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| ID | PMID | YEAR | Sequence | Name | Length | N-ter MOD | C-ter MOD | Linear/Cyclic | Chirality | Chem-MOD | Origin | Nature | Incubation Time | Concentration | Half Life | Units Half Life | Protease | Assay | Test Sample | Vivo/Vitro | Reference | Patent No. | Activity |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 20844765 | 2010 | Com6 | 8 | Free | Amidation | Cyclic (C1-C8) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 6.5 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=3.8μM for E.coli | |||
| 20844765 | 2010 | Com6 | 8 | Free | Amidation | Cyclic (C1-C8) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 6.5 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=0.9μM for S. aureus | |||
| 20844765 | 2010 | Com6 | 8 | Free | Amidation | Cyclic (C1-C8) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 6.5 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=0.9μM for B. subtilis | |||
| 20844765 | 2010 | Com7 | 8 | Acetylation | Amidation | Cyclic (C1-C8) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 6.5 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=30μM for E.coli | |||
| 20844765 | 2010 | Com7 | 8 | Acetylation | Amidation | Cyclic (C1-C8) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 6.5 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99=1.9μM for S. aureus | |||
| 20844765 | 2010 | Com7 | 8 | Acetylation | Amidation | Cyclic (C1-C8) | L | None | Synthetic | Antimicrobial | 9 hours | 5 µM | 6.5 | Human serum proteases | RP-HPLC | Human serum | in vitro | None | None | LD99.99 ‰¤ 0.45μM for B. subtilis | |||
| 15012592 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 1.25 mU of DPP IV | 5 ·8 | DPP IV | LC/MS equipped with a microbore C-18 HPLC | DPP IV | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 15012592 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon | Antihyperglycaemic, insulinotropic | Not reported | 2mM peptide incubated with 7.5 µl of human plasma | 6 ·2 | Human plasma proteases | LC/MS equipped with a microbore C-18 HPLC | Human plasma | in vitro | None | None | Insulinotropic activity in vitro at 5 ·6 mM glucose | |||
| 11099487 | 2000 | Int-H1-S6A,F8A | 30 | Free | Free | Linear | L | None | C-Myc derivative | Antiproliferative and proapoptotic | Not reported | Not mentioned | 7.29 | Fetal calf serum proteases | HPLC | Fetal bovine serum batch4 | in vitro | None | None | Not reported | |||
| 12578830 | 2003 | iAβ5p-C2 | 5 | Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 7 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 12578830 | 2003 | iAβ5p-C3 | 5 | (NMe)Sar | Amidation | Linear | L | None | Synthetic | β-sheet breaker peptides | Not reported | 20 nmol | 6 | Human plasma proteases | RP-HPLC | Human plasma | in vitro | None | None | >80% inhibition of amyloid fibrillogenesis | |||
| 15246869 | 2004 | GLP-1 | 30 | Free | Free | Linear | L | None | Glucagon-like peptide-1(7-36)amide | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 6.2 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=6.1 ±1.8nM | |||
| 15246869 | 2004 | GIP | 42 | Free | Free | Linear | L | None | Gastrointestinal incretin hormone | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 6 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | 8446620 | None | cAMP EC50=21.8 ±1.5nM | |||
| 15246869 | 2004 | (Abu2)GIP | 42 | Free | Free | Linear | L | 2-aminobutyric acid (Abu) | Synthetic | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 7.1 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=36.8 ±1.6nM | |||
| 10541299 | 1999 | Epoetin | 166 | Free | Free | Cyclic | L | Three N-linked carbohydrate chains | Recombinant human erythropoietin | Stimulates erythropoiesis | Not mentioned | Not mentioned | 8.5 ±2.4 | Human blood proteases | ELISA | Subcutaneously injected into patients with end-stage renal failure | in vivo | http://www.drugbank.ca/drugs/DB00016 | None | Not reported | |||
| 20382695 | 2010 | Taspoglutide | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Derivative of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 9.8 | Rat plasma protease | RP-HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.06nM for stimulating cAMP production | |||
| 20418955 | 2010 | Gcg-XTEN 288 | 319 | Free | XTEN | Linear | L | None | Glucagon derivative | Regulate blood glucose | Not mentioned | 12 nmol/kg | 9 | Cynomolgus monkey plasma proteases | Sandwich ELISA | Injected subcutaneouly into cynomolgus monkeys | in vivo | None | None | Elevated blood glucose levels for 10 €“12 hours | |||
| 20418955 | 2010 | Gcg-XTEN 144 | 175 | Free | XTEN | Linear | L | None | Glucagon derivative | Regulate blood glucose | Not mentioned | 12 nmol/kg | 8 to 10 | Cynomolgus monkey plasma proteases | Sandwich ELISA | Injected subcutaneouly into cynomolgus monkeys | in vivo | None | None | Not reported | |||
| 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 | |||
| 21114599 | 2010 | [Aib8]hGLP-1(7-36)NH2 | 30 | Free | Amidation | Linear | L | Aib--Aminoisobutyric acid | Analogue of glucagon like peptide-1 | Regulate blood glucose | Not mentioned | Not mentioned | 5.9 ±1.0 | Rat plasma proteases | HPLC | Rat plasma | in vitro | 14759771 | None | EC50=0.29 ±0.22nM for cAMP stimulation | |||
| 20593470 | 2010 | Peptide 6 | 41 | Free | Amidation | Linear | Mix | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 5.1 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 15 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 7.7 | None | HPLC | PBS | in vitro | None | None | EC50=0.77 ±0.25 | |||
| 20560643 | 2009 | Peptide 2 | 8 | Free | NH-3,5-Bzl(CF3)2 | Linear | Mix | Nle=norleucine | Synthetic analogues of TY027 | Opioid receptor agonist | 24 hours | Not mentioned | >6 | Rat plasma proteases | HPLC | Rat plasma | in vitro | None | None | IC50=14 ±1.6nM for MVD | |||
| 20560643 | 2009 | Peptide 5 | 8 | Free | NH-3,5-Bzl(CF3)2 | Linear | Mix | Nle=norleucine, O-β-glucosylated serine | Synthetic analogues of TY027 | Opioid receptor agonist | 24 hours | Not mentioned | >6 | Rat plasma proteases | HPLC | Rat plasma | in vitro | None | None | IC50=13 ±5.8nM for MVD | |||
| 14499707 | 2003 | GRF-1PEGLys12 | 29 | Free | Amidation | Linear | L | PEGylation on Lys12 | Growth hormone-releasing hormone (GRF) analogue | Stimulates release of growth hormone | 24 hours | Not mentioned | 10 | Human plasma proteases | Reporter gene assay | Human plasma | in vitro | None | None | Not reported | |||
| 20585128 | 2010 | Sub3-Agp | 12 | Free | Amidation | Linear | L | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub3 | Antimicrobial | Not reported | 150 µg/ml | >480 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=1 µg/ml for S. Aureus | |||
| 20585128 | 2010 | Sub3-DAgp | 14 | Free | Amidation | Linear | Mix | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub5 | Antimicrobial | Not reported | 150 µg/ml | >480 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=1 µg/ml for S. Aureus | |||
| 20585128 | 2010 | Sub3-Agp | 12 | Free | Amidation | Linear | L | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub3 | Antimicrobial | Not reported | 150 µg/ml | >480 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=2 µg/ml for P. Aeruginosa | |||
| 20585128 | 2010 | Sub3-DAgp | 14 | Free | Amidation | Linear | Mix | Agp=αamino-3-guanidino-propionic acid | Derivative of Sub5 | Antimicrobial | Not reported | 150 µg/ml | >480 | Proteases in mouse serum | RP-HPLC | 25% aqueous mouse serum | in vitro | None | None | MIC=2 µg/ml for P. Aeruginosa | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 10 | γ-secretase (protease) ALLN(protease inhibitor) | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 3080478 | 1985 | C4-LAP | 15 | Saturated acyl chain of 4 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~340 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C8-LAP | 15 | Saturated acyl chain of 8 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~410 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C12-LAP | 15 | Saturated acyl chain of 12 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | ~410 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 3080478 | 1985 | C16-LAP | 15 | Saturated acyl chain of 16 carbons | Free | Linear | L | None | Lipid associated peptide -20 | Not mentioned | Not reported | 300 µl | 513 ±12 | Not mentioned | Serum decay experiment | Blood sample of female Sprague-Dawley rat | in vivo | 6774331 | None | Not mentioned | |||
| 16990557 | 2006 | cNGR | 8 | Acetylation | Amidation | Cyclic | L | None | Synthetic peptide | Targets CD13/APN which is present on angiogenic vessels so used for molecular imaging | Not reported | 0.75μg/g | 9.1 ±0.3 | Proteases present in the tissue of angiogenetic vessels in mouse | Fluorometery | Mouse tissue of myocardial infarction (MI) model | 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 | |||
| 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-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-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-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 | |||
| 17986790 | 2007 | GLP-1/HAS | 30 | Free | Human serum albumin | Linear | L | None | Glucagon | Glucose-dependent insulinotropic effect | Not reported | 0.1 µmol/kg | 10 | Mouse blood proteases | ELISA | Mouse plasma (Intraperitoneally administered) | in vivo | None | None | 0.1 mmol/kg had glucose-lowering effect up to 4 h after administration | |||
| 18307313 | 2007 | CAP 3 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 10 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 10 µM for S.aureus | |||
| 18307313 | 2007 | CAP 3 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 10 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 7 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 3 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 10 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 4 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 7 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 11 µM for S.aureus | |||
| 18307313 | 2007 | CAP 7 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 7 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 7 | 2 | Free | NHBn | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 7 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 10 | 2 | Free | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 9 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 9 µM for S.aureus | |||
| 18307313 | 2007 | CAP 10 | 2 | Free | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 9 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 7 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 10 | 2 | Free | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 9 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 6 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 16 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 145 µM for S.aureus | |||
| 18307313 | 2007 | CAP 16 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 95 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 16 | 2 | Free | CH2CH2Ph | Linear | L | X= structure given in paper | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 81 µM for Methicillin- resistant S.epidermis | |||
| 18307313 | 2007 | CAP 16 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 145 µM for S.aureus | |||
| 18307313 | 2007 | CAP 16 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 95 µM for Methicillin- resistant S.aureus | |||
| 18307313 | 2007 | CAP 16 | 2 | Acetylation | Y= structure given in paper | Linear | L | Bip | Synthetic peptide | Antimicrobial | Not reported | 1 mg/mL | 7 | Trypsin | RP-HPLC | Trypsin | in vitro | None | None | MIC= 81 µM for Methicillin- resistant S.epidermis | |||
| 19601640 | 2009 | TATp | 11 | Free | Free | Linear | L | None | Synthetic peptide | Cell penetrating peptide | Not reported | 10 µL | >400 | Not mentioned | HPLC | Human plasma | in vitro | None | None | Not available | |||
| 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 | |||
| 19762245 | 2009 | TY039 | 8 | Free | NH-[3 €™,5 €™-(CF3 )2 Bzl] | Cyclic (C2-C5) | Mix | None | Synthetic peptide | Analgesic | Not reported | 50 µg/ml | >6 | Rat plasma proteases | HPLC | Rat plasma | in vitro | None | None | Not available | |||
| 19762245 | 2009 | TY035 | 8 | Free | NH-[3 €™,5 €™-(CF3 )2 Bzl] | Cyclic (C2-C7) | Mix | Nle | Synthetic peptide | Analgesic | Not reported | 50 µg/ml | >6 | Rat plasma proteases | HPLC | Rat plasma | in vitro | None | None | Not available | |||
| 19762245 | 2009 | TY038 | 8 | Free | NH-[3 €™,5 €™-(CF3 )2 Bzl] | Cyclic (C2-C7) | Mix | Nle | Synthetic peptide | Analgesic | Not reported | 50 µg/ml | >6 | Rat plasma proteases | HPLC | Rat plasma | in vitro | None | None | Not available | |||
| 22698865 | 2012 | TRAF6 Inhibitory peptide | 27 | Free | Free | Linear | L | None | TNF receptor associated factors 6 | Intracellular adapter protein | Not reported | 1.5 mg (peptide)/mice | 5.08 | Mouse blood proteases | Spectrofluorometry | Mice serum | in vivo | None | None | Not mentioned | |||
| 22698865 | 2012 | PEGylated TRAF6 Inhibitory peptide | 27 | Pegylation | Free | Linear | L | None | TNF receptor associated factors 6 | Intracellular adapter protein | Not reported | 1.5 mg (peptide)/mice | 8.99 | Mouse blood proteases | Spectrofluorometry | Mice serum | in vivo | None | None | Not mentioned | |||
| 22934681 | 2012 | GSH-PEG liposomal DAMGO | 5 | Free | Free | Linear | Mix | Methylation at phenylalanine | Synthetic peptide | Enhances and prolongs blood to-brain drug delivery of the opioid peptide DAMGO | Not reported | 12.5 mg/kg | 417 ± 140 | Rat blood proteases | ESI-LC ˆ’MS/MS | Rat blood plasma (Intravenous) | in vivo | None | None | Not mentioned | |||
| 3348603 | 1987 | DihydromycoplanecinA (DHMP A) | 10 | Free | Free | Cyclic | L | N-MeVal; N-methylvaline, EtPro; Ethylproline, N-MeThr; N-methylthreonine MePro; Methylproline, AMHA; 2-amino-5-methylhexanoic acid, N-MeLeu; N-methylleucine | Active metabolite in urine of mice and dogs | Antibiotic | Not reported | 10 mg/kg | 5.5 | Dog blood proteases | Not mentioned | Dog serum (Intravenous) | in vivo | None | None | LD50>6000mg/kg administered orally to mice | |||
| 20418955 | 2010 | Gcg-XTEN-288 (glucagon-XTEN fusion peptide) | 29 | Free | XTEN-288 | Linear | L | None | Glucagon-288 amino acid XTEN fusion peptide | Glucose homeostasis | Not reported | 12 nmol/kg | 9 | Monkey blood proteases | ELISA | Monkey plasma (Subcutaneous) | in vivo | None | None | Biologically active in cynomolgus monkeys for 6 hours | |||
| N.A. | 2009 | DX-890-Human Serum Albumin | 56 | Free | Human serum albumin | Linear | L | None | Kunitz domain peptide | Protease inhibitor | N.A. | Not mentioned | 380 | Mouse blood proteases | I-125 radiolabelling method | Mouse plasma (Intravenous) | in vivo | None | EP2090589A1 | 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. | 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. | 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 | |||
| 4034413 | 1985 | Leucine enkephalin analogue | 5 | Free | Free | Linear | L | Thiomethylene bond replacement between residue 4-5 | Derivative of Natural enkephalin | Analgesic | 20 minutes | 0.9 nM | 315 | Human serum protease | HPLC | Human serum | in vitro | None | None | Not reported | |||
| 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. | |||
| 9932163 | 1998 | Cemadotin-HCl | 5 | Free | Free | Linear | L | None | Synthetic analogue of Dolastatin 15 | Antimitotic | 24 hour | 10 - 27.5mg | 10 | Human blood proteases | Radioimmunoassay | Intravenous administration to human | in vivo | None | None | Cancer patient was administered with Cemadotin for 24 hours intravenously at dose of 10mg. Reduction in liver metastasis was observed by sonographic examination. | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 5.88 ±0.374 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 8.97 ±4.50 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 6.23 ±1.47 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 7522585 | 1994 | Antagonist D [D-Arg1,D-Phe5,D-Trp7,9,Leu11]-SP | 22 | Free | Free | Linear | Mix | None | Substance P (SP) analogue | Anticancer drugs | 1, 2, 5 and 24 hours | 0.1 μg/ml | 9 | Mouse liver proteases | RP-HPLC and Electrochemical Detection | Mouse liver homogenate | in vitro | None | None | Act as growth factors | |||
| 8545241 | 1995 | Dynorphin A (DYN A) analog-5 | 17 | Free | Free | Linear | L | The reduced bond psi [CH,-NH] was introduced at position 5-6 | Opoid | Physiological effect regulating peptide | 0-60 minutes | 100 μM peptide solution to 0.18-ml portions of brain membranes | >500 | Endopeptidase 24-11 (enkephalinase), mouse brain proteases | HPLC | Mouse brain homogenates | in vitro | None | None | Not reported | |||
| 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. | |||
| 19767127 | 2011 | Peptide 6 | 11 | Acetylation | Amidation | Linear | L | None | Ciliary neurotrophic factor (CNTF) | Neurotrophic peptide | 0, 15, 30, 60 and 120 min | 5 μg | >6 | Rat blood proteases | LC/MS/MS | Sprague-Dawley Rat plasma | in vivo | None | None | Peptide 6 effectively inhibited the LIF-mediated signaling and ˆ¼50% inhibition of 10 pM LIF was achieved with 100 pM Peptide 6. | |||
| 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 | |||
| 21185160 | 2011 | O-24 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 19th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | >480(79.6 ±0.2%) | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 | |||
| 22263969 | 2012 | 3d (Atrial natriuretic peptide- Fc dimer) | 84 | 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 | 5.5 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 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 | |||
| 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 | |||
| 25771000 | 2015 | MHDBAY (Recombinant PACAP-derived peptide) | 45 | Free | Free | Linear | L | None | Synthetic (Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide) | Insulin secretion stimulant | 37 C, 48 Hours | 10 µM | 9.71 | Fxa(Facor Xa) | HPLC-ESI/MS/MS | Buffer containing peptide sample | in vitro | None | None | AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control | |||
| 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 | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | Apr-14 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 10 ±0.5 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 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 | |||
| 24139844 | 2013 | Conjuagte 1 (conjugates of 4-aminocyclophosphamide (4-NH2-CPA)) | 4 | Succinylation | Amidated CPA | Linear | L | None | Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA) | Anti-cancer | Not mentioned | Not mentioned | 6.5 | PSA(Prostate-specific antigen ) | HPLC | Conjuagte 1+PSA(Prostate-specific antigen) | in vitro | None | None | Not reported | |||
| 25453979 | 2014 | MA(D-Leu-4)OB3 | 7 | Myristoylation | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in sterile phosphate buffered saline(PBS, pH 7.2) at a concentration of 0.1 mg | 5.9 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intra-muscular route of delivery) | in vivo | None | None | Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM | |||
| 25453979 | 2014 | MA(D-Leu-4)OB3 | 7 | Myristoylation | Free | Linear | Mix | None | Synthetic peptide amide with leptin-like activity | Regulate energy balance by inhibiting hunger | Not mentioned | Peptide was dissolved in 0.3% Intravail ® reconstituted in sterile deion-ized water at a concentratio | 8.2 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intranasal route of delivery) | in vivo | None | None | Efficacy of MA-[D-Leu-4]-OB3 on blood glucose levels in db/dbmice following oral delivery in 0.3% DDM | |||
| 1329046 | 1992 | Bombesin | 14 | Free | Amidation | Linear | L | Pyr=Pyro-glutamine | Autocrine peptide of SCLC cell line | Growth stimulator | 0-1080 minutes | 50μM | 417 | Degradative enzymes or SCLC cell line proteases | RP-HPLC | SCLC cell line NCI-H345 | in vitro | None | None | IC50= 1nM, Peptide were added at a 1 μM dose to inhibit growth of SCLC cell line | |||
| 1329046 | 1992 | [P]BN(6-13)PA [Bombesin antagonist] | 8 | Free | Propylamidation | Linear | Mix | None | Bombesin analogue | Growth inhibitors | 0-360 minutes | 50μM | 559 | Degradative enzymes or SCLC cell line proteases | RP-HPLC | SCLC cell line NCI-H345 | in vitro | None | None | IC50= 3nM, Peptide were added at a 1 μM dose to inhibit growth of SCLC cell line | |||
| 1346149 | 1992 | SS-28 (Somatostatin-28) | 28 | Free | Free | Cyclic (C17-C28) | L | None | Hormone produced by neuroendocrine neurons of the ventromedial nucleus of the hypothalamus. | Inhibitor of growth hormone release | 37 °C for 30-180 minutes | 50μM | 335.7 ±100.8 (Metabolic half life) | Hippucampul tissues proteases | Radioimmunoassay | Posterior Hippucampus tissues of brain of SDAT(Medical Research Council Brain Bank, Cambridge, England) | in vitro | None | None | Not reported | |||
| 3379352 | 1988 | IGF-1 (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | Labelled with 125I | Purified from bovine colostrum | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 6.0-7.0 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 3379352 | 1988 | Reduced IGF-1(bound form) (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | Labelled with 125I, Disulphide bond is reduced | Bovine IGF-1 | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 6 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 2556215 | 1989 | Angiotensin I (AI) | 10 | Free | Free | Linear | L | None | Derived from angiotensin | Precusor of angiotensin- II (AII) | 37 °C | 100 - 2000 ng/ml | 9.2 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (2.5%) | in vitro | None | None | Not mentioned | |||
| 2556215 | 1989 | Angiotensin I (AI) | 10 | Free | Free | Linear | L | None | Derived from angiotensin | Precusor of angiotensin- II (AII) | 37 °C | 100 - 2000 ng/ml | 8.3 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (5%) + converting enzyme inhibitor (MK422) with conc 10-6 M | in vitro | None | None | Not mentioned | |||
| 2556215 | 1989 | Angiotensin I (AI) | 10 | Free | Free | Linear | L | None | Derived from angiotensin | Precusor of angiotensin- II (AII) | 37 °C | 100 - 2000 ng/ml | 8.7 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum (10%) + Heat inactivation | in vitro | None | None | Not mentioned | |||
| 2556215 | 1989 | Angiotensin I (AI) | 10 | Free | Free | Linear | L | None | Derived from angiotensin | Precusor of angiotensin- II (AII) | 37 °C | 100 - 2000 ng/ml | 9.9 | Fetal calf serum proteases | Radioimmunoassay | Primary endothelial cells + Fetal calf Serum(10%) + converting enzyme inhibitor (MK422) with conc 10-6 M + heat inactivation | in vitro | None | None | Not mentioned | |||
| 8217216 | 1993 | AcSDKP (Acetyl-SDKP) | 4 | Acetylation | Free | Linear | L | None | Isolated from fetal calf bone marrow | Natural hemoregulatory | 37 °C for 24 hours | 4 X lO-7M, 10 µCi | 7 | Proteases from Human serum | HPLC | Human serum + 1μM catropril | in vitro | None | None | Not reported | |||
| 8217216 | 1993 | AcSDKP (Acetyl-SDKP) | 4 | Acetylation | Free | Linear | L | None | Isolated from fetal calf bone marrow | Natural hemoregulatory | 37 °C for 24 hours | 4 X lO-7M, 10 µCi | 5.5 | Proteases from Horse serum | HPLC | Horse serum | in vitro | None | None | Not reported | |||
| 8217216 | 1993 | AcSDKP (Acetyl-SDKP) | 4 | Acetylation | Free | Linear | L | None | Isolated from fetal calf bone marrow | Natural hemoregulatory | 37 °C for 24 hours | 4 X lO-7M, 10 µCi | 6 | Proteases from Mouse serum | HPLC | Mouse serum + 1μM catropril | in vitro | None | None | Not reported | |||
| 8218482 | 1993 | 125I-YRGDS-polymer conj µgate(Isocyanate containing polyurethane prepolymer) | 5 | Free | Free | Linear | L | Peptide covalently attached to Isocyanate containing polyurethane prepolymer | Synthetic RGD containing peptide | Cell attachment property | Not mentioned | Not mentioned | 7 | Proteases from mouse bood | HPLC | Mouse blood | in vivo | 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 | |||
| 8545241 | 1995 | Dynorphin A(1-11)-NH2 analogue 5 (DYN A analogue) | 11 | Free | Amidation | Linear | L | None | Human placenta Dynorphin A derivative | Incorporating the nonhydrolyzable [CH2-NH] peptide bond surrogate were tested for their in vitro enzymatic stability in mouse brain homogenates. | 37 °C | 100 µM | >500 | Proteases from mouse brain tissues | HPLC | Mouse brain homogenate | in vitro | None | None | Not reported | |||
| 8395230 | 1993 | Bradykinin | 9 | Free | Free | Linear | L | None | Endogenous peptide of kinin family | Vasodilator, Inflammatory mediator | 37 °C for 15-240 minutes | 10 µg/L of peptide | 381 ±51 | Neutral endopeptides in Human umbilical vein endothelial cells | Radioimmunoassay | Human umbilical vein endithelial cells + Lisinopril +phosphoramidon | in vitro | None | None | Not reported | |||
| 8395230 | 1993 | Bradykinin | 9 | Free | Free | Linear | L | None | Endogenous peptide of kinin family | Vasodilator, Inflammatory mediator | 37 °C for 15-240 minutes | 10 µg/L of peptide | 386 ±52 | Neutral endopeptides in Human umbilical vein endothelial cells | Radioimmunoassay | Human umbilical vein endithelial cells+ Lisinopril +phosphoramidon+amastatin | in vitro | None | None | Not reported | |||
| 20158487 | 2010 | PEG10kDa-[(123)I]-CCK-10 | 10 | Free | Amidation | Linear | L | SO3H Group at Tyr-4, Coupled to PEG(10KDa), PEG=Polyethylene glycol, CCK-10=Cholecystokinin | Peptide Hormone produced by small intestine | Stimulates the digestion of fat and protein | Not mentioned | Not available | 8 (Elimination half life t1/2 alpha) | Rat blood proteases | HPLC | Rat blood | in vivo | None | None | Not reported | |||
| 20382695 | 2010 | Taspoglutide | 30 | Free | Amidation | Linear | L | Aib=α-aminoisobutyric acid replacing Ala8 and Gly35 of hGLP-1[7-36] | Novel analog of hGLP1 | Treatment of type 2 diabetes(clinical trials) | 1 hour | 40 nm(1μg/μl upto 500μl) | 9.8 | Rat blood proteases | HPLC | Rat blood plasma | in vitro | http://www.drugbank.ca/drugs/DB00114 | None | cAMP stimulation,EC50=0.06nM | |||
| 20687610 | 2010 | c[E22,K26]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E22-K26 and E30-K34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 6.0 ±1.8 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00124 | None | EC50=1.6nM,pEC50=8.8 ±0.11 | |||
| 20687610 | 2010 | c[K22,E26]-c[K30,E34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between K22-E26 and K30-E34) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 7.3 ±0.4 | Dipeptidyl peptidase-IV | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human DPP-IV enzyme (0.2 ng/mL) in Tris buffer (25 mM, pH 8.0) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00125 | None | EC50=2.2nM,pEC50=8.7 ±0.14 | |||
| 20687610 | 2010 | c[E22,K26]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K37) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 10 ±3.5 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00129 | None | EC50=2.8nM,pEC50=8.3 ±0.03 | |||
| 20687610 | 2010 | c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K38) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 6.9 ±0.5 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00130 | None | EC50=5.3nM,pEC50=8.6 ±0.13 | |||
| 20687610 | 2010 | c[E16,K20]-c[E30,K34]GLP-1(7-36)-NH2 | 30 | Free | Amidation | Cyclic (Lactam bridge between E16-K20, E22-K26 and E30-K39) | L | None | Analog of GLP-1 | Diagnosis and treatment of diabetes | 24 hours | 100μM | 6.9 ±0.1 | Neutral endopeptidase 24.11 | HPLC | GLP-1 analogue (100 μM) was incubated with the recombinant human NEP 24.11 enzyme (1.0 μg/mL) in HEPES buffer (50 mM, pH 7.4, 50 mM NaCl) at 37 °C | in vitro | http://www.drugbank.ca/drugs/DB00131 | None | EC50=3.3nM,pEC50=8.5 ±0.04 | |||
| 23696181 | 2013 | C12-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | C12-Laa | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 301.34 ±18.93 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00182 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 85% approx. after 48 hours | |||
| 23696181 | 2013 | C12-C12-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | Two C12-Laa | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 353.39 ±13.63 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00183 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 80% approx. after 48 hours | |||
| 23696181 | 2013 | GlcNS-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | N-β-D-glucosamine succinamic acid(GlcNS) | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 318.04 ±75.13 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00184 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 85% approx. after 48 hours | |||
| 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 | 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. | |||
| 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 | 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) | |||
| 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 | |||
| 38554247 | 2024 | MVIIA | 25 | Free | Amidation | Cyclic (C1-C16,C8-C20, C15-C25) | L | None | Derived from the venom of cone snails (genus Conus) | Treatment of Refractory Chronic Pain | At 0, 1, 2, 4, 8, and 24 h, aliquots of peptides MVIIA at 37 celsisus | 100 µM | 8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 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 | 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. | |||
| 38293540 | 2024 | GLP-ABD-XTEN288 | 401 | GLP-1 molecule was linked to the N-terminus of ABD via a (GGGGS)3 linker (GLP-ABD), His-tag | ABD was connected to the N-terminus of the XTEN polypeptide (288 amino acids) through a (GGGGS)3 linker | Linear | L | None | Fusion protein of GLP-1, ABD, XTEN (either 144 or 288) | Antidiabetes, Antiobesity | At 1, 3, 7, 12, 18, 24, 30, 36 h, approximately 30 μL of blood was drawn from the tail vein | 5 nmol | 7.32 | C57Bl/6 mice plasma protease And DPP-4 | ELISA | C57BL/6 mice plasma | In Vivo | None | None | GLP-ABD-XTEN288 showed a Kd value of 27.78 nM | |||
| 37875481 | 2023 | biNV-IL-15-Cy7 | N.A. | Free | Free | Linear | L | Cy7 | Derived from Interleukin-15 | Antitumor | The blood sample was harvested at timed intervals (2 min, 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, 12 h, and 24 h) | N.A. | 5.66 | Mice blood protease | Fluorescence spectrophotometry | Mice blood | In Vivo | None | None | Not mentioned | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | 372 | Gastric fluid protease | Triple Quadrupole Mass spectrometry | Simulated Gastric Fluid (SGF) at pH = 1.3 | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 37373203 | 2023 | HM-10/10 | 20 | Free | Free | Linear | L | None | Chimeric high-density lipoprotein mimetic peptide | Anticancer | 120 minutes | 2 μM | 433 | N.A. | Triple Quadrupole Mass spectrometry | potassium phosphate buffers of pH 7.4 (basic) | In Vitro | None | None | Enzyme Activity = 0.682 at 2 microMolar of HM1010 (Cytochrome P450 (CYP1A2) Induction in Single-Donor Human Hepatocytes Lot HH1086) | |||
| 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 | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | (Prodrugs of Onc72) MIC values >50 μmol L−1 on E.coli BW25113 | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | Prodrugs Showed negligible hemolytic activity (below 0.2%) up to the highest tested concentration (50 μmol L−1), similar to the negative control (PBS) | |||
| 36631971 | 2023 | 20k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 20 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Oncocins | Antimicrobial | Prodrug and Onc72 concentrations were determined 5 min, 15 min, 30 min, 1 h, 2 h, 4 h, 8 h, and 24 h postadministration | 4.34 mmol/kg | 324 | CD-1 mice plasma protease | cELISA | CD-1 mice plasma | In Vivo | None | None | 20 kDa thiol-PEG: Reduced cell viability more significantly, to ≈70% for both cell lines | |||
| 36631971 | 2023 | 5k-prodrug | 23 | Onc72 N-terminally coupled via a short peptide linker LVPR to 5 kDa thiol PEGs | Amidation, Orn at position 23 | Linear | L | Orn at postion 19 | Synthetic | Antimicrobial | 0, 4, 8, 16, and 24 h aliquots (47.5 μL) were taken in triplicates | 31.5 μmol/L | 8 | Mouse serum protease | Serum stability assay | Mouse serum | In Vivo | None | None | 5 kDa thiol-PEG: Reduced cell viability to ≈89% for both HepG2 and HEK293 cell lines | |||
| 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 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 0.25, 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 | RTD-1 | 16 | Free | Free | Linear | L | None | Theta Defensin | Antimicrobial | Blood samples were collected at 0.25, 1, 2, 4, 8, and 24 H post-dose via terminal cardiac puncture | 5 mg/kg | 6.05 (Elimination Half Life) | Mouse plasma protease | LC-MS with reverse phase liquid chromatography | Mouse plasma | In Vivo | None | US 2022/0048569 W | Administering an effective amount of the effective 9-defensin or the effective 0-dcfcnsin analog to the individual in need of treatment, wherein the effective amount provides antimicrobial activity directed to the microbe | |||
| 36443381 | 2022 | SA10SC-RLX | 25 | Acetylation | Amidation | Linear | L | Attachment of a lipid moiety (C18-γ-Glu-PEG2) at K34 position, Aib, Nle | Synthetic | Treatment for Chronic Fibrotic and Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 2, 4, 6, 8, 24, 48, 72, 96 and 168 h (IV route) and 0.25, 0.5, 2, 4, 6, 8, 24, 48, 72, 96 and 168 h (SC route) | 1 mg/kg | 7 (Terminal Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | EC50 (nM) = 0.8 for EA.hy926_hRXFP1 | |||
| 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-1-3(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-1-5(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) | |||
| 36135098 | 2022 | GNRs-AAP1-1-Cy5 | 7 | Free | Free | Linear | L | Cy5 conjugation | AAP1/AAP1-1/AAP1-2 modified GNRs | Antiadhesive property | At 0, 0.08, 0.16, 0.33, 0.5, 1, 2, 6, 12, 24, 48, 72 h, adding 40 μL termination solution | 1 mg/ml | 7.7 (T1/2 b) | Mouse serum protease | HPLC | 1 mL mouse serum | In Vitro | None | None | N.A. | |||
| 36112771 | 2022 | BT8009 | 16 | Acetylation | Conjugation to MMAE cytotoxin via a valine–citrulline (V-Citr) cleavable linker,Val-Citriline linker and BTC joined by spacer Sar10 | Bicyclic | Mix | cyclised on TATA (1,3,5-Triacryloylhexahydro-1,3,5-triazine), 1Nal - 3-(1-naphthyl)-L-alanine, HArg – homo-arginine, HyP – hydroxyproline, MMAE = Monomethyl auristatin E, Cys16 with amidation modification, D-Asp4 modification | BT8009 and MMAE cytotoxin hybrid | Anticancer | 24 hours | 2 µM | 8.5 | Rats blood protease | LC-MS/MS | Rats blood sample | In Vitro | None | None | KD(nM) = 6.0±1.2 (Binding affinity for BT8009 binding to extracellular domains of Nectin-4 in Rat) | |||
| 36047255 | 2022 | MTP/RGD-CAL/TAN NS | 4 for MTP, 3 for cRGD | Free | MTP/RGD comodified with CAL/TAN NS | Linear | L(cRGD), Mix(MTP) | Dmt: 2',6'-dimethyltyrosine | Synthetic | Treatment of Acute Myocardial Infarction (Ami) | Blood samples were obtained at determined times until 72 h after injection and 15 μL of heparin (1000 U/mL) was added to each sample | 10 mg/kg | 8.22 | AMI rats plasma protease | N.A. | AMI rats plasma | In Vivo | None | None | Blank MTP/RGD NS and RGD-PEG-DSPE groups showed over 85% of cell viability. In contrast, drugs contained formulations exhibited cytotoxicity to some extent | |||
| 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. | |||
| 35849214 | 2022 | HSA | 585 | Free | Free | Cyclic (17 Disulfide Bond) | L | None | Human derived | Carrier Protein | 30 minutes | 3 mL/kg of 20% albumin | 8 | Human intravascular sample protease | N.A. | Human intravascular sample | In Vivo | None | None | N.A. | |||
| 35849214 | 2022 | HSA | 585 | Free | Free | Cyclic (17 Disulfide Bond) | L | None | Human derived | Carrier Protein | 120 minutes | 3 mL/kg of 20% albumin | 6.3 | Human intravascular sample protease | N.A. | Human intravascular sample | In Vivo | None | None | N.A. | |||
| 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 | |||
| 35677307 | 2022 | C15-rhG-CSF | 175 | Free | Free | Linear | L | C15-MAL fatty chain-modification of rhG-CSF at Cys18 position | rhG-CSF derivative | N.A. | sampling time - 0, 0.5, 2, 4, 8, 12, 24, 48, 72, 96, 120, 144, 168 h | 1.0 mg/kg | 5.72 ± 0.43 | Mice Serum Protease | ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 35653695 | 2022 | KLK7 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 6.2 ± 0.9 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK7)(nM) = 32, Kd(albumin)(nM) = 164 (for KLK7(1)-tag) | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | Free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 5.1 ± 0.7 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 35653695 | 2022 | KLK5 inhibitor | 11 | free | A short linker GKG was attached at C terminal and then ALbumin tag was linked with Lys via PEG2 | Cyclic (C2-C8 Disulfide Bond) | L | None | Synthetic | Treatment for Netherton syndrome | N.A. | 6.2 mg/kg | 5.8 ± 0.4 (Terminal Half Life) | Mice plasma protease | HPLC analysis with fluorescence detection | Mice plasma | In Vivo | None | None | Ki(KLK5)(nM) = 1.2, Kd(albumin)(nM) = 119 (for KLK5(1)-tag) | |||
| 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 | |||
| 35414877 | 2022 | B_3.1 | 25 | C18 diacid-gGlu-2xOEG | Amidation, FLAG tag | Cyclic | L | None | Synthetic | Targets GIP receptor | N.A. | 2 μM | 585 (Elimination Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | IC50(nM) = 347 | |||
| 35359494 | 2022 | CSP1-F7Cha/I12Cha | 17 | Free | Free | Linear | L | introduction of Cha residues at positions 7 and 12 | CSP1 analog | Modulates Quorum Sensing In Streptococcus Pneumoniae | Aliquots (100 μL) were taken at 0, 0.5, 1, 2, 3, 4, 5, 6, and 24 h time points | 1 mM | 6 | Chymotrypsin | RP-HPLC | PBS solution | In Vitro | None | None | EC50(nM) = 0.97 for CSP1-F7Cha/I12Cha against ComD1 receptor, EC50(nM) = 70 for CSP1-F7Cha/I12Cha against ComD2 receptor | |||
| 35174698 | 2022 | eGFP | 239 | Free | Free | Linear | L | None | Enhanced GFP | Tagging | N.A. | N.A. | 565 | E. Coli Bl21(De3) cells lysate protease | Fluorescence assay | E. coli BL21(DE3) cells lysate after 5 h removed the inducer | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35174698 | 2022 | GFP-Mf | 266 | GFP | Mf (M.fluorum) SsrA tag sequences | Linear | L | None | eGFP derivative | Increases Half Life | N.A. | N.A. | 424 | E. Coli Bl21(De3) star strain lysate protease | Fluorescence assay | E. coli BL21 (DE3) star strain lysate in which RNase E has been knocked out | In Vivo | PDB id: 4EUL | None | N.A. | |||
| 35053417 | 2022 | (WR)8WK(Glutaryl-Dox)βA] | 19 | Free | βAlanine at C terminal conjugation | Cyclic | L | An ester bond is utilized to attach Dox with a glutaryl linker | Synthetic | Treat Breast, Leukemia, and Lymphoma Malignancies | 4 h at 37 °C | 5 µM | ∼6 | Human Serum Protease | HPLC | 25% Human serum | In Vitro | None | None | At 10 μM: 65% reduction in cell viability after 72 hours for SK-OV-3 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 19% cell viability after 72 hours for MDA-MB-231 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 77% reduction in cell viability after 72 hours for MCF-7 Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ), At 10 μM: 64% reduction in cell viability after 24 hours for MES-SA/MX2 Cells (DOX-resistant) Cells (antiproliferative activity values for the [(WR)8WKβA]-Dox conjugate ) | |||
| 34807760 | 2022 | PLG0206 | 24 | Free | Free | Linear | L | None | Synthetic | Antimicrobial | Blood samples for PK assessment were collected at predose, at the midpoint of infusion, within 1 min of the end of infusion, and at 0.5, 1, 2, 4, 6, 8, 12, 20, 24, 36, and 48 h after the end of infusion | 0.05 mg/kg | 7.37 (Median Terminal Half Life) | Human plasma protease | HPLC-MS | Human plasma | In Vivo | Pubchem CID : 16152467 | None | N.A. | |||
| N.A. | 2022 | Dex-e9-XPLGLAG-r9-k(cy5) | 25 | Dextran | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Dex=Dextran, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 5 nmol | 6 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | hIL-18BP | 194 | Free | Free | Linear | L | None | Synthetic | Antagonist of IL-18 | Single subcutaneous administration: 0, 0.33, 1, 1.5, 3, 5, 7, 12, 24, 48, 72, 120, And 168 Hours (13 Points In Total), Single Intravenous Administration: 0, 0.083, 0.25, 0.5, 1.25, 3, 5, 10, 24, 48, And 72 Hours (11 Points In Total) | 3 mg/kg + 1 mg/kg | 6.51 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | IB 2021058964 W | IC50 of IL-18BP-His was 0.0240 nM | |||
| N.A. | 2022 | hIL-18BP | 194 | Free | Free | Linear | L | None | Synthetic | Antagonist of IL-18 | Single intravenous administration: 0, 0.083, 0.25, 0.5, 1.25, 3, 5, 10, 24, 48, And 72 Hours (11 Points In Total) | 1 mg/kg | 6.51 | Rats plasma protease | ELISA | Rats plasma | In Vivo | None | IB 2021058964 W | IC50 of IL-18BP-His was 0.0240 nM | |||
| 35177945 | 2022 | pGlu(Val13)apelin-13 | 13 | pGlu = Pyroglutamate | Val13 modifcation, carboxylation | Linear | L | None | Apelin-13 Analogue | Insulinotrophic Activity | 0, 2, 4, 8, 24 h | 20 microgram | 9.8 | Mouse plasma protease | RP-HPLC | Mouse plasma in the presence of 50 Mmol/L TEA-HCl Buffer | In Vitro | https://pubmed.ncbi.nlm.nih.gov/29412822/, https://pubmed.ncbi.nlm.nih.gov/27815337/ | None | EC50(M) = 1.59e-008 (In vitro insulin secretion) | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 7.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.32 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 7.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.32 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 9.76 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 6.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 9.76 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 9.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 32.87 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 11.01 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 7.3 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 6.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 0.93 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) withheparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 8.68 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 6.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.7 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 9.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 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 | [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 | [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) | |||
| 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 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 | |||
| 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 | |||
| 34122400 | 2021 | CATH2 | 27 | Free | Free | Linear | L | None | Cationic chicken heterophil-derived peptide | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 302 ± 34.5 | Human serum protease | HPLC | Human serum | In Vitro | None | None | The cytotoxicity of CbTP was lower than that of parental peptide CATH2 | |||
| 34122400 | 2021 | CbTP | 18 | Free | TP5 conjugation | Linear | L | None | A hybrid peptide combining TP5 and fragments of CATH2 | Immunomodulatory | 15 min at 37°C | 10 µg/mL | 353 ± 41.3 | Human serum protease | HPLC | Human serum | In Vitro | None | None | CbTP induced cytotoxicity in a dose-dependent manner, while even a high dose (80 µg/mL) of CbTP was nontoxic to RAW264.7 cells | |||
| 33940058 | 2021 | OPBP-1 | 12 | Free | Free | Linear | D | Substituition of A with Y at position 10 | Derived from H12 | Anticancer | Co-incubation of OPBP-1 with 10% human serum for 0 h, 1 h, 2 h, 4 h, 8 h, 16 h, 24 h, 32 h and 48 h. | 20 mg/kg | 8.69 ± 1.19 | Male SD rats plasma protease | RP-HPLC | Male SD rats plasma | In Vivo | None | None | After 2 weeks of daily administration of 0.5 mg/kg OPBP-1, the tumor growth was significantly inhibited in CT26 and B16-OVA models. | |||
| 33813091 | 2021 | TPP1 (SPIO NP@M-P) | 21 | FITC labelled | Free | Linear | L | None | Synthetic | Anticancer | Blood samples (20μL) were obtained at different points (0, 5, 30 min, 1,2, 4, 6, 9, 24 h) via tail bleeding | 4 mg/kg | 6 (Blood Clearance Half Life) | Mice blood plasma protease | Fluorescence spectrometry | Mice blood plasma | In Vivo | None | None | N.A. | |||
| 33791863 | 2021 | 125I-Ang Conj | 7 | Thiol bisphosphonate,Maleimidopropionyl,PEG conjugated at N terminus | Free | Linear | L | 125I labeled | Synthetic | Role in Renal and Cardiovascular Homeostasis | Blood samples (∼200 µL) were collected from the cannula into heparinized tubes before dosing and 5, 10, 15, 30, and 45 min and 1, 1.5, 2, and 3 h after administration | 4.5 mM | 6.6 | Rats plasma protease | Radioactivity assay | Rats plasma | In Vivo | None | None | Ang Conj. values were 20.4±0.5%,6.8±0.6%, 8.4±0.2%, and 11.6±0.2% | |||
| 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) | |||
| 33672039 | 2021 | GLP1_8A37C-HSA | 30 | Free | HSA | Linear | L | Substituition of amino acid A at position 2 | GLP-1 analogs | Antidiabetes | Blood samples (<70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 3, 6, 12, and 24 h after conjugate administration | 10 nmol/kg | 7.1 (T1/2b) | BALB/c mice plasma protease | Sandwich ELISA | BALB/c mice plasma | In Vivo | None | None | EC50=185 nM ( In vitro measurement of cAMP production by GLP-1R-overexpressing HEK-293 cells) | |||
| 33665501 | 2021 | PEG-PLG-Pt | n | PEGylation | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | PEGylation | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 8.8 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 11 in SKOV3 cells | |||
| 33665501 | 2021 | PEG-pHe-PLG-Pt (pH 7.4) | n | PEG-CDM | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | Poly(L-glutamic acid) is grafted with methoxy poly(ethylene glycol) (PEG) using a pH-sensitive linker, 2-propionic-3-methylmaleic anhydride = CDM | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 7.9 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 8.5 in SKOV3 cells | |||
| 33665501 | 2021 | PEG-MMP-PLG-Pt | n+6 | PEGylation | Cisplatin (CDDP) is complexed with the carboxyl groups of the L-glutamic acid | Linear | L | PEGylation through an MMP-sensitive peptide linker (PLGLAG), CDM = 2-propionic-3-methylmaleic anhydride | Synthetic | Anticancer | At predefined time points 5, 15, and 30 min, and 1, 3, 6, 12, and 24 h, 200.0 μL of blood samples were collected from the orbital cavities of rats | 3 mg/kg | 7.8 | Rats plasma protease | ICP-MS | Rats plasma | In Vivo | None | None | IC50 (μg mL−1) = 6.9 in SKOV3 cells | |||
| 33555858 | 2021 | B10-33 (Cpd 59) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C16), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 8.9 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 3.6 ± 2.0 (88%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 60(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(γE)3-C16), PEGylation,Aib,Nle | Synthetic | Treatment of Cardiovascular Diseases | Blood samples were collected from individual animals at the following time points: 0.083, 0.25, 0.5, 1, 3, 6, 8, 24, 48, and 72 h | 1 mg/kg | 6.4 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 3.2 ± 2.1 (74%) in OVCAR5 cells | |||
| 33555858 | 2021 | Cpd 63(B10-33 ) | 24 | Acetylation | Amidation | Linear | L | Lys24 conjugated with (-(PEG2)3-(γE)3-C16), PEGylation,Aib,Nle,acetylation at Lys10 and Lys23 | Synthetic | Treatment of Cardiovascular Diseases | N.A. | 1 mg/kg | 5.7 | Rats plasma protease | LCHRMS | Rats plasma | In Vivo | None | None | EC50 nM = 1.0 ± 0.6 (80%) in OVCAR5 cells | |||
| 33391505 | 2021 | [125I]SST-scFv8D3 | 115 | 125I labeled | scFv of 8D3 is added to SST | Cyclic (Disulfide Bond Bw C-C Of SST) | L | Serine, threonine and glycine were added to the linker | Synthetic | Treatment of Alzheimer's diseases | Eight microliter blood samples from the tail vein were obtained at 0.5, 1, 2, 4, 6 and 24-h post injection | 0.44±0.08 MBq | 6 | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | The measured activation of neprilysin by SST-scFv8D3 preserved around 70% of the activation obtained by SST alone | |||
| 32078672 | 2020 | rFVIII | 654 | Free | Free | Linear | L | None | Synthetic | Role In Clotting | N.A. | 125 IU/kg | 7.63 | HemA mice plasma protease | chromogenic activity assays | HemA mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 32078672 | 2020 | rFVIII | 654 | Free | Free | Linear | L | None | Synthetic | Role In Clotting | N.A. | 200 IU/kg | 5.43 | VWF Het mice plasma protease | chromogenic activity assays | VWF Het mice plasma | In Vivo | PDB id : 5K8D, https://pmc.ncbi.nlm.nih.gov/articles/instance/7180082/bin/bloodBLD2019001292-suppl1.pdf | None | ED50 values for BIVV001 (7.5 IU/kg) and rFVIII (7.9 IU/kg) were similar | |||
| 33057063 | 2020 | 1F7-MFc | 268 | Free | C-terminus of 1F7 is directly fused to the Fc fragment | Linear | L | Small set of mutations, including His2, Lys24, and P29 | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 6.6 | Mouse serum protease | ELISA | Mouse serum | In Vitro | PDB ID: 3U7U | None | EC50 (nM) = 0.4 for 1F7 in HER2/HER4 Luc | |||
| 33057063 | 2020 | ALM6-1F7 | 130 | Free | C-terminus of ALM6 is directly fused to 1F7 | Linear | L | Small set of mutations, including His2, Lys24, and P29 | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 6.6 | Mouse serum protease | ELISA | Mouse serum | In Vitro | None | None | EC50 (nM) = 0.4 for 1F7 in HER2/HER4 Luc | |||
| 32888078 | 2020 | Mouse Lau- PTEN-PDZ | 8 | N-Lauryl | Free | Linear | L | Lipidation | Synthetic | Treatment of Alzheimer's diseases | Samples (80 μL) were taken at 0, 3, 6,9, 15, 30, 45, 60, 90, 120, 180, 240, 360 and 1440 min | Peptide stock solutions (120 μL) were added to pre-warmed diluted plasma (50% v/v, 1080 μL) | 5.86 | 50% V/V mouse plasma protease | HPLC | 50% v/v mouse plasma | In Vitro | None | None | N.A. | |||
| 32858124 | 2020 | Cmpd# 12 | 16 | Acetylation, N-terminus of apelin-13 linked via, liphophilic moiety pIPhe polypeptide spacer (-γGlu-OEG-OEG-) with C15 | Free | Linear | Mix | hArg = Homo-Arginine, NMeLeu, Oic = Unnatural amino acid | Derived from pyr-apelin-13 | Treatment of Chronic Hepatic Failure | N.A. | 0.5 mg/kg | 6.3 | Male SD rats plasma protease | Scintillation proximity assay | Male SD rats plasma | In Vivo | None | None | Rat GTPγS (nM) EC50 ± SE = 4.39 ± 0.73 | |||
| 32582624 | 2020 | Entry 12 | 5 | Kψ[CH2NH]K substiuition | TMSAla-OH conjugation | Linear | L | Substiution of Y amino acid with K | NT(8-13) analogs | Improve Nts1-Induced Protective Hypothermia | NT(8-13) and compounds without reduced amine bounds were incubated during short incubation times (0, 1, 2, 5, 10, and 30 min), whereas all analogs with reduced amine bounds, except compound 2, were tested during longer incubation times (0, 1, 2, 4, 8, 16, and 24 h) at 37°C | 0.156 mM | 10 ± 1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Binding, Ki (nM) = 150 ± 60 for hNTS1 | |||
| 32348108 | 2020 | SAH-GLP-1-A8J(16,23,30) | 28 | Aminoisobutyric acid | Free | Linear | L | Modifcations include (R-octenyl alanine) and (bis-pentenyl glycine) and (S-octenyl alanine) | Single-stapled analogs of GLP-1 | Antidiabetes | 20 μl aliquots were removed at 0, 5, 15, 30, 60, 120 and 200 min | 10 μM | 320 | Mouse plasma protease | LC-MS/MS | Mouse plasma | In Vitro | PDB:3IOL | None | EC50 = 160 pM for SAH-GLP-1(16, 23, 30) | |||
| 32316169 | 2020 | GLP1_16HSA | 615 | Free | Free | Linear | L | Incorporation of HSA at V16 of GLP_1C | Synthetic | Antidiabetes | Blood samples (below 70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 2, 4, 8, 12, and 24 h after administration | 10 nmol/kg | 8.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | EC50 = 0.70 μM | |||
| 32316169 | 2020 | GLP1_19HSA | 615 | Free | Free | Linear | L | Incorporation of HSA at Y19 of GLP_1C | Synthetic | Antidiabetes | Blood samples (below 70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 2, 4, 8, 12, and 24 h after administration | 10 nmol/kg | 7.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | EC50 = 1.91 μM | |||
| 32316169 | 2020 | GLP1_28HSA | 615 | Free | Free | Linear | L | Incorporation of HSA at F28 of GLP_1C | Synthetic | Antidiabetes | Blood samples (below 70 μL) were collected from the retroorbital venous sinus at 0.16, 1, 2, 4, 8, 12, and 24 h after administration | 10 nmol/kg | 8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | None | None | EC50 = 6.85 μM | |||
| 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) | |||
| 35496622 | 2020 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 7.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.076 ± 0.013 for Lixisenatide (in vitro GLP-1 receptor activation potency) | |||
| 32133341 | 2020 | Apamin based analogs 9 | 21 | Free | Amidation | Cyclic(C1-C11, C3-C15 ) | L | None | Apamin based analogs | Roles in metabolism, arousal, learning and memory | N.A. | 0.05 μg/μl | 6.6 | Human serum protease | LC-MS | Human serum | In Vitro | None | None | Binding affinity pKi ± SEM [logM] = 6.76 ± 0.03 | |||
| 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 | |||
| 32023048 | 2020 | hICP NPs | 8 | Free | One 4-carboxy-3-fluorophenylboronic acid (PBA), Three cholic acids (CA) | Linear | L | ICP NPs were stacked into nanoparticle clusters upon coating with DA modified HA, Folic acid | Synthetic | Transcellular Tumor Penetration And Photo−Chemo Combination Therapy | Blood samples (∼0.2 mL each time point) were collected from the jugular vein cannula to centrifuge tubes containing 20 μL of 10 IU heparin at predetermined time points (5, 10, 15, 30, 60, 120, 180, 240, 360, 720, 1440 min) | 3 mg/kg | 7.97 ± 2.38 | Female wistar rats plasma protease | HPLC | Female wistar rats plasma | In Vivo | None | None | Additional phototherapy by treatment with laser further enhanced the antitumor activity of both ICP and hICP NPs, leading to a complete cure rate of 10% and 50%, respectively | |||
| 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 | |||
| 31809037 | 2020 | ApoE-Ms-SF | 19 | Free | PEG-P(CL-DTC) | Linear | L | None | Synthetic | Targeted Delivery Of Sorafenib To Hepatocellular Carcinoma | At fixed time points, 75 μL of blood was taken from the ophthalmic vein into a heparinized tube | 6 mg SF equiv/kg | 6.8 (Elimination Half-Lives) | BALB/c mice plasma protease | HPLC | BALB/c mice plasma | In Vivo | None | None | IC50: 8.5 μg/mL for ApoE-MS-SF | |||
| 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. | |||
| 31594790 | 2019 | Ac-RLYE | 4 | Acetylation | Free | Linear | L | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 8.8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 = 37.1 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31594790 | 2019 | rLYE | 4 | L-Arg replaced with D-Arg at position 1 | Free | Linear | Mix | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 7 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 >1,000 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 31594790 | 2019 | Ac-RLYE-NH2 | 4 | Acetylation | Amidation | Linear | L | None | Synthetic | Antitumor | 4 hours at 37°C | 2 µg/µl | 9.4 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50 = 52.5 pM (inhibitory activity against VEGF-A-induced tube formation of HUVEC) | |||
| 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 | |||
| 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 | |||
| 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 | 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 | |||
| 31278957 | 2019 | Ex-(EBP)10-6xHis | 96 | Free | Ten repeats of EBP without a linker sequence, (EBP)10 fused at the C-terminus of the exenatide for Ex-(EBP)10, 6xHis tag | Linear | L | Inserting valine to the X amino acid position in the EBP (VPGXG) sequence, labeled with Flamma® 675 vinylsulfone | Fusion protein of exenatide and elastin-based polypeptide from recombinant Saccharomyces cerevisiae | 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 | 7.7 | Mouse body protease | In vivo imaging system | Mouse body | In Vivo | None | None | N.A. | |||
| 31277465 | 2019 | Dox-peptide conjugate 13 | 14 | DOX | Free | Cyclic (Lys6-Glu14 bond) | L | C6 fatty acid linked between | Synthetic | Anticancer | An aliquot (40 µL) was removed at different time intervals, such as 4, 24, and 84 h | 0.25 mM | 10 | N.A. | RP-HPLC | PBS having pH values ranging from 6.5 to 7.4 | In Vitro | None | None | Dox conjugate 13 was moderately toxic with a reduced cell proliferation to a range of 25–35% as compared to Dox which reduced cell proliferation in the range of 20–34% for all selected four cell lines | |||
| 31276085 | 2019 | RWRWR peptide | 12 | Acetylation | Amidation | Linear | Mix | R amino acid substituition at 1,4, 11, FAM denotes 5,6-carboxyfluorescein conjugated with Orn,p=D-Proline6,O=Ornithine8 | Synthetic | Cell penetrating peptide | 37°C | 2 mg/ml | 420 | HeLa lysates protease | RP-HPLC | HeLa lysates + Assay buffer(10 mM Tris-HCl, pH 7.6) | In Vitro | None | None | N.A. | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected 5 min, 2, 6, 12, 24, 72 h post dosing | 10 mg/kg | 7.77 | Mouse plasma protease | LC–MS/MS | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600-6H | 118 | Free | PA-600-6H | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected at 15, 30 min, 1, 2, 3, 4, 8, 12,18, 24, 36, 48 and 72 h post dosing | 10 mg/kg | 7.03 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 5.2 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected immediately post dosing and at 5, 30 min, 2, 8, 24, 72 h post dosing | 3.5 mg/kg | 9.5 | Rats plasma protease | LC–MS/MS | Rats plasma | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. | 3 mg/kg | 8.31 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 8 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31156041 | 2019 | AD-114-PA600 | 118 | Free | PA-600 | Linear | L | None | Fusion protein of AD-114 with PA600 | Attenuates Renal fibrosis through blockade Of CXCR | Blood samples were collected pre-dosing and at the following time points post-dosing: 5 min, 1, 4, 12, 24, 48, 96, 168 h. | 10 mg/kg | 6.7 ± 1.1 | Cynomolgus monkeys plasma protease | LC–MS/MS | Cynomolgus monkeys plasma dosed at Day 8 | In Vivo | PDB id: >5AEA_1 | None | Kd(nM) = 4 (Human CXCR4 affinity) for AD-114-Im7-FH-PEG 30K | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 10 µg/kg | 5.4 ± 0.3 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 10 µg/kg | 5.8 ± 0.4 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 30 µg/kg | 5.4 ± 0.3 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 100 µg/kg | 5.2 ± 0.2 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 17.4 µ/kg | 9.0 ± 1.8 (Elimination Half Life) | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | N.A. | |||
| 31040673 | 2019 | CS-ES2-AF | 21 | CS (chondroitin sulfate) | VEGFR1-selective hexapeptide (GNQWFI, AF) ,amidation | Linear | L | FITC labeled | Synthetic | Antiangiogenic | Blood samples were collected through the fundus venous plexus, 0.5–24 hours after administration | 20 mg/kg | 7.57 ± 2.65 | Mice plasma protease | Fluorescence spectrometry | Mice plasma | In Vivo | None | None | The inhibitory rates of ES2-AF and CS-ES2-AF were similar (5 μg/mL–100 μg/mL), which indicated that the activity of ES2-AF was similar to CS-ES2-AF at relatively low concentrations | |||
| 35520704 | 2019 | Lip-Di-GLP-1 | 62 | Free | Bis-maleimide-C16 conjugation at C terminal | Linear | L | None | 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 | 7.0 ± 0.7 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | PDB id: 5VAI | None | EC50 = 0.056 ± 0.018 nM | |||
| 30904618 | 2019 | PAK | 253 | KLA linked with PsTag216 using flexible linker GGGGS at N terminal | Free | Linear | L | None | Fusion protein of PsTag216 and KLA | Antitumor | At 0.25 h, 0.5 h, 1 h, 2 h, 4 h, 8 h, 24 h, and 48 h post injection, a blood sample was obtained from the eye socket vein in mice | 1 μmol/kg | 5.05 ± 0.26 | Mice serum protease | ELISA | Mice serum | In Vivo | None | None | IC50 (μM) = 11.05 ± 0.73 for the cell line A375 (In vitro antitumor effects) | |||
| 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) | |||
| 30809901 | 2019 | FITC-AAR029b in Liposome | 6 | FITC labelled | Free | Macrocyclic | L | X=Structure given in paper | Derived from a class of peptides known as cyclic peptide triazoles (cPTs) | Antiviral | N.A. | 0.01 mg/kg | 8.87 ± 3.17(T1/2b-Elimination Half Life) | Rats plasma protease | Fluorescence assay | Rats plasma | In Vivo | None | None | EC50(nM) = 210±16 for AAR029b in Bal.01 virus | |||
| 30624060 | 2019 | Compound 27 | 6 | Lys(C18d-yGlu-(OEG)2) linker between hydroxyphenylacetic acid and peptide | Amidation | Linear | Mix | Nle = Nor-leucine, DMeAsp = N-methylated D-Asp, MePhe = Methylated-phenylalanine | CCK-8 analogue | Role in the regulation of energy balance | The blood samples were collected at following time points relative to dosing: predose, 0.083, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 10, 24, 48, 72, 96, 120, 168, 192, 216, 240, 264, and 288 h | 5 nmol/kg | 7.1 (Terminal Half Life) | Female göttingen minipigs plasma protease | LC-MS | Female göttingen minipigs plasma | In Vivo | None | None | pEC50 = 9.80 (In Vitro CCK-1R Potency) | |||
| 30600066 | 2019 | GSHP-ES2 | 11 | FITC-GSHP | Free | Linear | L | None | Synthetic | Antitumour, Antiangiogenic | Blood samples were collected through the fundus venous plexus 0.5–72 h after administration | 20 mg/kg | 9.11 | Mice plasma protease | fluorescence spectrometry | mice plasma | In Vivo | None | None | When the concentration was 5, 25, 50, 75, 100 and 125 μg/ml, the inhibitory rate of GSHP-ES2 was 6.47%, 16.47%, 24.57%, 31.36%, 44.45%, and 67.26%, respectively | |||
| 30543420 | 2019 | R2 | 53 | Free | Free | Linear | L | B-D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 7 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.025 ± 0.55 | |||
| 30517073 | 2019 | D6.4 | 178 | Free | Free | Linear | L | K142I mutation in El.3 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 5.3 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) =622 | |||
| 30517073 | 2019 | D6.4 | 178 | Free | Free | Linear | L | Q77E mutation | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 6.7 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) =451 | |||
| 30517073 | 2019 | D6.5 | 178 | Free | Free | Linear | L | T136V mutation in D6.4 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 6.8 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 620 | |||
| 30517073 | 2019 | D6.6 | 178 | Free | Free | Linear | L | Q77E mutation in D6.5 | LCN-2 derivative | Tightly complexes the plant poison colchicine for use as antidote as well as bioanalytical applications | 25°C | 256 nM | 9.4 | N.A. | Surface Plasmon Resonance (SPR) | PBS | In Vitro | Uniprot id: P80188 | None | KD(pM) = 702 | |||
| 30504081 | 2019 | VPGAG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 5.2 ± 0.1 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG160 | 800 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 7.3 ± 0.2 | N.A. | N.A. | N.A. | In Vitro | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPGAG160 | 800 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =G , X2= A | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 6.6 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50 = 10 nM for GLP1-VPGAG160 | |||
| 30504081 | 2019 | VPREG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =R, X2= E | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 9.6 ± 0.5 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30504081 | 2019 | VPRDG120 | 600 | A leader sequence (GCGYPG) was added to the N-terminus of the ZIPPs and ELPs to site specifically conjugate the maleimide derivative of Alexa488 | Free | Linear | L | X1 =R, X2= D | Zwitterionic polypeptide derivative | Intrinsically disordered zwitterionic polypeptides for drug delivery | 10 μl blood samples were collected into tubes with 100 μl of heparin at 40 s, 15 min, 0.5, 2, 4, 8, 24, 48 and 72 h after injection into the tail vein | 300 μM | 8.2 ± 0.3 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 30165247 | 2019 | PoIFN-α | 189 | Free | Free | Linear | L | None | Porcine IFN-α | Antiviral And Immune Regulatory Effects | Serum samples were collected at 0.5, 2.0, 4.0, 8.0, 12, 24,48, 72, 96, 120 and 144 h post injection | 2.5 mg/kg | 6.54 ± 0.16 | Rats serum protease | ELISA | Rats serum | In Vivo | None | None | On MDBK cell, PoIFNα-C2 protein showed almost 10-fold lower anti-VSV activity (3.0 × 107 U/μM) than that (2.4 × 108 U/μM) of PoIFN-α standard | |||
| 30555549 | 2018 | AuNp-DPA | 13 | Free | Au | Linear | L | None | Synthetic | Antitumor | N.A. | 2 mg/kg | 7.5 ± 0.8 | Mice blood protease | HPLC | Mice blood sample | In Vivo | None | None | AuNP-DPA inhibited tumor growth by 88% on day 13 compared to the control, even better than DOX (inhibition ratio of 64.3% in comparison with the control) | |||
| 30226777 | 2018 | E1 | 18 | Free | Free | Linear | L | None | Derived from the E1 envelope protein of GBV-C | HIV-1 fusion inhibitor peptide | At different incubation times (30 min, 1, 2, 4, 8, and 24 h) | 1 mg/mL | 8 | Human serum protease | HPLC | Human serum | In Vitro | None | None | N.A. | |||
| 30165332 | 2018 | DV1 | 21 | Free | Amidation | Linear | D | All D-amino acids | Synthetic | CXCR4 antagonist | Blood samples were collected into heparin-coated polypropylene centrifuge tubes at 0, 5, 10, 15, 30 min and 1, 2, 4, 6, 8, 12, 24, 36 and 48 h after the dose | 10 mg/kg | 8.7 ± 2.4 | Rats plasma protease | HPLC-MS/MS | Rats plasma | In Vivo | None | None | N.A. | |||
| 30012756 | 2018 | Murepavadin | 14 | Free | Free | Cyclic (N-C terminal end) | Mix | Acetate | Synthetic | Antimicrobial | Blood samples were taken predose and 1, 2, 3, 3.5, 4, 5, 6, 9, 15, and 27 h after the start of infusion | 2.2 mg/kg | 7.7 | Human plasma protease | LC-MS with electrospray ionization assay | Human plasma (Healthy Renal impairment group) | In Vivo | https://sci-hub.st/10.1080/14787210.2018.1441024 | None | MIC50 = 0.12 mg/L against P. aeruginosa | |||
| 29926478 | 2018 | MEDI0382 | 29 | Free | Free | Linear | L | Palmitic-Glu conjugation at Lys | Synthetic | Antidiabetes and Non‐Alcoholic Steatohepatitis | N.A. | 300 μg | 9.54 | Human plasma protease | LC-MS | Human plasma | In Vivo | PubChem CID: 134694273 | None | N.A. | |||
| 29799205 | 2018 | 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 | |||
| 29732120 | 2018 | Analogue 6 | 5 | Free | Free | Macrocyclic (N-C terminal end) | Mix | D-Phe | Synthetic | Inhibits pro-angiogenic integrins | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 9 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50(μM) = 140 ± 95 against αvβ3 | |||
| 29732120 | 2018 | Analogue 12 | 5 | Free | Free | Macrocyclic (N-C terminal end) | L | None | Synthetic | Inhibits pro-angiogenic integrins | At various time points (0, 1, 3, 5. 7, 9, 12, 24, 36, 48, 60 and 72 h) | 1 mg/ml | 7 | Human serum protease | HPLC | Human serum | In Vitro | None | None | IC50(μM) = 166 ± 98 against αvβ3 | |||
| 29721065 | 2018 | 64Cu-DOTA-F56-CM | 12 | 64Cu-DOTA | maleimidopropionic acid (MPA) at the C-terminal | Linear | L | None | Maleimidopropionic acid-conjugated peptide | Antiangiogenic | At 10, 30, 60, and 120 min | 7.4 mBq | 6.967 | SD rats blood protease | Radioactivity assay | SD rats blood | In Vivo | None | None | F56 and F56-CM reduced the angiogenesis of zebrafish embryos in a dose-dependent way | |||
| 29517911 | 2018 | 2b | 13 | Free | Free | Bicyclic (Cyclized On C1, C7, C13 By 1,3,5 Trismethylbenzene) | L | None | 2a analogue | Antidiabetes | 24 h at 37 °C | 0.16 mM | 7 | Human plasma protease | LC-MS/MS | Human plasma | In Vitro | None | None | Ki Values (nM) = 2.0 ± 0.9 against PKal from Rats | |||
| 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. | |||
| 29461833 | 2018 | Pyr analogue 6 | 13 | pGlu = Pyroglutamate | Free | Cyclic (Rx4-X8 Bond) | L | X= allylglycine, Rx=Na-ally-arginine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 7.7 ± 0.3 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 9.1 ±1.4 for 6 | |||
| 29461833 | 2018 | Pyr analogue 7 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X4-X8 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 9.9 ± 1.2 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 489 ±186 for 7L | |||
| 29461833 | 2018 | Pyr analogue 11 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X7-X11 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 6.6 ±0.4 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 1.4 ±0.4 for 11 | |||
| 29461833 | 2018 | Pyr analogue 13 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X9-X13 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 8.6 ±0.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 1.1 ±0.1 for 13 | |||
| 29461833 | 2018 | Pyr analogue 14 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X10-X14 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 7.8 ±1.1 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 445 ±62 for 14L | |||
| 29461833 | 2018 | Pyr analogue 15 | 13 | pGlu = Pyroglutamate | Free | Cyclic (X9-X13 Bond) | L | X= allylglycine, Nle = Nor-leucine | Pyr-13 analogue | Effects on Cardiac and Renal Functions as well as survival in a Systemic Inflammation Model Of Sepsis and Septic Shock | At selected time points (0, 2, 4, 7, and 24 h or 0, 10, 20, 60, and 120 min). | 1 mM | 6.8 ±1.6 | Rats plasma protease | UPLC-MS | Rats plasma | In Vitro | None | None | Ki binding (nM) = 0.15 ±0.01 for 15 | |||
| 29436835 | 2018 | Chol-PEG5k-PIE12-trimer | 48 | Chol-PEG5K-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 5.6 | Rats plasma protease | UHPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.030 ± 0.0010 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PEG5k-PIE12-trimer | 48 | Chol-PEG5K-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 7.2 | Rats plasma protease | UHPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.030 ± 0.0010 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 5.4 | Rats plasma protease | Ultra-High Performance Liquid Chromatography (UHPLC) | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | One ml blood samples were collected by venipuncture of a femoral vein at 0.083, 0.167, 0.25, 0.5, 1, 2, 4, 8, 16 and 24 h | 1 mg/kg | 7.4 | Male cynomolgus monkeys plasma protease | LC-MS | Male cynomolgus monkeys plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 1 (cycle 1 - 28days) | 96 mg/m2 | 6 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29423221 | 2018 | dTCApFs | 14 | Free | Free | Linear | D | None | Synthetic | Anticancer | day 29 (Cycle 2 day1) | 96 mg/m2 | 8.5 | Human plasma protease | N.A. | Human plasma | In Vivo | None | None | N.A. | |||
| 29391187 | 2018 | Peptide 6 | 41 | Free | ABD domain from Streptococcal G strain , Amidation | Linear | L | None | [Ser8]-GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein using a heparinised syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h postdose | 0.01 mg/kg | 5.8 ± 0.4 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC50(nM) = 1.7 | |||
| 29391187 | 2018 | Peptide 6 | 41 | Free | ABD domain from Streptococcal G strain , Amidation | Linear | L | None | [Ser8]-GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein using a heparinised syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h postdose | 0.01 mg/kg | 5.4 ± 0.3 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC50(nM) = 1.7 | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 7.14 | Rats serum protease | LC-MS | Rats serum after 5 mg/kg sHDL-PEG2k | In Vivo | None | None | N.A. | |||
| 29141139 | 2018 | 22A | 22 | Free | Free | Linear | L | None | ApoA-I mimetic peptide | Treatment of Cardiovascular Diseases | At pre-dose and 0.25, 0.5, 1, 2, 4, 8, 24 and 48 hours after dosing | 20 mg/mL | 5.05 | Rats serum protease | LC-MS | Rats serum after 2.5 mg/kg sHDL-PEG5k | In Vivo | None | None | N.A. | |||
| N.A. | 2018 | TRAIL-ASPD | 347 | Free | C-type lectin domain of human SP-D joined with Strep-tag II using linker | Linear | L | None | Trail-SPD Fusion Protein | Therapeutic, diagnostic and/or research applications | Serum samples were collected after several time points (predose, 5 min., 30 min., 2H, 6H and 24H) | 10 μg | 7 | CD1 mice serum protease | ELISA | CD1 mice serum | In Vivo | None | EP 17197297 A | TRAIL-SPD fusion proteins induced no hepatotoxic effects, even if ligands were secondarily cross-linked by antibodies | |||
| 29263923 | 2017 | FITC-conjugated E5 | 22 | FITC conjugation | Free | Linear | L | None | Synthetic | Inhibit Breast Tumor Progression | N.A. | 40 mg/kg | ~10 | Mouse serum protease | Fluorescence assay | Mouse serum | In Vivo | None | None | E5 (0.1 μM) had high affinity towards 4T1 cells and HUVECs | |||
| 29176766 | 2017 | M10 | 10 | Free | Free | Linear | L | None | Derived from the C-terminal part of the MET receptor tyrosine kinase | Antifibrotic | Plasma samples were collected by cardiac puncture in the presence of 0.01% of Na-Citrate at time intervals of 15 min, 30 min, 1h, 2h, 4h, 6h, 12 h, 24 h, and 48 h following injection | 1 mg/kg | 6.8 ± 0.7 | Mouse plasma protease | ELISA | Mouse plasma | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC4789156/ | None | N.A. | |||
| 28821462 | 2017 | LCFN72 | 183 | Free | Fusing the XTEN peptide of 72 amino acids through a linker | Linear | L | Gly-rich linker (GSSGGSGSSGGSGGGDEADGSRGSQKAGVDE) is used, Cy5 dye (Lumiprobe) were chemically conjugated to the amine groups of lysine residues on the exterior surface of the nanocages | wtFN derivative | Antitumor | N.A. | 50 mg/kg | 5.5 ± 0.1 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28799326 | 2017 | GLP-1-PEG-WT-albumin | 616 | Free | GLP-1 modified PEG-Mal group reacts with the free C34 of rHSA, chemical group attached between Lys31 (8-amino-3,6-dioxaoctanoyl-maleimidopropionyl) and D32 | Linear | L | None | Produced by secretion from yeast | 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 | 8.5 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | None | None | KD±SD (nM) = 856.5±94.9 against human FcRn receptor | |||
| 28799326 | 2017 | GLP-1-PEG-HB-albumin | 616 | Free | GLP-1 modified PEG-Mal group reacts with the free C34 of rHSA, chemical group attached between Lys31 (8-amino-3,6-dioxaoctanoyl-maleimidopropionyl) and D32 | Linear | L | K573P modification in HSA,GLP-1 modified with PEG-maleimide | Produced by secretion from yeast | 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 | 9.9 | NMR1 mice serum protease | AlphaLISA | NMR1 mice serum | In Vivo | None | None | KD±SD (nM) = 26.1±2.7 against human FcRn receptor | |||
| 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 | |||
| 28721592 | 2017 | GCSF-Lα | 462 | Met addition at N terminal of G-CSF | Free | Linear | L | Dimer joined by linker La - SGLEA–(EAAAK)4–ALEA–(EAAAK)4–ALEGS | Homodimeric G-CSF | Selectively stimulate proliferation | Blood samples were drawn from the rats at selected time points (0, 3, 6, 12, 18, and 24 h after injection) | 150 μg/kg | 8.7 | Rats serum protease | ELISA | Rats serum | In Vivo | Genbank accession no. NM_172219 | None | in vitro activity of GCSF-La reached 48% of that of the G-CSF monomer | |||
| 28714475 | 2017 | tagUK18 | 24 | tag | Free | Bicyclic(C9-C16,C16-C23 Disulfide Bond In Uk128) | L | Lys4 linked with Palm fatty acid | Synthetic | Inhibit urokinase | N.A. | 0.5 mg/kg | 7.4 ± 0.2 (T1/2b) | Rats plasma protease | RP-HPLC using a fluorescence detector | Rats plasma | In Vivo | None | None | Albumin binding (Kd) (nM) = 780±110 for rat albumin | |||
| 28714475 | 2017 | tag-3xPEG24-FXIIa inhibitor | N.A. | Tag-3xPEG24 | Amidation | Bi-Cyclic(C2-7, C7-C12 Disulfide Bond In Fxiia Inhibitor) | L | None | Synthetic | FXIIa Inhibitor | N.A. | 5 mg/kg | 5.2 ± 0.4 (T1/2b) | Rabbit plasma protease | RP-HPLC using fluorescence detector | Rabbit plasma | In Vivo | None | None | (EC5x) at 4.2±0.5 mM | |||
| 28711730 | 2017 | rhCNTF-ABD | 251 | Free | ABD035 | Linear | L | Linked by (G4S)3 linker | Fusion of recombinant human CNTF (rhCNTF) with an albumin-binding domain (ABD) | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 483.39 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50±SD = 0.51±0.18 for rhCNTF-ABD | |||
| 28711730 | 2017 | PEG-20k-rhCNTF | 187 | PEGylation (20KDa) | Free | Linear | L | None | Synthetic | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 441.24 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50±SD = 0.48±0.12ng/ml for rhCNTF | |||
| 28711730 | 2017 | PEG-40k-rhCNTF | 187 | PEGylation (40KDa) | Free | Linear | L | None | Synthetic | Treatment of Neurodegenerative or Metabolic diseases | At different time points (15min, 45min, 90min, 3h, 6h, 12h, 24h and 48h) | 1 mg/kg | 523.89 | SD rats serum protease | ELISA | SD rats serum | In Vivo | None | None | EC50±SD = 0.48±0.12ng/ml for rhCNTF | |||
| 28691076 | 2017 | Cyclic D,L-α-Peptides | 8 | Free | free | Cyclic | Mix | D-amino acid substituitons | Synthetic | Antiatherosclerotic | Blood was drawn (30–60 μL) from the retro-orbital sinus into a heparinized capillary tube before dosing (0 min) and at different intervals from 30 min to 8 h after dosing | 20 g | 6 | BALB/c mouse plasma protease | LC-MS/SIM | BALB/c mouse plasma | In Vivo | None | None | cytotoxicity LD50 (μM) = 36 for NCI | |||
| 28668697 | 2017 | 7c | 29 | Free | Free | Linear | L | X3= Structure given in paper, n = 108 | Derived from Xenopus GLP-1 | Antidiabetes | Blood samples (approximately 100 µL) were collected from the lateral tail vein at 0, 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 6, 8, 12 and 16 h | 50 nmol | 5.67 ± 0.30 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 1.4 ± 0.2 for peptide 7 (potency on the cloned human GLP-1 receptor) | |||
| 28606508 | 2017 | SAPSP-Dox | 21 | Dox = Doxorubicin, Cys incorporation for linking | Amidation | Linear | L | None | SAPSP peptide | Anticancer | 37 °C | 0.1 mM | 9.58 | Fetal Bovine Serum protease | RP-HPLC | Fetal Bovine Serum | In Vitro | None | None | IC50 (microM) = 1.19±0.13 against MCF-7 cells | |||
| 27881716 | 2017 | 22A-sHDL | 22 | Free | sHDL | Linear | L | None | 22A and sHDL fusion protein | Antiatherosclerotic | Blood collection at pre-dose and 0.25, 0.5, 1, 2, 4, 8 and 24 after dosing | 75 mg/kg | 6.27 | Rats serum protease | LC-MS | Rats serum | In Vivo | None | None | EC50 (mg /dL) = 53.77 | |||
| 27656777 | 2016 | VH4129 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic (C1-C8 Disulfide Bond) | Mix | c = D-Cys and Sar modification , Pip = Pipecolic acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 6.66 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | N.A. | |||
| 27656777 | 2016 | VH4131 | 8 | Pr = propionylation, c = D-Cys at N terminal | Amidation | Cyclic | Mix | c = D-Cys and Sar,Pen, Pip = non-natural amino acid | VH445 analogues | Vectors targeting the LDL receptor | Incubated at 4°C or 37°C | 2 µM | 10 | Mouse plasma protease | LC-MS/MS | (CD-1) mouse plasma | In Vitro | None | None | Introduction of the non-natural Sar residue at the Gly7 position had only minor impact on the affinity (compare VH4128 to VH4127 and VH4131 to VH4130 | |||
| 27243004 | 2016 | Api794 | 22 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (WO)3 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 311 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) = 0.28 ± 0.03 in HEK293 | |||
| 27243004 | 2016 | Api795 | 20 | Gu: N,N,N',N' tetramethylguanidino | Free | Linear | L | O = L-ornithine, (IO)2 repititive motifs substituited | Analogs of Api137 | Antimicrobial | After 0, 1, 2, 3, and 6 h aliquots (95 μL) were precipitated with aqueous TCA (25 μL, 15% w/v) | 70 mg/L | 354 | Mouse serum protease | N.A. | Mouse serum | In Vitro | None | None | IC50(g/l) > 0.6 in HEK293 | |||
| 27217590 | 2016 | PF1 | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | Substitution of the Pro7 to Gly and Leu8 to a Lys appended with a polyethylene glycol space and a palmitoyl group, Palm = Palmitic acid | OT analog | Non–brain-penetrant OT receptor agonist | Time points postdose: 0.033, 0.083, 0.25, 0.5, 1, 2, 4, 7, and 24 hours | 0.1 mg/kg | 8.5 | Wistar rats plasma protease | LC-MS/MS | Wistar rats plasma | In Vivo | None | None | EC50(nM) = 0.025 (OTR agonist) | |||
| 27217590 | 2016 | OT (oxytocin) | 9 | Free | Amidation | Cyclic (C1-C6 Disulfide Linkage) | L | None | Produced in the hypothalamus and released by the posterior pituitary gland | Treatment of Psychiatric Diseases, Including Autism Spectrum Disorders And Schizophrenia | Serial blood samples were collected from each mouse via the retro-orbital sinus at the following time points postdose: 0.5, 1, 2, 4, 6, and 24 hours | 20 mg/kg | 7.3 | C57Bl/6J mice plasma protease | LC-MS/MS | C57BL/6J mice plasma | In Vivo | None | None | EC50(nM) = 0.039 (OTR agonist) | |||
| 27166982 | 2016 | ADM analogue 3 | 39 | Tam (6-Carboxytetramethylrhodamine) labeling, Glycine substitution at position 1 | Amidation | Cyclic (C3-C8 Disulfide Linkage) | L | None | ADM analogue | Treatment of Cardiovascular Diseases | 37°C | 0.00001 M | 9.7 | Human blood plasma protease | RP-HPLC | Human blood plasma | In Vitro | None | None | EC50 = 13.2 nM for ADM analogue 15 | |||
| 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 | |||
| 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 | |||
| 26806490 | 2016 | CTP-IFN | 193 | CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG)) | Free | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 7.8 ± 0.7 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | PDB id: 1HCN | None | Specific antiviral bioactivity (U ng−1) = 65 ± 3, Specific antiproliferative bioactivity (U ng−1) = 19 ± 9 | |||
| 26806490 | 2016 | IFN-CTP | 193 | Free | CTP ( the terminal peptide of the β subunit of human chorionic gonadotropin (hCG)) | Linear | L | None | Recombinant human IFN-α2b | Antiviral, Anticancer | N.A. | 1*106 U / 200 g | 8.4 ± 1.5 (Elimination Half Life) | Wistar rats plasma protease | N.A. | Female Wistar rats plasma | In Vivo | None | None | Specific antiviral bioactivity (U ng−1) = 58 ± 6, Specific antiproliferative bioactivity (U ng−1) = 26 ± 8 | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 36 mg/kg | 5.18 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 1 | 180 mg/kg | 5.5 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 3.6 mg/kg | 6.6 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 3.6 mg/kg | 7.75 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 36 mg/kg | 5.36 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 180 mg/kg | 6.24 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) | |||
| 26713839 | 2016 | MOD-4023 | 275 | CTP fused to hGH | 2 CTP fused | Linear | L | None | Synthetic | Treatment of GHD | Day 26 | 180 mg/kg | 6.2 | Rats serum protease | Sandwich ELISA | Rats serum | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC3159989/, PDB id: 1HGU | None | EC50 = 15.8 ± 2.0 ng/ml (Proliferation of BAFB2B2 cells) |