GIP analogue | Antiobesity | Retro‐orbital blood samples (50 μl) were taken using EDTA coated glass capillaries at (1) t = 0, 0.5, 1, 1.5, 2 and 2.5 h, (2) t = 2.5, 3, 4, 6, 8 and 22 h, or (3) t = 22, 24, 26, 28, 30 and 32 h and immediately | 300 nmol/kg | 7.2 | Mouse Retro-Orbital Blood Plasma Protease | RIA | Mouse retro-orbital blood plasma | In Vivo | None | None | mGIPAnt‐1 inhibited the mouse GIP receptor with IC50 of 269 nM | |||
| 35688476 | 2022 | PEG-hUCN1 | 40 | Free | Amidation | Linear | L | Insertion of a cysteine residue at position 31 for pegylation PEG20 acetamide | Human UCN1 derivative | Treating Autoimmune disease | N.A. | 0.3 mg/kg | 13 | C57Bl/6J mice plasma protease | Laser capture/mass spectrometry | C57BL/6J mice plasma | In Vivo | None | None | At the CRHR1 receptor, the PEG-hUCN1 peptide was less potent than native CRH or UCN1 peptides with EC50 values of 47, 15, and 10 nM, respectively | |||
| 35688476 | 2022 | PEG-hUCN1 | 40 | Free | Amidation | Linear | L | Insertion of a cysteine residue at position 31 for pegylation | Human UCN1 derivative | Treating Autoimmune disease | N.A. | 1 mg/kg | 17 | C57Bl/6J mice plasma protease | Laser capture/mass spectrometry | C57BL/6J mice plasma | In Vivo | None | None | At the CRHR2 receptor, the PEG-hUCN1 peptide was also less potent than UCN2 or UCN1 peptides with EC50 values of 80, 10, and 6.6 nM, respectively | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 124 | Human Plasma Protease | LC-MS | Human plasma with Normal hepatic function | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 131 | Human Plasma Protease | LC-MS | Human plasma with Mild hepatic impairment | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 116 | Human Plasma Protease | LC-MS | Human plasma with Moderate hepatic impairment | In Vivo | None | None | N.A. | |||
| 35674880 | 2022 | Tirzepatide | 39 | Free | Free | Linear | L | C20 fatty diacid conjugation at the side chain of the Lys20, Aib = alpha-amino isobutyric acid at position 2,13 | GLP-1 analogs | Antidiabetes | Plasma concentrations of tirzepatide measured pre-dose, and at 8, 12, 24, 48, 72, 96, 168, and 336 hours post-dose | 5 mg | 122 | Human Plasma Protease | LC-MS | Human plasma with Severe hepatic impairment | In Vivo | None | None | N.A. | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 15.3 μg/kg | 0.498 ± 0.0100 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 5 μg/kg | 3.33 ± 1.57 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 20 μg/kg | 2.83 ± 1.42 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | N.A. | 60 μg/kg | 2.47 ± 0.571 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | 1 day | 20 μg/kg | 3.07 ± 1.28 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35646543 | 2022 | TB001 | 40 | Free | Amidation, GGPSSGAPPPS introduced in the C-terminal | Cyclic (R17-D21 Lactam Bridge) | Mix | D serine modifcation at 2, side chain modification at Lysine (n=12, R=CH3) | GLP-1 and GCG chimera analog | Treatment of Multiple Causes of Hepatic Fibrosis | 7 days | 20 μg/kg | 1.94 ± 0.305 | Rhesus monkeys plasma protease | HPLC–MS/MS | Rhesus monkeys plasma | In Vivo | None | None | GCGR EC50(nmol/L) = 0.01, GLP-1R EC50(nmol/L) = 0.04 | |||
| 35458385 | 2022 | EK1 | 36 | Free | Free | Linear | L | None | Expression in E. coli | Pan-cov fusion inhibitor | Serum samples were collected before (0 h) and after injection of EK1 (0.5 h, 1 h, 3 h, 7 h, and 12 h) or FL-EK1 (0.5 h, 1 h, 3 h, 7 h, 24 h, 48 h, 72 h, and 96 h) | 8.25 mg/kg | 1.8 ± 1.0 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | IC50(nM) = 69.0 ± 20.8 against B.1.1.7 (Alpha), IC50(nM) = 109.9 ± 25.3 against B.1.351 (Beta), IC50(nM) = 191.3 ± 17.0 against P.1 (Gamma), IC50(nM) = 190.6 ± 29.0 against B.1.617.2 (Delta), IC50(nM) = 135.6 ± 11.2 against B.1.525 (Eta), IC50(nM) = 107.1 ± 7.3 against B.1.617.1 (Kappa), IC50(nM) = 68.7 ± 25.4 against C.37 (Lambda), IC50(nM) = 236.8 ± 10.6 against B.1.1.529 (Omicron) | |||
| 35455421 | 2022 | T1144 | 37 | Free | Free | Linear | L | None | Fully or partially derived from the HIV-1 gp41 CHR domain | Antiviral (HIV fusion inhibitor) | Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested | 1.28 mg/kg | 7.48 ± 0.4 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | None | None | IC50(nM) = 3.9 against infection of HIV-1 IIIB (X4 tropic) strain | |||
| 35455421 | 2022 | T20 (enfuvirtide) | 36 | Free | Free | Linear | L | None | Derived from the natural sequence (aa 643–678) of the HIV-1 gp41 C-terminal heptad repeat (CHR) domain | Antiviral (HIV fusion inhibitor) | Blood samples were collected from the orbital sinus at 0, 0.5, 1.5, 3, 6, 9, 12, 24, 48, 72, 96 and 120 h after injection of the inhibitors tested | 1.26 mg/kg | 1.22 ± 0.2 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | None | None | IC50(nM)= 55.3 ± 2.4 against HIV-1 96USSN20 (X4/R5, A),IC50(nM) = 49.3 ± 4.9 against HIV-1 96USNG17 (X4, A), IC50(nM) = 50.1 ± 2.0 against HIV-1 90US_873 (R5, B), IC50(nM) =53.9 ± 4.3 against HIV-1 BZ167 (X4, B), IC50(nM) = 45.2 ± 3.2 against HIV-1 SE364 (R5, C), IC50(nM) = 46.9 ± 2.1 against HIV-1 PBL288 (R5, C), IC50(nM) = 77.1 ± 6.8 against HIV-1 92UG001 (X4/R5, D), IC50(nM) = 21.1 ± 1.1 against HIV-1 J32228M4 (R5, D), IC50(nM) = 55.6 ± 1.2 against HIV-1 DJ263 (R5, CRF02_AG), IC50(nM) = 61.2 ± 1.3 against HIV-1 CAM1475MV (R5, CRF02_AG) (infection on MT-4 cell) | |||
| 35414877 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Antidiabetes | At selected time points samples were taken: 5, 15, 30, 60, 120, 210, 300 mins | 1 μM | 35 | Human plasma protease | LC-MS | 80% pooled human Li-heparin plasma | In Vitro | PDB id: 5VAI | None | N.A. | |||
| 35180646 | 2022 | NPY1–36 | 36 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 4.66 ± 0.70 | Human plasma protease | LC-MS/MS | Human plasma after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY1–36 | 36 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 4.78 ± 1.07 | Human plasma protease | LC-MS/MS | Human plasma with 5 mg saxagliptin after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY3–36 | 34 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 26.9 ± 6.2 | Human plasma protease | LC-MS/MS | Human plasma after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35180646 | 2022 | NPY3–36 | 34 | Free | Amidation | Linear | L | None | Human derived | Vasoconstrictor | 168 min for a study day | N.A. | 25.5 ± 6.2 | Human plasma protease | LC-MS/MS | Human plasma with 5 mg saxagliptin after Heavy exercise | In Vivo | PDB id: 7RTA | None | N.A. | |||
| 35150805 | 2022 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 1200 nmol/kg | 0.137 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.42nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 2.5 µg/kg | N.A. | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 7.5 µg/kg | N.A. | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 15 µg/kg | 24.4 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In a phase II study, full PK sampling was performed at days 1, 10, 29, 85 and 183, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 60 (± 5 min), 90 (± 5 min), 120 (± 5 min) and 180 (± 5 min) min postdose | 30 µg/kg | 27 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at day 1 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 21 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at week 26 during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 26.6 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| 34431071 | 2022 | vosoritide | 39 | Free | Free | Cyclic (Cysteine (23->39)-Disulfide) | L | None | Analog of C-type natriuretic peptide | Treatment of Achondroplasia | In the phase III study, full PK sampling was performed at week 52, during which plasma samples were collected predose and at 5 (± 2 min), 15 (± 2 min), 30 (± 5 min), 45 (± 5 min), 60 (± 5 min), 90 (± 5 min) and 120 (± 5 min) min postdose | 15 µg/kg | 27.9 | Human plasma protease | ELISA | Human plasma | In Vivo | https://pubchem.ncbi.nlm.nih.gov/compound/119058036#section=2D-Structure | None | N.A. | |||
| N.A. | 2022 | Chem.37 (reference compound) | 33 | k=D-Lysine,Sar=N-terminal glycine, N£-octadecanoyl | Free | Linear | Mix | Aib substituitions at position 2 of semaglutide | Semaglutide Derivative | Antidiabetes | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 78 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| N.A. | 2022 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | GLP-1 receptor agonist | Blood samples (0.8 Ml) were taken via the second catheter at predetermined time points (0-3 weeks) | 10 nmol/kg | 69 (Terminal Half Life) | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vivo | None | EP 2021080747 W | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38 (4A) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2CHSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 9.4, 37 °C | N.A. | 6 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38(4B) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2NSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 9.4, 37 °C | N.A. | 15.8 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38 (4A) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2CHSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 7.4, 37 °C, | N.A. | 600 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35858423 | 2022 | MS-[Gln6,14]CNP-38(4B) | 38 | Free | Free | Linear | N.A. | Mod = (CH3)2NSO2-MS-BCN microsphere conjugation | Synthetic | Treatment of achondroplasia | pH 7.4, 37 °C, | N.A. | 1580 (Release Half Life) | N.A. | N.A. | N.A. | N.A. | None | None | N.A. | |||
| 35259149 | 2022 | Conjugate 2 | 31 | Free | Ethylene Diamine-modified chondroitin90 (CH) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | CH-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 25.3 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 9.9 nM | |||
| 35259149 | 2022 | Conjugate 2 | 31 | Free | Ethylene Diamine-modified chondroitin90 (CH) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | CH-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 100 nmol/kg | 30.3 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 9.9 nM | |||
| 35259149 | 2022 | Conjugate 3 | 31 | Free | Ethylene Diamine-modified heparosan (HPN) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | Hpn-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 33.6 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 7.0 nM | |||
| 35259149 | 2022 | Conjugate 3 | 31 | Free | Ethylene Diamine-modified heparosan (HPN) linked with C terminus of GLP-1C using linker C12 , (N-[λ-maleimidododecanoyloxy]-sulfosuccinimide ester (sulfo-LMDS, C12 derived from LMDS) | Linear | L | None | Hpn-Conjugated Glp-1C Peptide | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 100 nmol/kg | 25.8 (T1/2 Elimination Half Life) | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50 = 7.0 nM | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 0.25 mg | 116 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 0.5 mg | 124 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 1 mg | 106 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 2.5 mg | 120 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 5 mg | 123 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35651477 | 2022 | LY3298176 | 39 | Free | Amidation | Linear | L | Conjugated to a C20 fatty diacid moiety via a linker connected to the lysine residue at position 20 (C20 diacid-yGlu-(AEEA)2), two non-coded amino acid residues at positions 2 and 13 (Aib, α-amino isobutyric acid) | Fatty Acid Modified Peptide | Antidiabetes | Blood samples for PK assessment of LY3298176 in the SAD part were collected at predose, 8, 24, 48, 72, 96, 120, 168, and 336 hours postdose | 8 mg | 111 | Human plasma protease | HRAM LC/MS | Human plasma | In Vivo | https://pubmed.ncbi.nlm.nih.gov/30473097/ | None | GIPR, EC50 nM (cAMP potency) = 0.0224 | |||
| 35807558 | 2022 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety at Lys20 | Synthetic | Insulinotrophic | N.A. | 5 mg | 127 | Human plasma protease | N.A. | Human plasma With Multiple Dose (Participants Received 5‐Mg Tirzepatide Weeks 1‐8)(Japanese Participant With Type 2 Diabetes) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | N.A. | |||
| 35807558 | 2022 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety at Lys20 | Synthetic | Insulinotrophic | N.A. | 10 mg | 135 | Human plasma protease | N.A. | Human plasma With Multiple Dose (Participants Received 2.5‐Mg Tirzepatide, Weeks 1‐2; 5 Mg, Weeks 3‐4; 10 Mg, Weeks 5‐8) (Japanese Participant With Type 2 Diabetes) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | N.A. | |||
| 35807558 | 2022 | Tirzepatide | 39 | Free | Amidation | Linear | L | C20 fatty diacid moiety at Lys20 | Synthetic | Insulinotrophic | N.A. | 15 mg | 121 | Human plasma protease | N.A. | Human plasma With Multiple Dose(Participants Received 5‐Mg Tirzepatide, Weeks 1‐2; 10 Mg, Weeks 3‐6; 15 Mg, Weeks 7‐8) (Japanese Participant With Type 2 Diabetes) | In Vivo | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | N.A. | |||
| 35807558 | 2022 | PYY3-36 | 34 | Free | Free | Linear | L | None | Neuropeptide Y | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | PYY3−36 (methylamide) | 34 | Free | Methyl amide addition at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = >10,000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeTyr36]PYY3−36 | 34 | Free | Methylated Tyr36 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 370 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 4000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeArg35]PYY3−36 | 34 | Free | Methylated Arg35 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 620 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeGln34]PYY3−36 | 34 | Free | Methylated Gln34 at C terminus | Linear | L | Methylated Gln34 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 890 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 0.40 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [MeArg33]PYY3−36 | 34 | Free | Methylated Arg33 at C terminus | Linear | L | Methylated Arg33 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 2500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoTyr36]PYY3−36 | 34 | Free | β-homoTyr36 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 430 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 4000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoArg35]PYY3−36 | 34 | Free | β-homoArg35 at C terminus | Linear | L | None | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 680 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 6300 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoGln34]PYY3−36 | 34 | Free | β-homoGln34 at C terminus | Linear | L | β-homoGln34 modification | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 1200 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 160 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [β-homoArg33]PYY3−36 | 34 | Free | β-homoArg33 at C terminus | Linear | L | β-homoArg33 modification | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 230 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 200 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [Trp30, MeArg35]PYY3−36 | 34 | Free | MeArg35 at C terminus | Linear | L | Trp30 modification, Methylated Arg35 | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 980 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 2500 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | [Trp30,β-homoArg35]PYY3−36 | 34 | Free | β-homoArg35 at C terminus | Linear | L | Trp30 modification | PYY analogue | Antidiabetes, Antiobesity | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 570 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/ | None | Ki(nM) = 10,000 (In Vitro Binding of Peptide Analogues against Human Y1 receptor) | |||
| 35807558 | 2022 | GLP-1 | 31 | Free | Free | Linear | L | None | Glucagon | Treatment Of Type 2 Diabetes | The reaction was stopped at selected time points (5, 15, 30, 60, 90, 120, 150, 180, 210, 240, 270, and 300 min) | 1 μM | 46 | Minipigs plasma protease | LC-MS | Minipigs plasma | In Vitro | https://pubmed.ncbi.nlm.nih.gov/34647404/, https://pubmed.ncbi.nlm.nih.gov/30399314/, PDB id: 5VAI | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 1 | 34 | Free | Amidation | Linear | L | None | Derived from PYY | Antiobesity | Blood samples (0.8 ml) were taken either from the jugular vein using vacutainer or from the IV catheter not used for dosing according to one of the following schedules: Predose, and 5, 15, 30, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 192 h, 216 h, 240 h, 264 h and 288 h post dosing; or Predose, and 5, 30 min, 1 h, 2 h, 4 h, 7 h, 11 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 216 h, 264 h post dosing | 15 nmol/kg | 17 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.6 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 2 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 4 (C18 diacid-γGlu-2xAdo) | Derived from PYY | Antiobesity | Blood samples (0.8 ml) were taken either from the jugular vein using vacutainer or from the IV catheter not used for dosing according to one of the following schedules: Predose, and 5, 15, 30, 45 min, 1 h, 1.5 h, 2 h, 3 h, 4 h, 6 h, 8 h, 10 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 192 h, 216 h, 240 h, 264 h and 288 h post dosing; or Predose, and 5, 30 min, 1 h, 2 h, 4 h, 7 h, 11 h, 24 h, 48 h, 72 h,96 h, 120 h, 168 h, 216 h, 264 h post dosing | 15 nmol/kg | 14 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 10 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 3 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 5 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 8.8 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 25 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 7 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 9 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 12 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 40 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 8 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 10 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 8.4 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 13 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 9 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 11 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 11 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 1.3 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 11 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 13 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 13 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 16 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 20 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 22 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 36 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 4 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 21 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 23 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 19 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 2 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 27 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 29 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 39 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 32 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 28 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 76 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 500 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 31 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 33 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 56 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 50 for Y2 receptor | |||
| 34707178 | 2021 | PYY3-36 analogues 33 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 35 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 67 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 34 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 4 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 35 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 28 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 36 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 99 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 37 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 2 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 38 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 4 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 39 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 13 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 40 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 20 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 41 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 97 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 42 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 75 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 43 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 78 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 44 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 0.5 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 45 | 34 | Free | Amidation | Linear | L | Fatty acid conjugation at position 4, MeArg4 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 83 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 46 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 84 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 47 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 62 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 48 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 104 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 49 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 113 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 50 | 35 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 120 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 51 | 36 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 114 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 34707178 | 2021 | PYY3-36 analogues 52 | 36 | Free | Amidation | Linear | L | Fatty acid conjugation at position 30, Acetylation at Asn28 | Derived from PYY | Antiobesity | N.A. | 15 nmol/kg | 79 | Male göttingen minipigs plasma protease | LC-MS | Male göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 30 for Y2 receptor | |||
| 34506138 | 2021 | α/sulfono-γ-AApeptide hybrid analogue 15 | 35 | Free | Amidation | Linear | L | Substitution of L-serine at position 2 with α-aminoisobutyric acid (Aib), X1 = Structure given in paper | α/Sulfono-γ-AApeptide Hybrid Analogues of Glucagon | Regulating glucose homeostasis | blood samples were obtained at 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h after injection | 5 mg/kg | ~4 | C57Bl/6J female mice plasma protease | LC-MS/MS | C57BL/6J female mice plasma | In Vivo | None | None | EC50 (nM) = 0.86 (Bioactivity of α/Sulfono-γ-AApeptide Hybrid Analogues in Cre Luc Production Functional Assay) | |||
| 34459035 | 2021 | FLAGHIF1α | 34 | Free | Free | Linear | L | FLAG tag | Hypoxia-Inducible Factor 1-alpha | Role in survival, metabolism, and angiogenesis | N.A. | N.A. | ~50% Increase | Cells lysate protease | CHX assay, Western blotting | HEK293 Flp‐In T‐REx cell lysate after pevonedistat treatment | In Vitro | PDB id: 1LQB | None | N.A. | |||
| 34455010 | 2021 | ELA-32 | 32 | pGlu = Pyroglutamate | Free | Cyclic (Cys-Cys Disulfide Bond) | L | None | Derived from Zebrafish | Anticancer, Treatment of Cardiovascular Disease | Blood sample were withdrawn at time points: 0, 2, 5, 10, 15, 30, 60, 120, 240 min | 5 μg/mL | 47.2 ± 5.7 | Human plasma protease | LC–MS/MS | Human plasma | In Vitro | None | None | N.A. | |||
| 34455010 | 2021 | ELA-32 | 32 | pGlu = Pyroglutamate | Free | Cyclic (Cys-Cys Disulfide Bond) | L | None | Derived from Zebrafish | Anticancer, Treatment of Cardiovascular Disease | Blood sample were withdrawn at time points: 0, 2, 5, 10, 15, 30, 60, 120 min | 5 μg/mL | 44.2 ± 3 | Human kidney homogenate protease | LC–MS/MS | Human kidney homogenate | In Vitro | None | None | N.A. | |||
| 34450223 | 2021 | GLP-2DARPin | 31 | Genetic fusion of modified GLP-1 to the N-terminal of DARPins through a flexible linke (GGGGS)3 further DARPin linked with another DARPin using PT-linker | Free | Linear | L | FITC labeled | GLP-1 analogs | Antidiabetes | At 0.5, 2, 4, 7, 10, 24, 36, 48 and 72 h after injection, 20 μL of blood was collected | 2 mg/mL | 52.3 ± 4.6 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Glucose-lowering effect of GLP-DARPin was more potent than that of GLP-2DARPin, EC50 of GLP-2DARPin was 0.51 ± 0.04 nM | |||
| 34450223 | 2021 | GLP-DARPin | 31 | Genetic fusion of modified GLP-1 to the N-terminal of DARPins through a flexible linke (GGGGS)3 | Free | Linear | L | FITC labeled | GLP-1 analogs | Antidiabetes | At 0.5, 2, 4, 7, 10, 24, 36, 48 and 72 h after injection, 20 μL of blood was collected | 2 mg/mL | 18.0 ± 2.8 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Glucose-lowering effect of GLP-DARPin was more potent than that of GLP-2DARPin, EC50 of GLP-2DARPin was 9.06 ± 0.15 nM | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1.1 | Human plasma protease | N.A. | Human adult plasma (in Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1.24 | Human plasma protease | N.A. | Human adult plasma (in Non-Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 0.89 | Human plasma protease | N.A. | Human pediatrics plasma (in Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34402197 | 2021 | Teduglutide | 33 | Free | Free | Linear | L | None | GLP-2 analogue | Treatment of Short Bowel Syndrome | N.A. | 0.05 mg/kg | 1 | Human plasma protease | N.A. | Human pediatrics plasma (in non - Japanese patients with SBS) | In Vivo | DB id: DB08900 | None | N.A. | |||
| 34201398 | 2021 | [L6-optP7]-Mco | 35 | Free | Free | Cyclic(Cys-Cys Multiple Disulfide Loops) | L | None | Synthetic | Antimicrobial | For 0, 0.5, 1, 3, 6, and 24 h at 37 °C | 100 μM | 435 | Human serum protease | UPLC-MS | Human serum | In Vitro | None | None | MIC(µM) = 62 for Pseudomonas aeruginosa in growth media MH,MIC(µM) = 62 for E.coli in growth media MH,MIC(µM) = 62 for K. pneumoniae in growth media MH,MIC(µM) = 62 for A. baumannii in growth media MH,MIC(µM) > 62 for VRE in growth media MH,MIC(µM) > 62 for MRSA in growth media MH | |||
| 34048741 | 2021 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Salivary gland of the lizard Heloderma suspectum | Antidiabetes | Blood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h | 0.07 mg/kg | 0.32 ± 0.04 | Male SD rats plasma protease | ELISA | Male SD rats plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 34048741 | 2021 | M4 | 40 | Free | Cys addition at C terminal | Linear | L | M, R amino acid substitutions | Synthetic | Antidiabetes | Blood samples were collected from the lateral tail vein at 0, 0.083, 0.25, 0.5, 1, 2, 3, 4, 6, 8 and 10 h | 0.07 mg/kg | 1.80 ± 0.23 | Male SD rats plasma protease | ELISA | Male SD rats plasma | In Vivo | None | None | EC50(nM) = 38.49 ± 4.58 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 33969456 | 2021 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples for PK assessment were obtained during the first 9 days of dosing (7–45 samples per subject) and following the last dose on day 10 (16–38 samples per subject) | N.A. | 158 | Human plasma protease | LC-MS | Human plasma (Healthy subjects) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/ | None | N.A. | |||
| 33969456 | 2021 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples for PK assessment were obtained during the first 9 days of dosing (7–45 samples per subject) and following the last dose on day 10 (16–38 samples per subject) | N.A. | 146 | Human plasma protease | LC-MS | Human plasma (Subjects with T2D) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/ | None | N.A. | |||
| 33894838 | 2021 | Cagrilintide | 37 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | Mix | LPPTNVGSNTP all D-amino acids, Lipidation on Lys1 | amylin analogue | Antiobesity | Blood samples for pharmacokinetic testing were collected before dosing at baseline (week 0) and at weekly visits, and after the last dose (week 19) at 4, 8, 12, 24, 48, 72, 96, 168, 336, 504, 672, 840, and 1008 h after dosing | 0·16 − 4·5 mg | 159 – 195 | Human plasma protease | N.A. | Human plasma | In Vivo | pubchem CID: 171397054 | None | N.A. | |||
| 33894838 | 2021 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples for pharmacokinetic testing were collected before dosing at baseline (week 0) and at weekly visits, and after the last dose (week 19) at 4, 8, 12, 24, 48, 72, 96, 168, 336, 504, 672, 840, and 1008 h after dosing | 2·4 mg | 145 – 165 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 33825469 | 2021 | Native Ex4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 0.72 ± 0.07 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33706686 | 2021 | TB01-3 | 39 | Free | 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 | ~1 | 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_8G37C-HSA | 31 | Free | HSA | Linear | L | Substituition of amino acid G 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 | 3.2 (T1/2a) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50= 1340 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33672039 | 2021 | GLP1_8G37C-HSA | 31 | Free | HSA | Linear | L | Substituition of amino acid G 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 | 9 ( T1/2b) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50= 1340 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 50 nmol/kg | 53.19 ± 1.42 | SD rats serum protease | LC-MS/MS | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 100 nmol/kg | 58.37 ± 4.51 | SD rats serum protease | LC-MS/MS | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 200 nmol/kg | 73.68 ± 6.52 | SD rats serum protease | LC-MS/MS | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 50 nmol/kg | 56.40 ± 2.71 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 100 nmol/kg | 63.15 ± 4.93 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33336763 | 2020 | LM06 | 33 | Free | Free | Linear | L | None | OXM analogs | Antidiabetes | The serum sample of SD rats and monkeys were collected at the time points of 0, 4, 8, 12, 24, 36, 48, 72, 96, 120, 144 and 168 h from the tails of SD rats and right fore of monkeys, respectively | 200 nmol/kg | 114.91 ±7.32 | Cynomolgus monkeys serum protease | LC-MS/MS | Cynomolgus monkeys serum | In Vivo | None | None | EC50 (nM) = 0.352 (Receptor activation of LM peptides for GLP-1R) | |||
| 33310780 | 2020 | NYBSP-4 | 34 | Acetylation | Amidation | Linear | L | 2-(7-octenyl)alanine-2-(4-pentenyl)alanine modifications | Derived from ACE2 | Antiviral | 0, 10, 30, 60, and 120 min | 1mM | >289 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | IC50 = 1.97 ± 0.14 μM in HT1080/ACE2 cells | |||
| 32844654 | 2020 | Peptide 4 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 10, 17 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | N.A. | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 2.3 ± 0.3 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 8 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 23, 30 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | N.A. | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 1.2 ± 0.1 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 11 | 34 | Free | Amidation | Linear | L | None | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | 1.2 | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 0.29 ± 0.03 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 13 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 10, 17 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | N.A. | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 0.62 ± 0.09 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 18 | 34 | Free | Amidation | Cyclic (Cys-Cys Disulfide Bond) | L | Cysteine substiution at 23, 30 | PYY analog | Antiobesity | Blood samples were collected at 0.25, 0.5, 0.75, 1, 1.17, 1.33, 1.5, 2, 4, 6, 8, 24, 30, and 48 h after the start of infusion | 0.033 mg/kg | 4.5 | Mouse plasma protease | UPLC-MS/MS | Mouse plasma | In Vivo | None | None | EC50 (nM) = 0.91 ± 0.08 for hNPY2R (cAMP) | |||
| 32844654 | 2020 | Peptide 11 | 34 | Free | Amidation | Linear | L | None | PYY analog | Antiobesity | Blood samples were collected between 0.25 and 48 h | 0.1 mg/kg | 1.21 | Rats plasma protease | UPLC-MS/MS | Rats plasma | In Vivo | None | None | EC50 (nM) = 0.29 ± 0.03 for hNPY2R (cAMP) | |||
| 32841660 | 2020 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1R agonist | Attenuates renal fibrosis | N.A. | 90 nmol/kg | 64.74 ± 3.06 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.11 (In vitro receptor activation profiles of GLP-1 peptides for GLP-1R) | |||
| 32812282 | 2020 | ACTH | 39 | Free | Free | Linear | L | None | Deriving from the pro-opimelanocortin (POMC) | Stimulates The Adrenal Cortex To Produce And Secrete Cortisol | 4 ◦C for 15 min | 40 μM | 250 | Human plasma protease | RP-HPLC | Human plasma | In Vitro | None | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 68.5 ± 12.0 µg/kg | 16.8±5.66 (Terminal Half Life) | (IP) corn oil treated rats plasma protease | ELISA | Corn oil treated rat plasma | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 64.5 ± 13.2 µg/kg | 24.5±0.05 (Terminal Half Life) | Untreated rats plasma protease | ELISA | untreated rats plasma | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 64.5 ± 13.2 µg/kg | 75.5 ± 17.9 (Terminal Half Life) | Untreated rats CSF protease | ELISA | untreated rats CSF | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32759365 | 2020 | hAβ40 | 40 | Free | Free | Linear | L | None | Synthesized in neurons and degraded in the brain and liver | Treatment of Alzheimer's diseases | Serial blood sampling (0.15 mL) was performed after IV injections via the carotid artery catheter at times 0, 0.5, 1, 2, 5, 10, 15, 30, 45, 60, 90, 120, 150, and 180 min post-dose | 68.5 ± 12.0 µg/kg | 47.9 ± 20.9 (Terminal Half Life) | (IP) corn oil treated rats CSF protease | ELISA | Corn oil treated rat CSF | In Vivo | pdb id: 8KEW | None | N.A. | |||
| 32736262 | 2020 | EX | 39 | Free | Amidation | Linear | L | None | Produced by the salivary glands of Gila monster | Antiobesity | Blood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio | 50 nmol/kg | 0.69 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32506501 | 2020 | ACTH | 39 | Free | Free | Linear | L | None | Derived from POMC | Stimulates the adrenal glands to release cortisol | 37 °C | 2 µM | 3.79 | Human plasma protease | Glo-sensor transfected cell-based luminescence assay | Human plasma | In Vitro | None | None | EC50 (M) = 1.54E-09 for MC1R-ACTH | |||
| 32506501 | 2020 | ACTH | 39 | Free | Free | Linear | L | None | Derived from POMC | Stimulates the adrenal glands to release cortisol | 37 °C | 2 µM | 86.33 | Human CSF protease | Glo-sensor transfected cell-based luminescence assay | Human CSF | In Vitro | None | None | EC50 (M) = 1.54E-09 for MC1R-ACTH | |||
| 32404523 | 2020 | PEG40-NC | 34 | Free | Free | Linear | L | PEGylation at Asn637 in native gp41 | Derived from the gp41 CHR | Therapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys | Blood samples (300 μl) were collected from the tail vein before administration and at different intervals after injection (3, 6, 9, 20, 23, 29, 48, 72, and 96 h) | 1.7 μmol/kg | 10.39 | Rats plasma protease | HIV inhibition assay | Rats plasma | In Vivo | None | None | [EC50] = 18.51 nM for PEG40-NC (antiviral activity) | |||
| 32404523 | 2020 | C34 | 34 | Free | Free | Linear | L | None | Derived from the gp41 CHR | Therapeutic Efficacy In Simian-Human Immunodeficiency Virus-Acutely Infected Rhesus Monkeys | Blood samples (300 μl) were collected from the tail vein before administration and at different intervals after injection (3, 6, 9, 20, 23, 29, 48, 72, and 96 h) | 1.7 μmol/kg | 0.6 | Rats plasma protease | HIV inhibition assay | Rats plasma | In Vivo | None | None | [EC50] = 18.51 nM for PEG40-NC (antiviral activity) | |||
| 32348108 | 2020 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 170 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | None | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32243137 | 2020 | OXM-1 | 37 | Free | Free | Linear | Mix | Incorporation of D-ser in place of L-ser at 2nd position | Derived from proglucagon | Antiobesity, Antisteatotic | N.A. | 40 μg/kg | 6 (Terminal Half Life) | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 10 for OXM-1 (in Vitro Potency of Stapled Peptides in Human GLP-1R- and GCGR-Mediated CRE-Luc Reporter Assays) | |||
| 32243137 | 2020 | O14 | 40 | Free | Addition of the 12 C-terminal residues of Ex-4 to a C-terminal truncated OXM, amidation | Linear | Mix | Two cysteine group conatins fatty acid moteity(L3 = Structure given in paper) , Incorporation of D-ser in place of L-ser at 2nd position | OXM analogs | Antiobesity, Antisteatotic | N.A. | 40 μg/kg | 8.3 (Terminal Half Life) | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.03 for O-14 (in Vitro Potency of Stapled Peptides in Human GLP-1R- and GCGR-Mediated CRE-Luc Reporter Assays) | |||
| 32075870 | 2020 | hGLP-2 | 33 | Free | Free | Linear | L | None | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 1 mg/kg | 6.4 ± 0.2 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.07 for hGLP-2 receptor | |||
| 32075870 | 2020 | Glepaglutide | 39 | Free | KKKKKK amino acids substiuitions at C terminal | Linear | L | G,E,T,S,L,A,A,A,A amino acid substuitions at positions 2,3,5,8,10,11,16,24,28 respectively | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 19 ± 1.9 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.03 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 16 ± 0.8 (Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.2 mg/kg | 159 ± 27(Elimination Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 474 ± 80 (Elimination Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.025 mg/kg | 782 ± 365 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 43 ± 4 (Elimination Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 6 h post injection | 0.100 mg/kg | 88 ± 11 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 1 mg/kg | 11.7 ± 1.4 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 5 mg/kg | 22.5 ± 1.3 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 1 mg/kg | 0.5 ± 0.1 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 5 mg/kg | 0.5 ± 0.0 (Terminal Half Life) | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.25 mg/kg | 32.4 ± 6.1 (Terminal Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Apraglutide | 33 | Free | Amidation | Linear | L | Gly2, Nle10, D-Phe11, Leu16 modification | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.15 mg/kg | 30.1 ± 3.1 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.24 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.25 mg/kg | 0.9 ± 0.1 (Terminal Half Life) | Male cynomolgus monkeys plasma protease | LC-MS/MS | Male cynomolgus monkeys plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 32075870 | 2020 | Teduglutide | 33 | Free | Free | Linear | L | G amino acid substituition at position 2 | Derived from hGLP-2 | Treatment of Short Bowel Syndrome | Blood samples were collected at multiple time points up to 169 h post injection | 0.15 mg/kg | 2.7 ± 0.8 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50(nM) = 0.09 for hGLP-2 receptor | |||
| 31996466 | 2020 | D6PV | 40 | Free | Free | Linear | L | Replaces 18A with a modified central region of apoC-II | Derived from apoC-II | TG-Lowering Effects | N.A. | 46.7 mg/kg | 3 (Initial Elimination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | Equilibrium dissociation constant (Kd) of D6PV binding to HDL was determined to be 18.5 μM | |||
| 31996466 | 2020 | D6PV | 40 | Free | Free | Linear | L | Replaces 18A with a modified central region of apoC-II | Derived from apoC-II | TG-Lowering Effects | N.A. | 46.7 mg/kg | 9 (Terminal Elimination Half Life) | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | Equilibrium dissociation constant (Kd) of D6PV binding to HDL was determined to be 18.5 μM | |||
| 31901754 | 2020 | Compound 16a | 39 | Free | Amidation | Linear | L | Amino acid residues located at 24 substituted by the residues of Exenatide in the same location, Position 16 was replaced by Cys for coupling hybrid peptides with fatty chains | OXM analogs | Antiobesity, Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48, 72 and 96 h time points, 100 μL of mixture was aliquoted | 1000 ng/mL | 71.79 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | EC50 = 3.8 ± 0.4 pM for mGLP1R | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 43 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 9.9 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 52 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 12 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 32 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 10 mg/kg | 8.3 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 38 (T1/2, b) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31479925 | 2020 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Gln28 modifcations | Exenatide analogs | Antidiabetes | Blood samples (w1.5 mL) were drawn before dosing and at 10, 20, 30, 40, 50, 60, 80, 100, 120, 150, and 180 min after dosing from the jugular vein | 5 mg/kg | 13 (T1/2, a) | Cat plasma protease | LC-MS/MS | Cat plasma (Diabetic) | In Vivo | PDB id: 7MLL | None | N.A. | |||
| N.A. | 2020 | HA-Aib-Linker-SEQ ID No. 5 | 40 | HA = Hyaluronic acid hydrogel linked with GLP-1 analogue | Amidation | Linear | Mix | Linker Z = Structure mentioned in patent, dSer substituitions at position 2 | GLP-1-Linker-Ha Conjugate | Antidiabetes, Antiobesity | Plasma sample were taken at 0,1,4,8,24,48 H And Once A Day On Day 3 to 21 at the same time | 0.623 mg/kg | 139 | Minipigs plasma protease | LC-MS/MS | Minipigs plasma | In Vivo | None | US 201715829596 A | EC50 hGLP-1R = 1.9 pM for Sequence No. 5 | |||
| 31805154 | 2019 | IBP-CP24 | 37 | IBP conjugation to the N-terminus of CP24 | 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 | 46.11 | Rhesus monkeys plasma protease | Sandwich ELISA | Rhesus monkeys plasma | In Vivo | None | None | IC50(nM) = 0.7±0.3 for IBP-CP24 in virus subtype A (92UG029) | |||
| 31774631 | 2019 | BAY55-9837 | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 0.31 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31774631 | 2019 | BAY-exosome | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 7.76 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31774631 | 2019 | BAY-exosome-SPION | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | N.A. | 5 mg/kg | 8.39 | Kunming mice plasma protease | ELISA | Kunming mice plasma | In Vivo | https://sci-hub.se/10.2337/diabetes.51.5.1453 | None | N.A. | |||
| 31580912 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | Fluorescence dye | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 1.6 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | PDB id: 7MLL | None | EC50(M) = 6.1 × 10−10 ± 9.3 × 10−11 | |||
| 31580912 | 2019 | Exenatide K12C | 39 | Free | Amidation | Linear | L | K12C modification, fluorescence dye | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 2.5 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 4.0 × 10−11 ± 1.4 × 10−12 for K12C-PEG 5KDa | |||
| 31580912 | 2019 | K12C-PEG 5kD | 39 | Free | Amidation | Linear | L | K12C modification, fluorescence dye, PEG(5KDa) conjugation at Lys27 | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 1.7 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 4.0 × 10−11 ± 1.4 × 10−12 | |||
| 31580912 | 2019 | K12C-PEG 40 kD | 39 | Free | Amidation | Linear / Branched | L | Fluorescence dye, PEG40 conjugation at Lys27 | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 5.5 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 1.0 × 10−10 ± 2.9 × 10−11 | |||
| 31580912 | 2019 | C40-PEG 40 kD | 40 | Free | Cys40 conjugation at C terminal, PEG(40 KDa) | Linear | L | Fluorescence dye | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 5.1 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 1.9 × 10−10 ± 7.1 × 10−11 | |||
| 31580912 | 2019 | K12C-PEG 10 kD-K12C | 39 | Free | Free | Linear | L | Lys27 conjugaged with (PEG(10KDa)-HGEGTFTSDLSCQMEEEAVRLFIEWLKNGGPSSGAPPPS) | Synthetic | Hypoglycemic Activity | Fluorescence intensity was monitored in nude mice by non-invasive live imaging at 0, 1, 2, 4, 8, 24, and 48 h | 1 mg/ml | 2.1 | Nude mice serum protease | Fluorescence assay | Nude mice serum | In Vivo | None | None | EC50(M) = 4.4 × 10−11 ± 4.9 × 10−12 | |||
| 31413801 | 2019 | PrRP31 analog 18-S4 | 31 | Free | Amidation | Cyclic (C6-C13 Disulfide Bond) | L | C6 and C13 linked with S4 = Structure given in paper, residue 8 modification with Nle, residue 23 modifcation with hArg | Prolactin releasing peptide analogs | Antiobesity | Blood samples (70 μL) were collected from retro-orbital or saphenous vein at the following time points: 0.25, 0.5, 1, 3, 7, 24, 48 and 72 h | 5 mg/kg | 8.44 | CD-1 female mice plasma protease | LC-MS | CD-1 female mice plasma | In Vivo | None | None | EC50 = 7.8nM towards GPR10 receptor | |||
| 31389463 | 2019 | OXM | 37 | Free | Free | Linear | L | None | Secreted postprandially by intestine L-cells | Antidiabetes, Antiobesity | blood was sampled pre-dose and at 0.5, 1, 2, 4, 8, 24, 48, 72, and 96 h post-dose | 30 nmoL/kg | 2.1 ± 0.6 | SD rats plasma protease | LC-MS, ELISA | SD rats plasma | In Vivo | pdb id: 7LLY_5 | None | EC50(nM) = 0.691 for Human GLP-1R | |||
| 31368418 | 2019 | EX | 39 | Free | Free | Linear | L | O=Ornithine | GLP-1 analogs | Antidiabetes | Blood samples were collected before and after administration at 1, 3, and 6 h and 1–35 d | 2 mg/kg | 2.59 ± 0.05 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The blood glucose levels of saline-treated controls remained at 20 mM, while EX or LA-EX rapidly decreased the levels of blood glucose to approximately 10 mM after administration, which were maintained for approximately 6 h | |||
| 31368418 | 2019 | LA-EX | 39 | EX acylation with LA (Lactic acid) | Free | Linear | L | O=Ornithine | GLP-1 analogs | Antidiabetes | Blood samples were collected before and after administration at 1, 3, and 6 h and 1–35 d | 2 mg/kg | 5.95 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | The blood glucose levels of saline-treated controls remained at 20 mM, while EX or LA-EX rapidly decreased the levels of blood glucose to approximately 10 mM after administration, which were maintained for approximately 6 h | |||
| 31480738 | 2019 | PEG2kC34 | 35 | 2 kDa PEG conjugated to the N-terminus of cC34 through Mal linker | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 fusion inhibitory peptides) | Blood samples (300 μL) were harvested from the tail vein before injection and at different time intervals after injection (0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10.0 and 24.0 h | 1.7 μmol/kg | 2.57 ± 0.71 | Rats plasma protease | N.A. | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC7343207/ | None | EC50 =4.14 ± 1.89 for NL4-3 strain | |||
| 31480738 | 2019 | PEG5kC34 | 35 | 5 kDa PEG conjugated to the N-terminus of cC34 through Mal linker | Free | Linear | L | None | Synthetic | Antiviral (HIV-1 fusion inhibitory peptides) | Blood samples (300 μL) were harvested from the tail vein before injection and at different time intervals after injection (0.5, 1.0, 2.0, 4.0, 6.0, 8.0, 10.0 and 24.0 h | 1.7 μmol/kg | 5.11 ± 3.54 | Rats plasma protease | N.A. | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC7343207/ | None | EC50 =4.59 ± 1.83 for NL4-3 strain | |||
| 31443263 | 2019 | LL-37 | 37 | Free | Free | Linear | L | None | Synthetic | Antiinflammatory (Treatment of Several Intestinal Inflammation Conditions) | 37 °C | N.A. | 242.47 ± 45.09 | 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 | |||
| 31278957 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | Labeled with Flamma® 675 vinylsulfone | Exendin-4 analogs | Antidiabetes | The fluorescence images of the mice were measured at 0, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 147 h after injection | 20 μg | 2.2 | Mouse body protease | In vivo imaging system | Mouse body | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 31235532 | 2019 | CNP-39 | 39 | Proline substituition (amino acid 1) | Free | Cyclic (1 Disulfide Bond) | L | Glycine (amino acid 2) modifcation | CNP derivative | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Samples from animals treated with the daily CNP-39 molecule were also obtained after the 1st and the 26th dose: at pre-dose, 0.08, 0.25, 0.5, 1, 2, and 4 hours postdose | 20 μg/kg per day for 26 weeks | 0.35 | Cynomolgus monkeys plasma protease | competitive radioimmunoassay | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31235532 | 2019 | TransCon CNP (CNP-38) | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | 4xPEG10KDa modification at Lys26 through transient linker | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Blood samples for CNP38 analysis were collected and analyzed following the 1st and the 26th dose at the following time points: 0 (prior to dosing), 6, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose | 40 μg/kg per week for 26 weeks | 92.6 | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31235532 | 2019 | TransCon CNP (CNP-38) | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | 4xPEG10KDa modification at Lys26 through transient linker | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | Blood samples for CNP38 analysis were collected and analyzed following the 1st and the 26th dose at the following time points: 0 (prior to dosing), 6, 12, 24, 36, 48, 72, 96, 120, 144, and 168 hours postdose | 100 μg/kg per week for 26 weeks | 86.7 | Cynomolgus monkeys plasma protease | HPLC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = <1 for TransCon CNP (NPR-C Affinity) | |||
| 31235532 | 2019 | CNP-38 | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | 4 days | 100 μg/ml | 12.6 ± 3.9 | Recombinant human NEP protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 100 (NPR-C Affinity) | |||
| 31235532 | 2019 | 5-kDa PEG-linker CNP-38 | 38 | PEG5KDa through permanent linker | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities Associated with Fibroblast Growth Factor Receptor 3–related Skeletal Dysplasias | 4 days | 100 μg/ml | Stable | Recombinant human NEP protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 199 ± 12 (NPR-C Affinity) | |||
| 31235532 | 2019 | 5-kDa PEG-linker CNP-38 | 38 | PEG5KDa through permanent linker | Free | Cyclic (1 Disulfide Bond) | L | None | CNP-38 analog | Treatment of Comorbidities associated with Fibroblast Growth Factor Receptor 3–Related Skeletal Dysplasias | 4 days | 100 μg/ml | 65.4 | Recombinant Human Nep Protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate = 83 ± 7 (NPR-C Affinity) | |||
| 31235532 | 2019 | 4x 10-kDa PEG-linker CNP-38 | 38 | Free | Free | Cyclic (1 Disulfide Bond) | L | PEG40KDa modification at Lys26 through permanent linker | CNP-38 analog | Treatment of Comorbidities associated with Fibroblast Growth Factor Receptor 3–Related Skeletal Dysplasias | 4 days | 100 μg/ml | Stable | Recombinant Human Nep Protease | HPLC-UV | Recombinant human NEP (2.5 mg/ml) + digest buffer (50 mM Tris-HCl, 10 mM NaCl, pH 7.4) | In Vitro | None | None | Ratio IC50 CNP-38/IC50 CNP-38 conjugate < 2 (NPR-C Affinity) | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 3 mg | 0.242 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 9 mg | 0.326 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 18 mg | 0.392 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 24 mg | 0.521 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31069381 | 2019 | Tozuleristide | 36 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35 Disulfide Linkage) | L | Fluorophore indocyanine green (ICG) at Lysine27 | Derived from chlorotoxin | Used for fluorescence imaging of tozuleristide in adult subjects with gliomas | Collected before dosing at 1, 5, 15,30, 60, and 120 min postdose, presurgery, and 24 h after surgery | 30 mg | 0.485 | Human serum protease | LC-MS/MS | Human serum | In Vivo | PubChem id: 121488172 | None | N.A. | |||
| 31038930 | 2019 | Exenatide | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples (ca. 0.6 mL) were collected from the posterior aorta 1, 2, 8, 24, 48, 72, 96, 120, and 168 h after administration | 25 nmol/kg | 0.9 | Mice plasma protease | ELISA | Mice plasma | In Vivo | PDB id: 7MLL | None | Exenatide presented similar GLP-1 activities with EC50 values of 1.1 | |||
| 35520704 | 2019 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected | 50 nmol/kg | 3.9 ± 0.3 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | EC50 = 0.72 ± 0.27 nM | |||
| 30901967 | 2019 | YIK-C16 | 37 | Free | palmitic acid (C16) was conjugated to the C-terminus of YIK (at Lys37) with a linker GSG between C16 and YIK | Linear | L | T639I mutation | HP23-E6-IDL analogue | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection 1, 3, 7, 11, 13, 15, 17, and 19 h for lipopeptide YIK-C16 | 5 mg/kg | 5.9 ± 3.2 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 69 ± 8 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of YIK-C16 against infection by HIV-1 mutants resistant to T20) | |||
| 30901967 | 2019 | YIK | 34 | Free | Free | Linear | L | T639I mutation | HP23-E6-IDL analogue | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides YIK | 5 mg/kg | 1.3 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 784 ± 32 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of YIK against infection by HIV-1 mutants resistant to T20) | |||
| 30901967 | 2019 | HP23-E6-IDL | 32 | Free | Free | Linear | L | None | Synthetic | Antiviral (Anti-Hiv Activity) | Mouse serum samples were collected before (0 h) and after injection (0.5, 1, 2, 4, and 6 h for peptides HP23-E6-IDL | 5 mg/kg | 1 | Mice serum protease | N.A. | Mice serum | In Vivo | None | None | IC50(pM) = 912 ± 29 in HIV-1 NL4-3 D36G (WT)(Inhibitory activities of HP23-E6-IDL against infection by HIV-1 mutants resistant to T20) | |||
| 30794654 | 2019 | ASB20123 | 39 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | C-type natriuretic peptide derivative | Treatment of Growth failure and Dwarfism | N.A. | 20 nmol/kg | 31.3 ± 4.8 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30794654 | 2019 | ASB20123 | 39 | Free | Free | Cyclic (C6-C22 Disulfide Bond) | L | None | C-type natriuretic peptide derivative | Treatment Of Growth Failure And Dwarfism | N.A. | 50 nmol/kg | 32.1 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | None | N.A. | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h | 100 nmoL/kg | 31.4 ± 1.6 | SD rats serum protease | ELISA | SD rats serum | In Vivo | PDB id: 1JRJ | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h | 200 nmol/kg | 31.7 ± 1.5 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | None | Exendin-4 analogs | Antidiabetes | Blood samples were collected at 0, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 48, 72,96, and 144 h | 400 nmol/kg | 30.7 ± 2.2 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Exendin-4 | Antidiabetes | Blood samples were collected at 0, 0.25, 0.5, 0.75, 1, 2, 4, 6,8, and 12 h after injection | 100 nmoL/kg | 1.7 ± 0.3 | SD rats serum protease | ELISA | SD rats serum | In Vivo | PDB id: 7MLL | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30309736 | 2018 | PE | 40 | Free | PEG(20k) | Linear | L | Introduction of Cys at C terminal of Exendin-4 | Exendin-4 analogs | Antidiabetes | For 33 consecutive days, after the first administration for 6 days,eight rats received PE (100 nmoL/kg, 200 mL, s.c.) once every 84 h | 100 nmoL/kg | 27.6 ± 5.1 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50 values of Exendin-4, those of PE to activate GLP-1R in vitro was slightly decreased by 6.9- fold | |||
| 30174173 | 2018 | GsMTx4 | 35 | Free | Free | Linear | L | None | Isolated from the venom of the spider Grammostola spatulata | Treatment of Duchenne Muscular Dystrophy | 6 times over 14 days – sacrifice on day 28 | 10 mg/kg | 1 | Mice plasma protease | LC-MS | Mice plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC2217226/ | None | 1 μM GsMTx4 in vitro experiments shows 0.1–5.0 μM effective in suppressing MSC activity in various disease models | |||
| 30170067 | 2018 | ES2-AF | 33 | ES2 | Free | Linear | L | None | Synthetic | Treatment of diseases caused by Diabetic Eye Disease, Rheumatoid Arthritis And Other Neo-Vascularization, Anti-Angiogenesis Activity | Blood samples were collected through the jugular vein at 5 min, 15 min, 30 min, 1 h, 2 h, 6 h, 12 h, 24 h, and 48 h after administration | 25 mg/kg | 2.785 | Wistar rats plasma protease | Fluorescence spectrometry | Wistar rats plasma | In Vivo | None | None | KD (mol· L−1) = 3.011 × 10−4 | |||
| 30170067 | 2018 | HA-ES2-AF | 33 | ES2-AF peptide was conjugated with HA by the formation of an amide linkage between the amino group of the ES2-AF peptide and the activated carboxyl of HA | Free | Linear | L | None | Synthetic | Treatment of diseases caused by Diabetic Eye Disease, Rheumatoid Arthritis And Other Neo-Vascularization, Anti-Angiogenesis Activity | Blood samples were collected through the jugular vein at 5 min, 15 min, 30 min, 1 h, 2 h, 6 h, 12 h, 24 h, and 48 h after administration | 25 mg/kg | 18.07 | Wistar rats plasma protease | Fluorescence spectrometry | Wistar rats plasma | In Vivo | None | None | KD (mol· L−1) = 4.779 × 10−10 | |||
| 30096651 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At 1, 2, 3, 4, 6, 12, 24 and 48 h after injection, three Kunming mice were sacrificed at each time point and blood samples (~200 mL) were collected through extracting eyeball | 50 nmol/kg | 3.6 ± 0.2 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | the potency of 6 was 5.2 times higher than liraglutide | |||
| 30096651 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Blood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin | 50 nmol/kg | 4.2 ± 0.3 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | the potency of 6 was 5.2 times higher than liraglutide | |||
| 30041153 | 2018 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 30041153 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 3 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 30041153 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 0.9 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Exenatide | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 30041153 | 2018 | Liraglutide | 31 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Attenuates Renal Fibrosis | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | >4 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 30023916 | 2018 | Conjugate 2 | 31 | CH90 linked by linker EDA–(LMDS) | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 25.3 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 9.9 nM | |||
| 30023916 | 2018 | Conjugate 2 | 31 | CH90 linked by linker EDA–(LMDS) | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 30.3 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 9.9 nM | |||
| 30023916 | 2018 | Conjugate 3 | 31 | Free | HPN50 linked by linker EDA–(LMDS) | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 33.6 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 7.0 nM | |||
| 30023916 | 2018 | Conjugate 3 | 31 | Free | HPN50 linked by linker EDA–(LMDS) | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | Blood samples were collected from the tail vein at 0, 12, 24, 48, 72, 96, 120, and 144 h postadministration | 300 nmol/kg | 25.8 (T1/2 Elimination Half life) | Mice plasma protease | ELISA | Mice plasma | In Vivo | None | None | EC50 = 7.0 nM | |||
| 30023916 | 2018 | CH10-conjugated peptides | 31 | Free | CH10 linked by linker | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 16 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 30023916 | 2018 | (CH30,CH40,CH70)-conjugated peptides | 31 | CH30/CH40/CH70 linker by linker | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 22 - 25 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 30023916 | 2018 | PEG30k-conjugated GLP-1C peptide | 31 | PEG30K | Free | Linear | L | Substituition of G for A at position 2 | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 17.5 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | EC50 = 5.2 nM | |||
| 30023916 | 2018 | 10 kDa PEG-modified GLP-1 | 31 | PEG10K | Free | Linear | L | None | Synthetic | Antidiabetes | 37 °C for 2 h | N.A. | 105.5 (T1/2 Elimination Half life) | 0.125 U/12.5 Μl C-Abc And 0.0125 U/12.5 Μl Chondroitinase Acii | HPLC | N.A. | In Vitro | None | None | N.A. | |||
| 29799205 | 2018 | 4i | 39 | Free | Free | Linear | L | X3 = structure given in paper | GLP-1 analogs | Antidiabetes | Serial blood samples (100–200 µL) were collected from fundus venous plexus in microcentrifuge tubes (EDTA containing) at 0, 1, 2, 3, 4, 6, 12, 24 and 48 h | 50 nmol/kg | 5.4 ± 1.0 | SD rats plasma protease | LC-MS/MS. | SD rats plasma | In Vivo | None | None | EC50(nM) = 0.88 ± 0.43 | |||
| 29799205 | 2018 | 5b | 39 | Free | Free | Linear | L | X4 = structure given in paper | GLP-1 analogs | Antidiabetes | Serial blood samples (100–200 µL) were collected from fundus venous plexus in microcentrifuge tubes (EDTA containing) at 0, 1, 2, 3, 4, 6, 12, 24 and 48 h | 50 nmol/kg | 11.0 ± 1.2 | SD rats plasma protease | LC-MS/MS. | SD rats plasma | In Vivo | None | None | N.A. | |||
| 29799205 | 2018 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 35.4 | SD rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | N.A. | |||
| 29799205 | 2018 | 4g | 38 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 21.5 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) =0.18 ± 0.02 | |||
| 29799205 | 2018 | 4h | 38 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 31.6 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.57 ± 0.19 | |||
| 29799205 | 2018 | 4i | 38 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 39.5 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) =0.88 ± 0.43 | |||
| 29799205 | 2018 | 4j | 38 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 24.1 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.31 ± 0.03 | |||
| 29799205 | 2018 | 4k | 38 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 30.1 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.68 ± 0.24 | |||
| 29799205 | 2018 | 4l | 38 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 40.5 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 2.09 ± 0.21 | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 156.4 | Human plasma protease | LC‐MS/MS | Human plasma (Normal hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 142.1 | Human plasma protease | LC‐MS/MS | Human plasma (Mild hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 146.7 | Human plasma protease | LC‐MS/MS | Human plasma (Moderate hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29693715 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | Blood samples were taken on day 1 at up to 30 minutes prior to the first administration of semaglutide and 1 hour after dosing; predose on days 2, 4, 6, 8, and 9; on day 10 at up to 30 minutes predose | 5 mg for 5 days followed by 10 mg for 5 days | 153.7 | Human plasma protease | LC‐MS/MS | Human plasma (Severe hepatic function) after 10th dosing | In Vivo | None | None | N.A. | |||
| 29673717 | 2018 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | 3.6 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | PDB id: 7MLL | None | EC50 (pM) = 1.8 ± 0.8 | |||
| 29673717 | 2018 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points | 1000 ng/mL | 15.4 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vitro | None | None | N.A. | |||
| 29673717 | 2018 | I-4 | 31 | Free | Amidation | Linear | L | Cys37-Gly8-GLP1(7-36) modification and fatty acid conjugation through Mal at Cys37 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) = 6.1 ± 1.9 | |||
| 29673717 | 2018 | I-5 | 31 | Free | Amidation | Linear | L | Cys37-Gly8-GLP1(7-36) modification and fatty acid conjugation through Mal at Cys37 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) = 9.3 ± 1.1 | |||
| 29673717 | 2018 | I-6 | 31 | Free | Amidation | Linear | L | Cys37-Gly8-GLP1(7-36) modification and fatty acid conjugation through Mal at Cys37 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) = 19.8 ± 2.1 | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 151.7 | Human plasma protease | LC–MS/MS | Human plasma (Normal renal function) | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC8736331/ | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 159.3 | Human plasma protease | LC–MS/MS | Human plasma (Mild renal function ) | In Vivo | None | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 162.8 | Human plasma protease | LC–MS/MS | Human plasma (Moderate renal function) | In Vivo | None | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 164.9 | Human plasma protease | LC–MS/MS | Human plasma (Severe renal function group) | In Vivo | None | None | N.A. | |||
| 29623579 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | GLP-1 analogs | Antidiabetes | After 10th dosing | 5 days of semaglutide 5 mg followed by 5 days of semaglutide 10 mg | 152.8 | Human plasma protease | LC–MS/MS | Human plasma (ESRD Renal function group) | In Vivo | None | None | N.A. | |||
| 29540315 | 2018 | GUB09-123 | 33 | Free | Amidation | Linear | L | None | Synthetic | GLP-1/GLP-2 co-agonist | Blood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point) | 800nmol/kg | 0.9 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | GLP-1R, EC50 (nM) = 0.07 | |||
| 29540315 | 2018 | GUB09-145 | 34 | Free | Amidation | Linear | L | Lipidation at Lys14 (C16-yE-) | GUB09-123 analogue | GLP-1/GLP-2 co-agonist | Blood samples were collected by decapitation of the animals at nine different time points after administration (0.25, 0.5, 0.75, 1, 2, 4, 6, 10 and 24 hours, n=3 for each time point) | 800nmol/kg | 2.7 | Mice plasma protease | LC-MS/MS | Mice plasma | In Vivo | None | None | GLP-1R, EC50 (nM) = 0.17 | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 0.5 mg | 145 | Human plasma protease | LC–MS/MS | Human plasma (Japanese subjects) | In Vivo | None | None | N.A. | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 1 mg | 163 | Human plasma protease | LC–MS/MS | Human plasma (Japanese subjects) | In Vivo | None | None | N.A. | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 0.5 mg | 159 | Human plasma protease | LC–MS/MS | Human plasma (Caucasian subjects) | In Vivo | None | None | N.A. | |||
| 29536338 | 2018 | Semaglutide | 31 | Free | Free | Linear | L | Aib modification at position 2, Lys26 side chain conjugated with (ADO-linker-Glu-C18) | Antidiabetes | GLP-1R agonist | Blood samples for pharmacokinetic assessment of semaglutide were taken before the first dose (0 h), for 1 week following a single 0.25 mg dose(6, 12, 18, 24, 30, 36, 42, 48, 60, 72, 84, 96, 120,144, 168 h), then weekly prior to the next dose(trough values), and for 5 weeks following thefinal dose (0 h then 6, 12, 18, 24, 30, 36, 42, 48,60, 72, 84, 96, 120, 144, 168, 336, 504, 672 and 840 h). | 1 mg | 167 | Human plasma protease | LC–MS/MS | Human plasma (Caucasian subjects) | In Vivo | None | None | N.A. | |||
| 29528634 | 2018 | GLP2-2G | 33 | Free | Free | Linear | L | Ala2 was substituted with Gly | GLP-2 analogue | Treatment of Short Bowel Syndrome | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 25 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.035 ± 0.003 | |||
| 29516741 | 2018 | Liraglutide | 32 | Free | Free | Linear | L | Lys-34 is replaced by Arg and Lys-26 is acylated with a C16 palmitic acid linkd with γGlu | GLP-1 analogs | Antidiabetes | Serial blood samples were collected at the 0, 0.083, 0.25, 0.5, 1, 2, 4, 7 and 24-h time points | 30 μg/kg | 6.59 | Monkeys plasma protease | LC-MS/MS | Monkeys plasma | In Vivo | None | None | N.A. | |||
| 29433929 | 2018 | CT105 | 38 | Amidation | Acetylation | Linear | L | None | Synthetic | Antiviral (against HIV Virus) | Serial blood samples were collected from each animal before injection and at 0.08, 0.25, 0.5, 1, 2, 4 and 8 h after injection | 6 mg/kg | 2.7 | Rats plasma protease | IC-ELISA | Rats plasma | In Vivo | None | None | IC50(nM) =0.26 against HIV variant R3A | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 117 | Human serum protease | ELISA | Human serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis in Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 30 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis In Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 60 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 29421564 | 2018 | HDL-SP | 34 | MPB-Mal modified, additional cysteine residue on N-terminus of SP | Free | Linear | L | None | Synthetic | Therapeutic Angiogenesis In Diabetic Hindlimb Ischemia | 0 to 72 h at 37°C | 5 nmol | 96 | Diabetic rats serum protease | ELISA | Diabetic rats serum | In Vitro | None | None | N.A. | |||
| 29029327 | 2017 | Alu-HCG | 31 | Free | HCG | Linear | L | None | Derived from the exonization of an Alu-J element in the glycoprotein hormone alpha (GPHA) gene | Role in Placental development | N.A. | 2 mg/ml | 82.3 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1 | 5 µg | 1.8 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1 | 5 µg | 1.6 | Human plasma protease | ELISA | Human plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 1 | 5 µg | 1.8 | Human plasma protease | ELISA | Human plasma with Metformin | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8 | 5 µg | 1.9 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8 | 5 µg | 1.3 | Human plasma protease | ELISA | Human plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 8 | 5 µg | 1.9 | Human plasma protease | ELISA | Human plasma with Metformin | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84 | 10 µg | 1.6 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28932995 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Synthetic | Antidiabetes | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84 | 10 µg | 1.8 | Human plasma protease | ELISA | Human plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28932995 | 2017 | rE-4 | 39 | Free | Deamidation at C terminal | Linear | L | None | Exendin-4 analogs | GLP-1R agonist | Blood samples for pharmacokinetic evaluation of rE-4 and exenatide were collected at specified times (0, 0.25, 0.5,0.75, 1, 1.5, 2, 3 and 4 h) on days 84 | 10 µg | 1.3 | Human plasma protease | ELISA | Human plasma | In Vivo | None | None | N.A. | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 14.9 ± 3.1 | Rats plasma protease | RIA | Rats plasma without NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 0.02 mg/kg | 12.7 ± 1.2 | Rats plasma protease | RIA | Rats plasma with NEP inhibitor | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28) | 34 | Free | Ghrelin (12-28) | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 11 nmol/kg | 15.03 ± 4.31 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | CNP(6-22)ghrelin(12-28) exhibited NPR-B activity within one-tenth of that observed for CNP(1-22) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22) | 34 | Ghrelin (12-28) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 12 nmol/kg | 17.75 ± 3.99 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28) | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22) | 34 | Ghrelin (12-28) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 13 nmol/kg | 14.86 ± 2.64 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The activity of ghrelin(12-28)CNP(6-22) was about ten-fold less potent than that of CNP(6-22)ghrelin(12-28) | |||
| 28899838 | 2017 | CNP(6-22)ghrelin(12-28)amide | 34 | Free | Ghrelin(12-28)amide | Cyclic (C1-C17 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 14 nmol/kg | 14.50 ± 0.85 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | The CNP(6-22)ghrelin(12-28)amide maintained agonist activity comparable to that of CNP(1-22) | |||
| 28800217 | 2017 | Peptide 22 | 34 | Free | Free | Linear | L | Ala5 substituition in GpTx-1 | derived from Grammostola porteri (Tarantula spider) (Lasiodora porteri) | Potently inhibits the voltage-gated sodium channels Nav1.7/Scn9A | At 0.5, 1, 1.25, 1.5,2,3, and 4 hours post-dose, 3 mice were euthanized and then blood samples were collected | 5 mg/kg | 0.605 | Mice plasma protease | LC-MS/MS | Mice serum | In Vivo | https://sci-hub.se/10.1021/jm501765v | None | IC50=0.58-10 nM for GpTx-1 | |||
| 28799326 | 2017 | GLP-1 | 31 | Free | Free | Linear | L | None | GLP-1 | Antidiabetes | Blood samples were collected from the tail vessel in time intervals of predose 0.5, 1, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 and 192 hours | 5 mg/kg | 0.03 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | PDB id: 5VAI | None | EC50 = 5.257*10-11 | |||
| 28771355 | 2017 | GLP-1 analogue 4 | 31 | Free | Free | Linear | L | K34R substituition at GLP-1, Conjugated with indomethacin via γGlu attached to the ε-amine of Lys26 of the GLP-1 analog | GLP-1 analogs | Antidiabetes | Blood sampled at eight time-points within 24 h | 5 mL/kg | 55 | Lean mice plasma protease | Luminescent Oxygen Channeling Immunoassay | Lean mice plasma | In Vivo | None | None | GLP-1R EC50 ± SEM (nM) = 0.068 ± 0.037 | |||
| 28771355 | 2017 | GLP-1 analogue 6 | 31 | Free | Diflunisal is linked to the GLP-1 peptide through its hydroxyl group | Linear | L | K34R substituition at GLP-1, at Lys20 indomethacin is linked through a γGlu residue-Lys, DIF=diflunisal, Dehydroxylation of DIF | GLP-1 analogs | Antidiabetes | Blood sampled at eight time-points within 24 h | 5 mL/kg | 299 | Lean mice plasma protease | Luminescent Oxygen Channeling Immunoassay | Lean mice plasma | In Vivo | None | None | GLP-1R EC50 ± SEM (nM) = 0.547 ± 0.211 | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | Chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.03 mg | 5.14 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC9488713/ | None | For human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | Chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.07 mg | 7.38 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | For human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.2 mg | 19.3 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 0.6 mg | 23.2 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 1.8 mg | 25.4 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 3.6 mg | 19.9 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28741871 | 2017 | RG7697 | 40 | Free | Acylated at a C-terminal lysine with a saturated C16 lipid | Cyclic (L14-E21, Q17-N24 Lactam Bridge) | L | Aib modification at position 2, 20 | chimera of GLP-1 and GIP peptides | Antidiabetes | RG7697 were collected in EDTA-containing tubes initially at predose, 1, 2, 4, 6, 8, 10, 12, 14, 16, 18, 20, 24, 30, 36, 48, 60, 72 and 96 hours post dose, and at follow-up visit (first 2 cohorts). In later cohorts, additional time points were collected at 2.5, 3 and 3.5 hours post dose, while the 96-hour sample was deleted | 5 mg | 15.3 / 15.7 (T1/2b- Appearant Terminal Half Life) | Human plasma protease | LC-MS | Human plasma | In Vivo | None | None | for human GLP-1 (EC50 = 5 pM) and GIP (EC50 = 3 pM) receptors | |||
| 28668697 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | 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 | 2.35 ± 0.23 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50(nM) = 1.79 ± 0.47 (EC50 values represent the concentration (nM) of agonists to simulate half-maximum GLP-1 receptor cAMP activation) | |||
| 28605180 | 2017 | MS-exenatide (MeSO2-) | 39 | Tetra PEG hydrogel linked with exenatide using linker MeSO2- | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.3 µmol/g | 244 | Mouse serum protease | LC-MS/MS | Mouse serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | MS-exenatide (-CN) | 39 | Tetra PEG hydrogel linked with exenatide using linker -CN | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.4 µmol/g | 730 | Mouse serum protease | LC-MS/MS | Mouse serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | MS-exenatide (MeSO2-) | 39 | Tetra PEG hydrogel linked with exenatide using linker MeSO2- | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.3 µmol/g | 310 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | MS-exenatide (-CN) | 39 | Tetra PEG hydrogel linked with exenatide using linker -CN | Amidation | Linear | L | None | Exenatide analogs | Antidiabetes | Blood samples (300 µL) were drawn at 0, 1, 2, 4, 8, 24, 48, 72, 120, 168, 240, 336, 432, 504, 600, 672 h for both linkers and additional samples were obtained at 840, 1008, 1176, 1344, 1512, 1680, 1848, and 2016 h for the linker with Mod = CN | 1.4 µmol/g | 880 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 80 µg/mL | 18 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 for exenatide | |||
| 28605180 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 80 µg/mL | 50 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 0.21 ±0.0 | |||
| 28605180 | 2017 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Substituiting Asn28 with Gln28 | Exenatide analogs | Antidiabetes | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 49 µg/mL | 17 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 11 ±3.7 | |||
| 28605180 | 2017 | [Gln28]exenatide | 39 | Free | Amidation | Linear | L | Substituiting Asn28 with Gln28 | Exenatide analogs | Antidiabetes | Blood samples were drawn pre-dose and at 10 min, 30 min, 1 h, 2 h, 3 h, 4 h, 6 h, 8 h and 24 h after dosing | 49 µg/mL | 48 | Rats serum protease | LC-MS/MS | Rats serum | In Vivo | PDB id: 7MLL | None | IC50(nM) = 11 ±3.7 | |||
| 28522195 | 2017 | [Gly2]GLP-2 | 33 | Free | Free | Linear | L | Ala2 to Gly2 | GLP-2 analogue | Treatment of Short Bowel Syndrome | Blood samples were collected from the tail vein at 0, 1, 2, 3, 4, 5,6, 9 and 12 h after administration | 2 mg/mL | 1.62 (Terminal Half Life) | Rats plasma protease | N.A. | Rats plasma | In Vivo | None | None | EC50 values of [Gly2]GLP-2 = 8.40 nM | |||
| 28522195 | 2017 | native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | Blood samples were collected from the tail vein at 0, 1, 2, 3, 4, 5,6, 9 and 12 h after administration | 2 mg/mL | 4.59 (Terminal Half Life) | Rats plasma protease | N.A. | Rats plasma | In Vivo | None | None | EC50 values of GLP-2 = 2.58 nM | |||
| 28457895 | 2017 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 1 hour | 25 nmol/kg | ~0.35 | ICR mice retro-orbital sinus protease | Exenatide ELISA | ICR mice retro-orbital sinus | In Vivo | PDB id: 7MLL | None | both exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity | |||
| 28437610 | 2017 | m-exendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | N.A. | 25 nmol/kg | 43.11 | Murine plasma protease | ELISA | Murine plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28437610 | 2017 | Native Ex4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | N.A. | 25 nmol/kg | 1.9 | Murine plasma protease | ELISA | Murine plasma | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 28389388 | 2017 | PEG-HsTX1[R14A] | 34 | PEGylation | Amidation | Cyclic (C3-C24, C9-C29, C13-C34 Disulfide Linkage) | L | Substituting arginine 14 with alanine | From scorpion Heterometrus spinnifer | Immunomodulation in Inflammatory Arthritis | 2 hours | 1 mg/kg | 37.3 | Lewis rats serum protease | Anti-PEG ELISA | Lewis rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3968461/ | None | IC50 of 35.9 ± 6.3 nM | |||
| 28356733 | 2017 | SCD | 32 | Free | Chitosan-modified SeNP (SC) | Linear | L | None | Peptide-conjugated selenium nanoparticles | Antidiabetes | Orbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing | 1 mg/kg | 14.12 | DB/DB mice orbital blood protease | LC-MS/MS | DB/DB mice orbital blood sample | In Vivo | None | None | IC50 of SC for INS-1 cells was 66.10 μM | |||
| 28356733 | 2017 | DBAYL | 32 | Free | Free | Linear | L | None | PACAP-derived peptide | Antidiabetes | Orbital blood was collected at each time point before dosing and from 0.5 to 24 h post dosing | 1 mg/kg | 1.98 | DB/DB mice orbital blood protease | LC-MS/MS | DB/DB mice orbital blood sample | In Vivo | None | None | EC50 of DBAYL at VPAC1 was 804 nM | |||
| 28209419 | 2017 | Native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | N.A. | 8 μg/kg | ~120 | Human plasma protease | GLP-2 (1–33) specific radioimmunoassay | Adult human plasma | In Vivo | PDB id: 2L63 | None | N.A. | |||
| 28209419 | 2017 | Native GLP-2 | 33 | Free | Free | Linear | L | None | Glucagon | Treatment of Short Bowel Syndrome | Samples were taken prior to GLP-2 administration and at 60, 90 and 180 min post injection on Day 3 of therapy or Day 42 | 2.5 μg/kg | ~45 | Human plasma protease | GLP-2 (1–33) specific radioimmunoassay | Infant human plasma | In Vivo | PDB id: 2L63 | None | N.A. | |||
| 27689406 | 2017 | GLP-1 | 31 | Free | Free | Linear | L | None | Synthetic | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 1.2 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | PDB id: 5VAI | None | N.A. | |||
| 27689406 | 2017 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Exendin-4 | Antidiabetes | A total of 19 other samples were taken at the following time points from the beginning of peptide infusion: 0, 30, 35, 40, 45,50, 55, 60, 62, 64, 66, 68, 70, 75, 80, 85, 90, 95, and 100 min | 30 nmol/ml | 35.1 | Surgical rats plasma protease (Wistar Rat) | RIA | Surgical rats plasma (Wistar rat) | In Vivo | PDB id: 7MLL | None | EC50 (pM) = 1.8 ± 0.8 | |||
| 28953210 | 2017 | 99mTc-exendin(9-39) | 31 | 99Mtc Radiolabeled | Free | Linear | L | None | Exendin4 analogs | Antidiabetes | Whole-body images from four healthy individuals were acquired at 20 min, 2, 6, and 24 h after 99mTc-exendin(9-39)/octreotide administration | N.A. | 1.2 (T1/2 a- Fast ) (Activity Half Life) | Human blood protease | N.A. | Human blood | N.A. | PDB id: 7MLL | None | N.A. | |||
| 28953210 | 2017 | 99mTc-exendin(9-39) | 31 | 99Mtc Radiolabeled | Free | Linear | L | None | Exendin4 analogs | Antidiabetes | Whole-body images from four healthy individuals were acquired at 20 min, 2, 6, and 24 h after 99mTc-exendin(9-39)/octreotide administration | N.A. | 8.7 (T1/2 b- Slow)(Activity Half Life) | Human blood protease | N.A. | Human blood | N.A. | PDB id: 7MLL | None | N.A. | |||
| 28953210 | 2017 | 99mTc-exendin(9-39) | 31 | 99Mtc Radiolabeled | Free | Linear | L | None | Exendin4 analogs | Antidiabetes | Whole-body images from four healthy individuals were acquired at 20 min, 2, 6, and 24 h after 99mTc-exendin(9-39)/octreotide administration | N.A. | 1.7(T1/2 b-Slow)(Activity Half Life) | Human blood protease | N.A. | Human blood | N.A. | PDB id: 7MLL | None | N.A. | |||
| 28870261 | 2017 | EXT-Sol | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | At specific time 0, 0.25, 0.5, 1,1.5, 2, 3, 4, 6, 8 h after injection | 50 μg/kg | 0.22 ± 0.03 (T1/2a- Distribution) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28870261 | 2017 | EXT-SBA-15 | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | Collected at 0, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120 h | 50 μg/kg | 0.26 ± 0.05(T1/2a- Distribution) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28870261 | 2017 | EXT-Sol | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | At specific time 0, 0.25, 0.5, 1,1.5, 2, 3, 4, 6, 8 h after injection | 50 μg/kg | 0.60 ± 0.08(T1/2b-Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 28870261 | 2017 | EXT-SBA-15 | 39 | Free | Free | Linear | L | Substituition of amino acids G,L,K,Q,M,E,E,V,R,L,E,K,N,O,P,S,S,G,A,P,P,P,S | Exendin4 analogs | Antidiabetes | Collected at 0, 0.5, 1, 1.5, 2, 3, 5, 8, 12, 24, 36, 48, 72, 120 h. | 50 μg/kg | 14.53 ± 0.70(T1/2b-Elimination Half Life) | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | None | None | EXT-SBA-15 exhibited efficacy that is comparable to EXT-Sol on 5 h | |||
| 27240277 | 2016 | ENF | 36 | Free | Free | Linear | L | None | Synthetic | Antiviral (against HIV infection) | N.A. | 1.7 μmol/kg | 1.5 ± 0.1 (Elimination Half Life) | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | EC50(nM) = 3 ± 0 | |||
| 27240277 | 2016 | PEG2k-ENF | 36 | mPEG(2KDa)-Maleimide | Free | Linear | L | None | Synthetic | Antiviral (against HIV infection) | N.A. | 1.7 μmol/kg | 16.1 ± 3.8 (Elimination Half Life) | SD rats plasma protease | HPLC | SD rats plasma | In Vivo | None | None | EC50(nM) = 4 ± 0 | |||
| 27232339 | 2016 | GLP-1-IgG2σ-Fc | 31 | Free | Human IgG2σ constant heavy-chain linked via a peptide linker (GGGSGGGSGGGS) with human GLP-1 (A8G/G26E/R36G) at C terminal | Linear | L | GLP-1 variant (A8G/G26E/R36G) linked to the human IgG2σ constant heavy-chain by a peptide linker (GGGSGGGSGGGS) | GLP-1 analogs | Antidiabetes | Blood (0.6 mL) was collected from the foreleg vein immediately pre-administration (time 0), and at 2, 4, 8, 12, 48, 72, 96, 192,240, and 288 h after a single subcutaneous injection of GLP-1-IgG2σ-Fc | 0.1 mg/kg | 57.1 ± 4.5 | Cynomolgus monkeys plasma protease | ELISA | Cynomolgus monkeys plasma | In Vivo | PDB id: 5VAI | None | Cells incubated with medium containing 16.8 mM glucose secreted significantly more insulin in the presence of 10 nM (5.2 ± 0.4 ng/mL) and 100 nM (7.3 ± 0.3 ng/mL) GLP-1-IgG2σ-Fc, as compared with control cells (2.5 ± 0.5 ng/mL) | |||
| 27166982 | 2016 | ADM analogue 3 | 39 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (C3-C8 Disulfide Linkage) | L | None | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 9.7 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 17 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 84.6 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 20 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | Nα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 126.2 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 3 | 39 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (C3-C8 Disulfide Linkage) | L | None | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 3.3 | Porcine liver homogenate protease | RP-HPLC | Porcine liver homogenate | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27166982 | 2016 | ADM analogue 20 | 38 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (Dpr3-E8 Lactam Bridge) | L | Nα-Methylation of Lysine at position 33, K1, Dpr3 = Diaminopropionic acid,E8 substituitions and Pam = Palmitoylation modification at side chain of Lys1 | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 38 | Porcine liver homogenate protease | RP-HPLC | Porcine liver homogenate | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 27155328 | 2016 | I-3 | 38 | Free | Amidation | Linear | L | X3(Fatty acid structure given in paper) linked with Ser11 | Exendin-4 analogs | Antidiabetes | At 0, 1, 2, 4, 6, 8, 12, 24, 36, 48 and 72 h time points, 100 lL mixture was aliquoted | 1000 ng/mL | 35.6 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vitro | None | None | EC50(pM) =38.47 ± 9.86 | |||
| 26905040 | 2016 | WT-EX4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | 37 °C | 200 μg/mL | 16.9 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-2K | 40 | Free | PEG(2KDa) linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antidiabetes | 37 °C | 200 μg/mL | 69.2 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-5K | 40 | Free | PEG(5KDa) linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antidiabetes | 37 °C | 200 μg/mL | 62.8 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-20K | 40 | Free | PEG(20KDa) linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antidiabetes | 37 °C | 200 μg/mL | 69.7 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | WT-EX4 bound to GLP-1R, with a dissociation constant of Kd(app) ≈ 0.142 nM | |||
| 26905040 | 2016 | EX4-50K | 40 | Free | (PEG(50KDa))3 linked with Ex-4 through Mal (Maleimide) | Linear | L | None | Exendin-4 analogs | Antisepsis | 37 °C | 200 μg/mL | 234.2 | Mice plasma protease | RP-HPLC | CLP-induced septic mice plasma | In Vitro | None | None | A dissociation constant of Kd(app) ≈ 0.159 nM was obtained for the interaction between GLP-1R and EX4-50 | |||
| 26877782 | 2016 | Native Extendin-4 | 39 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At predetermined times (0, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96 h), blood samples were collected from tail vein of each animal | 25 nmol/kg | 5.16 ± 5.23 | DB/DB mice plasma protease | Exendin-4 EIA | DB/DB mice plasma | In Vivo | None | None | IC50 = 0.21 ± 0.08 nM | |||
| 26877782 | 2016 | Abextide | 40 | Free | tEB (Truncated Evans blue) dye linked via Maleimide | Linear | L | Cys addition at C terminal of Ex4 | Exendin-4 analogs | Antidiabetes | At predetermined times (0, 1, 2, 4, 6, 8, 12, 24, 48, 72, 96 h), blood samples were collected from tail vein of each animal | 25 nmol/kg | 36.28 ± 7.01 | DB/DB mice plasma protease | Exendin-4 EIA | DB/DB mice plasma | In Vivo | None | None | IC50 = 0.18 ± 0.06 nM | |||
| 26869426 | 2016 | HsTX1[R14A] | 34 | Free | Amidation | Cyclic (C3-C24, C9-C29, C13-C31 Disulfide Linkage) | L | R14A substituitions | Isolated from the scorpion Heterometrus spinnifer | Treatment of Autoimmune Diseases | Blood samples (500 mL) were collected at 5, 15,30, 60, 120, 180, 240, and 300 min | 2 mg/kg | 79.6 ± 6.5 (Terminal elimination half life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/instance/2144240/pdf/10631983.pdf | None | IC50 value of 45 pM (affinity for Kv1.3 channels) | |||
| 26835125 | 2016 | IONP-HA-GEM-CTX-Cy5.5 | 36 | Conjugation of HA into CTX at N terminal in IONP-HA-GEM | Cy5.5 labeled | Linear | L | None | Synthetic | Glioblastoma therapy | At 1.5, 3, 6, 16, 24 and 48 h after injection, blood (20-50 L) was collected from tail veins | 2 mg/ml | ~2.8 | BALB/c mice blood plasma protease | Fluorescence spectrometry | BALB/c mice blood plasma | In Vivo | PDB id: 1CHL | None | N.A. | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 10.1 ± 0.5 (Elimination Half Life) | Human blood plasma protease | RIA | Human blood plasma with 2 × 100 mg sitagliptin | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 9.4 ± 0.8 (Elimination Half Life) | Human blood plasma protease | RIA | Human blood plasma | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Blood was sampled at t = −15, 0, 60, 90, and 120 min relative to start of the infusion as well as frequently after the infusion was discontinued at t = 122, 125, 130, 135, 140, 150, 165, 195, and 240 min | PYY infusions for 2 h on four separate days of either 1) 1.6 pmol·kg−1·min−1 PYY1–36, 2) 1.6 pmol·kg−1·min−1 PYY1–36 after DPP-4 inhibition, 3) 0.8 pmol·kg−1·min−1 PYY3–36 | 14.9 ± 1.3 (Elimination Half Life) | Human blood plasma protease | RIA (total PYY assay) | Human blood plasma | In Vivo | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Samples were taken regularly (t = 0, 0.5, 1, 2, 3, 4, 6, 8, 21, and 24 h) | 0.6 pmol/mL | 22.8 ± 8.0 − 3.6 ± 0.6 | Human blood plasma protease | RIA (when correcting for NH2-terminal degradation) | Human blood with EDTA, aprotinin (500 KIE/ml), and the DPP-4 inhibitor valine pyrrolidide (0.01 mmol/l, final concentration (when correcting for NH2-terminal degradation) | In Vitro | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26818056 | 2016 | PYY1–36 | 36 | Free | Amidation | Linear | L | None | Released from enteroendocrine cells | Anorexic effects | Samples were taken regularly (t = 0, 0.5, 1, 2, 3, 4, 6, 8, 21, and 24 h) | 0.6 pmol/mL | 8.6 ± 3.6 | Human blood plasma protease | RIA (when we corrected for NH2-terminal degradation) | Human blood plasma with EDTA, aprotinin (500 KIE/ml), and the DPP-4 inhibitor valine pyrrolidide (0.01 mmol/l, final concentration (when correcting for NH2-terminal degradation) | In Vitro | https://febs.onlinelibrary.wiley.com/doi/epdf/10.1111/j.1432-1033.1984.tb08298.x | None | The human Y2 receptor was activated by hPYY3–36 with an EC50 value of 3.5 nmol/l | |||
| 26808305 | 2016 | αAnalogue | 37 | Fatty acid moiety attached to Ser1 at N terminal | Amidation | Cyclic (Disulfide Bridge Between Positions 2 And 7) | L | None | CGRP analogue | Vasodilatory effect | Blood (200 µl) was sampled from vena sublingualis from anaesthetised rats at pre-dose and at 0.5, 1, 3, 7 and 24 h post dosing | 151 nmol/kg | 10.2 ± 0.9 | SD rats plasma protease | ELISA | SD rats plasma | In Vivo | https://sci-hub.st/10.1126/science.2994212, | None | N.A. | |||
| 26774588 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 175 | Minipigs heparin-plasma protease | LC-MS | Minipigs heparin-plasma | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-36 | 34 | Free | Amidation | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 220 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma with 10 mM EDTA | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-35 | 33 | Free | Free | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 6 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma | In Vitro | None | None | N.A. | |||
| 26774588 | 2016 | PYY3-35 | 33 | Free | Free | Linear | L | None | Isolated and purified from porcine small intestine | Decrease appetite and food-intake | Conducted at 37ºC and aliquots were taken at 2, 5, 15, 30, 60, 120 and 240 min | 1 µM | 39 | Minipigs heparin-plasma protease | LC-MS | minipigs heparin-plasma with 10 mM EDTA | In Vitro | None | None | N.A. | |||
| 26752086 | 2016 | ABB28 | 38 | 7 mer ABD domain conjugated at N terminus | Amidation | Linear | L | Biotinylation | Synthetic | Antitumor | N.A. | 30 nmol | 2 | BALB/c mice plasma protease | ELISA | BALB/c mice plasma | In Vivo | None | None | IC50 ranges from 2.1–2.5 mM (In the absence of FBS) for ABB28 | |||
| 26752086 | 2016 | BB28 | 31 | conjugating a truncated antimicrobial peptide B28 to the N-terminus of the tumor-homing peptide bombesin | Amidation | Linear | L | Biotinylation | Synthetic | Antitumor | N.A. | 30 nmol | <5 | BALB/c mice plasma protease | ELISA | BALB/c mice plasma | In Vivo | None | None | IC50 ranges from 2.5–3.0 mM (In the absence of FBS) for BB28 | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 0.05784 | Chymotrypsin | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with Chymotrypsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 3.53 | Aminopeptidase N | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with APN (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 10.16 | Carboxy-Peptidase A | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with CPA (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 12.38 | Trypsin | Mass spectrometry | Intestinal fluid buffer (pH 6.8) with Trypsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | N.A. | 23.88 nmol/mL | 14.28 | Pepsin | Mass spectrometry | Gastric fluid solution (pH 1.2) with Pepsin (0.2 U/mL) | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 37°C | 100 µg/mL | 1.718 | Intestinal duodenum homogenate protease | Ultraviolet spectroscopy | Intestinal duodenum homogenate | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 37°C | 100 µg/mL | 1.462 | Intestinal jejunum homogenate protease | Ultraviolet spectroscopy | Intestinal jejunum homogenate | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 26725426 | 2016 | Exenatide | 39 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 37°C | 100 µg/mL | 1.229 | Intestinal ileum homogenate protease | Ultraviolet spectroscopy | Intestinal ileum homogenate | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 28989813 | 2016 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled with Alexa Fluor | Derived from Heloderma suspectum | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 1.7 ± 0.2 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 0.08 ± 0.01 | |||
| 26574515 | 2016 | CII-a | 40 | Free | Free | Linear | L | Two amphipathic helices linked by proline19 | Synthetic | Treatment of Hypertriglyceridemia | 0, 0.5, 1, 4, 7, 24, and 48 hours | 1.0μmol/kg of body weight | 1.33 ± 0.72 | Apoc2 Mutant Mice Plasma Protease | MALDI-TOF MS | Apoc2 mutant mice plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4293430/ | None | peptide C-II-a dose of 5 μmol/kg achieved a maximum decrease of approximately 90% after 30 minutes, with plasma TG remaining below baseline levels for up to 48 hours | |||
| 26574515 | 2016 | CII-a | 40 | Free | Free | Linear | L | Two amphipathic helices linked by proline19 | Synthetic | Treatment of Hypertriglyceridemia | 0, 0.5, 1, 4, 7, 24, and 48 hours | 1.0 μmol/kg of body weight | 1.33 ± 0.72 | Apoc2 mutant mice plasma protease | MALDI-TOF MS | Apoc2 mutant mice plasma | In Vivo | None | None | peptide C-II-a dose of 5 μmol/kg achieved a maximum decrease of approximately 90% after 30 minutes, with plasma TG remaining below baseline levels for up to 48 hours | |||
| 28989813 | 2016 | Exendin | 39 | Free | Amidation | Linear | L | Fluorescently labeled with Alexa Fluor | Isolated from the saliva of the Gila monster lizard (Heloderma suspectum) | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 0.7 ± 0.1 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 0.08 ± 0.01 | |||
| 28989813 | 2016 | 54.6 kDa EG9 | 40 | Free | Poly[Oligo(Ethylene Glycol)9 Methyl Ether Methacrylate] = Poegma(54.6 Kda) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-C-POEGMA conjugates | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 6.2 ± 0.5 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 1.91 ± 0.35 | |||
| 28989813 | 2016 | 55.6 kDa EG3 | 40 | Free | Poly[Oligo(Ethylene Glycol)3 Methyl Ether Methacrylate] = Poegma(55.6Kda) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-C-POEGMA conjugates | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 7.6 ± 0.7 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 4.17 ± 0.13 | |||
| 28989813 | 2016 | 71.6 kDa EG3 | 40 | Free | Poly[Oligo(Ethylene Glycol)3 Methyl Ether Methacrylate] = Poegma(71.6Kda) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-C-POEGMA conjugates | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 9.0 ± 1.7 (T1/2 Absorption Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | PDB id: 7MLL | None | EC50(nM) = 5.11 ± 0.23 | |||
| 107-968-725-190-134 | 2016 | Ex-4 | 39 | Free | Free | Linear | L | None | NA | N.A. | 30 min | 25 μM | 38 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | singly stapled SAH-Ex(A) | 39 | Stapled | Free | Linear | L | None | NA | N.A. | 30 min | 25 μM | 94 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | singly stapled SAH-Ex(B) | 39 | Stapled | Free | Linear | L | None | NA | N.A. | 30 min | 25 μM | 128 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 107-968-725-190-134 | 2016 | doubly stapled peptide SAH-Ex(A, B) | 39 | Stapled | Stapled | Linear | L | None | NA | N.A. | 30 min | 25 μM | 295 | chymotrypsin | ELISA | male C57BL/6 mice serum | in vivo | https://lens.org/107-968-725-190-134 | US 9,296,805 B2 | N.A. | |||
| 032-864-902-079-483 | 2016 | glucagon-like peptide-2 | 33 | removing α-carbon of histidine | thiol group | Linear | L | None | NA | NA | NA | NA | Increased | NA | NA | NA | in vivo | https://lens.org/032-864-902-079-483 | US 9504757 B2 | NA |