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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 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 22286034 | 2012 | Motilin | 22 | Free | Free | Linear | L | None | Motilin is a gastro-intestinal peptide hormone | Endocrine regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 3.3 ±1.0 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.9x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(6 €“28) | 35 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 11.7 ±3.4 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.5x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(8 €“28) | 33 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 11.1 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.4x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(10 €“28) | 31 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.6x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“28) | 29 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.9 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.6x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(14 €“28) | 27 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 8.0 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=6.1x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(16 €“28) | 25 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 9.4 ±0.6 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.2x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(18 €“28) | 23 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 5.3 ±1.3 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.0x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(19 €“28) | 22 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 6.0 ±0.3 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.1x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“26) | 27 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 10.4 ±0.1 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.5x10-9nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“24) | 25 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 5.8 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=4.8x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“22) | 23 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 6.3 ±0.5 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=2.4x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“20) | 21 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 7.0 ±2.6 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=7.3x10-11nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“18) | 19 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 3.1 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=8.8x10-10nM for GPR38 agonist activity | |||
| 22286034 | 2012 | Motilin(1 €“12)ghrelin(12 €“16) | 17 | Free | Free | Linear | L | None | Chimeric peptide of motilin and ghrelin | Regulator of gastro-intestinal motility | Not mentioned | 10 nmol/kg | 2.4 ±0.7 | Rat plasma proteases | Radioimmunoassay | Intravenouly injected in Sprague-Dawley rats | in vivo | None | None | EC50=1.2x10-10nM for GPR38 agonist activity | |||
| 22592200 | 2012 | Ghrelin | 28 | Free | Free | Linear | L | Fatty acid ie n-octanoic acid present at serine at position 3, (125)I labelling | Ghrelin | GH-releasing and appetite stimulating peptide | Not reported | Not mentioned | 15-18 | Rat blood proteases | Radioactivity measured by scintillation counter | Administered into blood of rats | in vivo | 15788704 | None | Not reported | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 5.6 ±0.45 | Human blood proteases | Not mentioned | Human plasma of patients with mild, stable heart failure | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 11 ±1.3 | Human blood proteases | Not mentioned | Human plasma of patients with mild, stable heart failure given infusion of metoprolol | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 5.7 ±0.8 | Human blood proteases | Not mentioned | Human plasma (Normal humans) | in vivo | None | None | Not given | |||
| 16476851 | 2014 | BNP | 32 | Free | Free | Linear | L | None | B-type cardiac natriuretic peptides | Vasodilator | Not reported | Not mentioned | 6.6 ±1.3 | Human blood proteases | Not mentioned | Human plasma (Normal humans given infusion of metoprolol) | in vivo | None | None | Not given | |||
| 19552923 | 2011 | GLP-1-Tf | 30 | Human transferrin protein | Amidation | Linear | L | None | Proglucagon molecule | Insulinomimetic and insulinotropic | Not reported | 27.9 ± 5.8 μg/ml | 27 | Rabbit blood proteases | ELISA | Rabbit serum (Intravenous injection) | in vivo | None | None | Not available | |||
| 19552923 | 2011 | GLP-1 | 30 | Free | Amidation | Linear | L | None | Proglucagon molecule | Insulinomimetic and insulinotropic | Not reported | 27.9 ± 5.8 μg/ml | 1 to 2 | Rabbit blood proteases | ELISA | Rabbit blood | in vivo | None | None | Not available | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 52.1 | Mouse blood proteases | EIA | Mice blood serum (oral delivery in 0.5% Intravail) | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 25.8 | Mouse blood proteases | EIA | Mice blood serum (oral delivery in 1.5% Intravail) | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 23.6 | Mouse blood proteases | EIA | Mice blood serum (oral delivery in 3.0% Intravail) | in vivo | None | None | Not mentioned | |||
| 21329733 | 2011 | Octreotide acetate | 8 | Free | Free | Cyclic (C2-C7) | Mix | 2-hydroxy-1-(hydroxymethyl) | Synthetic analog of Somatostatin | Used for treatment of acromegaly | Not reported | 30μg/100μl | 1.3 | Mouse blood proteases | EIA | Mice blood serum (Subcutaneous injection) | in vivo | None | None | Not mentioned | |||
| 21334413 | 2011 | Exendin-4 | 39 | Free | Free | Linear | L | None | Venom of the lizard Heloderma suspectum | Binds and activates the GLP-1 receptor | Not reported | 500 μg/kg | 2.4 | Rat blood proteases | Radioimmunoassay | Rat plasma | in vitro | None | None | Not mentioned | |||
| 21664938 | 2011 | GLP-1 | 30 | Free | Free | Linear | L | None | Proglucagon molecule | Anti-hyperglycemic hormone | Not reported | 300 μg/kg | <2 | Rat blood proteases | ELISA | Serum of rats (Subcutaneous injection) | in vivo | None | None | Binding constants to the GLP-1 receptor= 27.62 ± 2.13nM | |||
| 21664938 | 2011 | GLP715a | 46 | Free | Free | Linear | L | None | Proglucagon molecule | Anti-hyperglycemic hormone | Not reported | 300 μg/kg | 48 | Rat blood proteases | ELISA | Serum of rats (Subcutaneous injection) | in vivo | None | None | Binding constants to the GLP-1 receptor= 6.18 ± 1.27nM | |||
| 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 | DAMGO | 5 | Free | Free | Linear | Mix | Methylation at phenylalanine | Synthetic peptide | Opioid peptide | Not reported | 5.0 mg/kg | 9.2 ± 2.1 | Rat blood proteases | ESI-LC ˆ’MS/MS | Rat blood plasma (Intravenous) | 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 | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 0.1 mg/kg | 19.0 ± 2.0 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.67 106/ µl 21 days after the administration | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 0.5 mg/kg | 34.0 ± 5.9 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.67 106/ µl 21 days after the administration | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 5 mg/kg | 99.0 ± 37.1 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.67 106/ µl 21 days after the administration | |||
| 23318685 | 2013 | Peginesatide | 40 | Acetylation | Dimerization using PEGylation | Cyclic (C6-C15, C26-C35) | L | Nal, Pegylation | Synthetic peptide | Erythropoiesis-stimulating agent | Not reported | 5[C14] mg/kg | 84.0 ± 9.56 | Monkey blood proteases | ELISA | Monkey blood plasma | in vitro | None | None | Increase in RBCs of 1.73 106/ µl 21 days after the administration | |||
| 23836030 | 2013 | HNG ( substitution at position 14 (Gly for Ser) in HN seq) | 24 | Free | Free | Linear | L | None | Synthetic peptide | Cytoprotective | Not reported | 16 fold higher than original concentration | ~30 | Mouse plasma proteases | ELISA | Mice plasma | in vitro | 15655255 | None | Not available | |||
| 24378440 | 2013 | EGFR2R-lytic peptide | 32 | Free | Free | Linear | Mix | None | Synthetic peptide | Cytotoxic and antitumor | Not reported | Not mentioned | 9.4 ± 1.5 | Not mentioned | Not mentioned | Bovine serum | in vivo | None | None | Not available | |||
| 24378440 | 2013 | EGFR2R-lytic peptide-gelatin complex | 32 | Free | Free | Linear | Mix | None | Synthetic peptide | Cytotoxic and antitumor | Not reported | Not mentioned | 19.3 ±2.9 | Not mentioned | Not mentioned | Bovine serum | in vivo | None | None | Not available | |||
| 8181115 | 2014 | Atrial natriuretic factor (ANF) | 28 | Free | Free | Linear | L | None | Cardiac atria | Peptide hormone | Not reported | Not mentioned | 2.5 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not available | |||
| 8406670 | 2014 | Atrial natriuretic factor (ANF) | 28 | Free | Free | Linear | L | None | Cardiac atrium in response to myocardial stretch | Peptide hormone | Not reported | Not mentioned | 20 to 180 | Human blood proteases | Radioimmunoassay | Human blood plasma | in vitro | None | None | Not available | |||
| N.A. | 2011 | Motilin | 22 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 3.26 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin A | 35 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.74 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin B | 34 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin C | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.9 ±0.53 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin D | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.9 ±0.50 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin E | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin F | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.37 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin G | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.25 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin H | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.43 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin I | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.76 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin J | 25 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 6.34 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin K | 23 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 6.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin L | 21 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 4.89 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin M | 19 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 2.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin N | 28 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.12 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin O | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.73 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin P | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.67 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Q | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.65 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin R | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.13 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin S | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.29 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin T | 29 | Free | Free | Linear | L | Ornithine | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.47 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin U | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.66 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin V | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.14 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin W | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin X | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.89 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Y | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.6 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin Z | 30 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.53 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-i | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.55 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-ii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.5 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-iii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.65 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-iv | 27 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 7.73 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-v | 29 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 8.94 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-vi | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 9.94 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-vii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 12.78 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-viii | 31 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 11.56 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-ix | 26 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 4.39 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-x | 28 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 5.25 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xi | 26 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 10.29 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xii | 33 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 13.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric Motilin-xiii | 34 | Free | Free | Linear | L | None | Motilin | Regulator of motility of digestive tract | N.A. | 10 nM/ Kg | 13.09 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 2.88 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-A | 39 | Free | Free | Cyclic (C1-C17) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 24 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-B | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 40 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-C | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 27.2 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 11.2 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-A | 39 | Free | Free | Cyclic (C1-C17) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 46.4 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-B | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 57.3 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric ANP-C | 39 | Free | Free | Cyclic (C18-C34) | L | None | ANP (Atrial natriuretic peptide) | Regulator of sodium ions in heart | N.A. | 0.1 mg/ Kg | 37.8 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 7.8 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-A | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 20.7 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-B | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 24 | Not mentioned | Competitive Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 2.93 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-A | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 21.7 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-B | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 0.1 mg/ Kg | 362 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-C | 34 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 15.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-D | 37 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 20.3 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-E | 46 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 18.4 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-F | 51 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 17.38 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-G | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 17.75 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-H | 34 | Free | Free | Cyclic (C18-C34) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 14.86 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-I | 34 | Free | Amidation | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 14.5 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-J | 39 | Free | Free | Cyclic (C6-C22) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 20 nm/ Kg | 31.24 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-K | 35 | Free | Free | Cyclic (C1-C17) | L | None | CNP-22 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 20 nm/ Kg | 18.03 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-53 (C-type natriuretic peptide) | 58 | Free | Free | Cyclic (C42-C58) | L | None | CNP-58 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 15.72 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2011 | CNP-22 (C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | CNP-58 (C-type natriuretic peptide) | Third member of natriuretic peptide family with multiple functions | N.A. | 10 nm/ Kg | 1.11 | Rat blood proteases | Competitive Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP2277890A1 | Not mentioned | |||
| N.A. | 2012 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | 520 micro g/Kg | 0.8 | Not mentioned | EIA | Rat plasma (Subcutaneous) | in vivo | None | EP2423233A2 | Blood glucose after 24 hour >25 mM | |||
| N.A. | 2012 | Exendin-4-α1AT(P357N) | 39 | Free | Fusion of Alpha-1 Antitrypsin Monovariant [α1AT(P357N)] | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | 520 micro g/Kg | 19.1 | Not mentioned | EIA | Rat plasma (Subcutaneous) | in vivo | None | EP2423233A2 | Blood glucose after 24 hour ~10 mM | |||
| N.A. | 2013 | SP16 | 13 | Free | Free | Linear | L | None | Human alpha-1-antitrypsin | Anti-inflammatory and immune modulator peptide | N.A. | 5 mg/ Kg | 1.9 | Rat blood proteases | LC-MS/MS | Rat plasma (Intravenous) | in vivo | None | WO2013106273A2 | Not mentioned | |||
| N.A. | 2012 | Intermedin or adrenomedullin peptide | 39 | Free | Free | Linear | L | None | Preproadrenomedullin | Calcium homeostasis | N.A. | Not mentioned | 1.5 | Rat blood proteases | ELISA | Rat plasma (Intravenous) | in vivo | None | WO2012138867A2 | Not mentioned | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ kg | 1.5 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 1.3 | Not mentioned | Radioimmunoassay | Rat plasma (Subcutaneous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | Val8-GLP-1-OH | 31 | Free | Addition of hydroxyl group | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 10 micro g/ kg | 0.05 | Rat blood proteases | Radioimmunoassay | Rat plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 100% (as reference) | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 59.5 | Monkey blood proteases | Radioimmunoassay | Monkey plasma (Intravenous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | V8E22I33C45-40kDa PEG | 39 | Free | Pegylation | Linear | L | None | Glucagon like peptide1 | Insulinotropic peptide | N.A. | 0.1 mg/ Kg | 61.6 | Not mentioned | Radioimmunoassay | Monkey plasma (Subcutaneous) | in vivo | None | EP1605897B1 | EC50= 9.4% with respect to Val8-GLP-1-OH | |||
| N.A. | 2012 | Exendin-4 | 39 | Free | Free | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 0.7 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 100% (as reference) | |||
| N.A. | 2012 | Exendin-4(N)-PEG-Fc | 39 | Pegylation | Addition of Fc | Linear | L | None | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 62 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= <0.2 % with respect to Exendin-4 | |||
| N.A. | 2012 | Exendin-4(Lys27)-PEG-Fc | 39 | Free | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 61 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 13.2 % with respect to Exendin-4 | |||
| N.A. | 2012 | DM exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into dimethylhistidyl (DM) group | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 69 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 2.6 % with respect to Exendin-4 | |||
| N.A. | 2012 | DA exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into desaminohistidyl (DA) group | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 54 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 13.2 % with respect to Exendin-4 | |||
| N.A. | 2012 | HY exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into betahydroxylamidazolpropionyl (HY) | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 52 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 7.6 % with respect to Exendin-4 | |||
| N.A. | 2012 | CA exendin-4(Lys27)-PEG-Fc | 38 | Modification of His1 of Exendin-4 into imidazoacetyl (CA) group | Addition of Fc | Linear | L | Pegylation at K27 | Venom of Heloderma horridum | Insulinotropic peptide | N.A. | Not mentioned | 52 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 8.5 % with respect to Exendin-4 | |||
| N.A. | 2012 | DA GLP-1 (Lys20,28)-PEG-Fc | 39 | Modification of His1 of Exendin-4 into desaminohistidyl (DA) group | Addition of Fc | Linear | L | Pegylation at K20 and K28 | Glucagon like peptide1 | Insulinotropic peptide | N.A. | Not mentioned | 27 | Not mentioned | Not mentioned | blood | Not mentioned | None | EP2114438B1 | EC50= 2 % with respect to Exendin-4 | |||
| 7911441 | 2014 | Octreotide | 8 | Free | Free | Cyclic (C2-C7) | L | None | Somatostatin analogue | Growth Hormone Inhibitor | Not mentioned | 125 μg/kg | 113 | Patient blood proteases | Not mentioned | Patients with severe renal impairment | in vivo | None | None | Octreotide considerably inhibits pentagastrin stimulated gastric acid secretion and significantly diminishes exocrine pancreatic function. | |||
| 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. | |||
| 21185160 | 2011 | O-1(Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 68 ±15 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-1(Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 25 ±4 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-2 (Oncocin) | 18 | Free | Free | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 120 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 64 μg/mL in E.coli BL21A1 and 128 μg/mL M.luteus | |||
| 21185160 | 2011 | O-4 (Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 120 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC =16μg/mL in E.coli BL21A1 and 64 μg/mL M.luteus | |||
| 21185160 | 2011 | O-5 (Oncocin) | 19 | Free | Amidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 90 ±1 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 16 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-6 (Oncocin) | 19 | Free | Amidation | Linear | L | Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 210 ±60 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-7 (Oncocin) | 19 | Free | Amidation | Linear | L | Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 98 ±6 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 8μg/mL M.luteus | |||
| 21185160 | 2011 | O-8 (Oncocin) | 19 | Free | Amidation | Linear | L | Nir=Nitro-arginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 78 ±2 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-9 (Oncocin) | 19 | Free | Amidation | Linear | L | Nmr =N-methylarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 79 ±3 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-10 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 94 ±1 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-11 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 19th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 160 ±5 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4μg/mL in E.coli BL21A1 | |||
| 21185160 | 2011 | O-12 (Oncocin) | 19 | Free | Propylamidation | Linear | L | None | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | >120 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-14 (Oncocin) | 19 | Free | Amidation | Linear | L | orn =Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 90 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-15 (Oncocin) | 19 | Free | Amidation | Linear | L | Beta-Hr =β-homoarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 150 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4μg/mL in E.coli BL21A1 and 16 μg/mL M.luteus | |||
| 21185160 | 2011 | O-16 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 15th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 58 ±2 | Mouse serum proteases | MALDI-TOF-MS | 25% mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-17 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 55 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-18 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine, Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 62 ±4 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-19 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=Homoarginine, Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 111 ±6 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 2 μg/mL M.luteus | |||
| 21185160 | 2011 | O-20 (Oncocin) | 19 | Free | Amidation | Linear | L | Agp = α-amino-3-guanidinopropionic acid | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 171 ±20 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC =8 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-21 (Oncocin) | 19 | Free | Amidation | Linear | L | Har=homoarginine, Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 75 ±1 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-22 (Oncocin) | 19 | Free | Amidation | Linear | L | Agp = α-amino-3-guanidinopropionic acid, Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 103 ±5 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 4 μg/mL M.luteus | |||
| 21185160 | 2011 | O-23(Oncocin) | 19 | Free | Amidation | Linear | L | Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 176 ±8 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 8 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 21185160 | 2011 | O-24 (Oncocin) | 19 | Free | Amidation | Linear | Mix | D-Arg at 19th position | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | >480(79.6 ±0.2%) | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 | |||
| 21185160 | 2011 | O-25 (Oncocin) | 19 | Free | Propylamidation | Linear | L | Orn=Ornithine | 2kDa Oncopeltus peptide derivatives | Antimicrobial | 30-480 Minutes | 7.5 μg/100μl | 102 ±2 | Mouse serum proteases | MALDI-TOF-MS | Full mouse serum | in vivo | None | None | MIC = 4 μg/mL in E.coli BL21A1 and 8 μg/mL M.luteus | |||
| 22186872 | 2011 | Angiotensin I | 10 | Free | Free | Linear | L | None | Derived from angiotensinogen | Precursor of angiotensin-II | Room Temperature | 1mg/mL | 1 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Bradykinin | 9 | Free | Free | Linear | L | None | Endogenous peptide of kinin family | Vasodilator, Inflammatory mediator | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | β-Endorphin | 31 | Free | Free | Linear | L | None | Endogenous opioid neuropeptide in neurons of both the central and peripheral nervous system. | Agonist of the opioid receptors | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | [Leu5]Enkephalin | 5 | Free | Free | Linear | L | None | Endogenous opioid neuropeptide in neurons of both the central and peripheral nervous system. | Neurotransmitter | Room Temperature | 1mg/mL | <5 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Substance P | 11 | Free | Amidation | Linear | L | None | Member of the tachykinin neuropeptide family. | Neurotransmitter | Room Temperature | 1mg/mL | 10 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Oxytocin | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Hypothalamus | Cause contraction of the uterus during labor and intiate milk release from breast | Room Temperature | 1mg/mL | 1 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Somatostatin | 14 | Free | Free | Cyclic (C3-C14) | L | None | Neuropeptide secreted by Hypothalamus | Inhibits insulin and glucagon secretion. | Room Temperature | 1mg/mL | 10 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22186872 | 2011 | Vasopressin | 9 | Free | Amidation | Cyclic (C1-C6) | L | None | Anti-diuretic hormone secreted by pitutiary gland | Anti-diuretic and regulates retention of water | Room Temperature | 1mg/mL | >7 | Hydolytic activity of bacterial strain B-9 | HPLC and LC/ITMS | Bacterial strain B-9 cell culture | in vitro | None | None | Not reported | |||
| 22263969 | 2012 | ANP-Fc (Atrial natriuretic peptide- Fc) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation. | Natriuretic and vasodilator | 4-72 hours | 0.5mg/kg of protein | 2 to 5 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 22263969 | 2012 | 2m (monomer Atrial natriuretic peptide- Fc ) | 39 | Free | Fc region | Cyclic (C7-C23 & C-residues of Fc region) | L | None | Synthetic ANP peptides linked to the N-terminus of recombinantly expressed Fc using native chemical ligation. | Natriuretic and vasodilator | 4-72 hours | 0.5mg/kg of protein | 3.9 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 22263969 | 2012 | 3m (monomer Atrial natriuretic peptide- Fc ) | 42 | 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 | 4.5 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 22263969 | 2012 | 2d (Atrial natriuretic peptide- Fc dimer) | 78 | 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 | 2.8 | Rat plasma proteases | ELISA | Female Wistar rats Plasma | in vivo | None | None | Not reported | |||
| 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 | |||
| 23318502 | 2013 | GLP-1(7 €“36)NH2 [Glucagon-like peptide-1] | 30 | Free | Amidation | Linear | L | None | GLP-1 | Regulate blood glucose | Blood sample collected after 32-60 minutes after the infusion of peptide | 20pmol/kg | 4.8 ±0.8 | Pig kidneys proteases | Radioactivity measurement | Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | Ex-4 (Exendin-4) | 39 | Free | Free | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | Blood sample collected after 50-130 minutes after the infusion of peptide | 10 pmol/kg | 32.8 ±4.1 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | Ex(1 €“30) or Exendin(1 €“30) | 30 | Free | Free | Linear | L | None | Synthetic derived from Exendin 4 | GLP-1 receptor agonist | Blood sample collected after 42-130 minutes after the infusion of peptide | 20 pmol/kg | 28.4 ±1.7 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23318502 | 2013 | GLP-1Arg34(7 €“36), Ex(31 €“39) or [GLP-Ex] | 39 | Free | Free | Linear | L | None | Synthetic | GLP-1 receptor agonist | Blood sample collected after 42-130 minutes after the infusion of peptide | 20 pmol/kg | 19.5 ±3.3 | Pig kidneys proteases | Radioactivity measurement | (Bolus injection)Pig kidney | in vivo | None | None | Not reported | |||
| 23813302 | 2013 | TRV027 | 8 | Sar=Sarcosine | Free | Linear | Mix | D-Ala at 8th position | Synthetic β-arrestin-biased agonist | Beta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitment | Not mentioned | 0.01 - 20 μg/kg/min dose | <2 (intial half life) | Human plasma proteases | LC/MS/MS | Human plasma | in vivo | None | None | Not reported | |||
| 23813302 | 2013 | TRV027 | 8 | Sar=Sarcosine | Free | Linear | Mix | D-Ala at 8th position | Synthetic β-arrestin-biased agonist | Beta €arrestin €biased AT1R(Angiotensin type 1 Receptor) ligand, antagonize G-protein signaling & stimulates beta-arrestin recruitment | Not mentioned | 0.01 - 20 μg/kg/min dose | ~ 10 (Terminal half life) | Human plasma proteases | LC/MS/MS | Human plasma | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 5-120 minutes | 10mg/ml | >240 | Serum and plasma proteases | LC-MS | Male beagle dog plasma | in vitro | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 4 hours at 37C | 1 µM | >110 | Dog hepatocyte proteases | LC-MS | Male beagle dog hepatocyte | in vitro | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 2-120 minutes | 20μg/Kg | 0.05 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(9-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 3-120 minutes | 50μg/Kg | 0.54 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 24588343 | 2014 | GLP-1(7-36)(Glucagon Like protein-1) | 28 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 4-120 minutes | 50μg/Kg | 2.1 | Dog hepatocyte proteases | LC-MS | Male beagle dog plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 25025626 | 2014 | Vasotab TY | 76 | Free | Free | Linear | L | None | Salivary glands of the horsefly ofTabanus yao | Vasodialator and anti-thrombic | 1-480 minutes | 5mg/kg | >1 | Mouse plasma proteases | ELISA | Kunming Mouse plasma (Dose i/v injected) | in vivo | None | None | At the dosages of 5,10, and 20 nmol/kg, vasotab TY inhibited thrombus formation by47.2, 72.2, and 86.1%, respectively. | |||
| 25025626 | 2014 | Vasotab TY | 76 | Free | Free | Linear | L | None | Salivary glands of the horsefly ofTabanus yao | Vasodialator and anti-thrombic | 1-480 minutes | 5mg/kg | 50 | Mouse lungs proteases | ELISA | Kunming Mouse lungs (Dose i/v injected) | in vivo | None | None | At the dosages of 5,10, and 20 nmol/kg, vasotab TY inhibited thrombus formation by47.2, 72.2, and 86.1%, respectively. | |||
| 25039358 | 2014 | Gly8-GLP-1(7-36)(Glucagon Like protein-1) | 30 | Free | Amidation | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Vasodialator | 37 °C for 2-72 hours | 1000ng/ml | 0.6 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 8.3 ± 0.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 4.8 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =1.6 ± 0.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist, Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 17.1 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 6 | 30 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 15 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 18.1 ± 0.9 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 7 | 30 | Free | Amidation | Linear | L | X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 52.2 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 18.6 ± 1.3 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 8 | 30 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 12.9 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 7.1 ± 0.9 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 9 | 30 | Free | Amidation | Linear | L | X-2 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 21.6 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 8.1 ± 0.6 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 10 | 30 | Free | Amidation | Linear | L | X-1 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 11.8 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 =12.1 ± 0.5 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 11 | 30 | Free | Amidation | Linear | L | X-2 = Lys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 20.3 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 19.9 ± 1.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 12 | 31 | Free | Amidation | Linear | L | X-1 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 5.4 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 11.3 ± 0.6 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 13 | 31 | Free | Amidation | Linear | L | X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 18.4 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vitro | None | None | GLP-1 receptor Activation potency with EC50 = 16.8 ± 0.7 pM in HEK-293 cells | |||
| 25039358 | 2014 | Exendin-4 | 39 | Free | Amidation | Linear | L | None | Derived from Saliva of Gila monster | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 2.5 ±1.2 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 =1.6 ± 0.4 pM in HEK-293 cells | |||
| 25039358 | 2014 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist | 37 °C for 2-72 hours | 1000ng/ml | 14 .9 ±0.9 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 =9.5 ± 0.8 pM in HEK-293 cells | |||
| 25039358 | 2014 | Coumarin-modified GLP-1 derivative 7 | 30 | Free | Amidation | Linear | L | X-2 = Cys- conjugated-7-hydroxyCoumarin maleimide | Analog of human GLP-1 | Hypoglycaemic | 37 °C for 2-72 hours | 1000ng/ml | 22 .9 ±7.2 | Rat plasma proteases | LC-MS/MS | Rat Plasma | in vivo | None | None | GLP-1 receptor Activation potency with EC50 = 18.6 ± 1.3 pM in HEK-293 cells | |||
| 25243635 | 2014 | VGLP1 (Glucagon like peptide 1 derivative) | 31 | Free | Free | Cyclic (C18-C26) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | <5 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | VGLP1K3 (Glucagon like peptide 1 derivative) | 34 | Free | Free | Cyclic (C18-C26) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | <80 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | VGLP1K6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | ~ 70 | DPP IV | ELISA | DPP IV | in vitro | None | None | The insulin levels were increased dramatically to 906.53b ± 22.18pmol/L within 60 min after GLP-1 administration | |||
| 25243635 | 2014 | VGLP1S6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | ~ 7.5 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | VGLP1V6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 37 °C for 0.1-24 hours | 500μg | ~ 5 | DPP IV | ELISA | DPP IV | in vitro | None | None | Not reported | |||
| 25243635 | 2014 | GLP-1(Glucagon Like protein-1) | 31 | Free | Free | Linear | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 5-90 hours | 500μg | <2 | DPP IV | ELISA | DPP IV | in vitro | None | None | The insulin levels were increased dramatically to 806.74 ± 30.60 pmol/L within 15 min after GLP-1 administration | |||
| 25243635 | 2014 | VGLP1K6 (Glucagon like peptide 1 derivative) | 37 | Free | Free | Cyclic (C12-C20) | L | None | Glucagon Like protein-1 (GLP-1) | Antihyperglycemic | 5-90 hours | 300μg/Kg body weight of rats | ~ 70 | Rat serum proteases | ELISA | Subcutaneously injected in Sprague ˆ’Dawley (SD) rats | in vivo | None | None | The insulin levels were increased dramatically to 906.53b ± 22.18pmol/L within 60 min after GLP-1 administration | |||
| 25324697 | 2014 | SHSMP(Sadat-Habdan Mesenchymal stimulating Peptide) | 13 | Free | Free | Linear | L | None | SHSMP(Sadat-Habdan Mesenchymal stimulating Peptide) | Angiogenesis Factor | Blood sample collected after 30-480 minutes after the infusion of peptide | 5mg/kg | 90 | Rat plasma proteases | HPLC | Sprague Dawley rats (Dose i/m injected) | in vivo | Patent US7399826 B1 | None | Not reported | |||
| 25894376 | 2015 | P32 (Fibroblast growth factor 2- binding peptide derivative) | 11 | Free | Amidation | Linear | Mix | None | Fibroblast growth factor 2- binding peptide derivative | Anti-proliferative | 37 °C for 1-48hours | 0.3478μM | 12 | Human plasma proteases | HPLC | Human plasma | in vitro | None | None | P32 significantly inhibited the proliferation of SGC-7901, MGC-803, and KATOIII cells induced with 20ng/ml of FGF2, and the IC50 values of P32 were 0.77, 1.69, and 1.09 μmol/L, respectively | |||
| 25894376 | 2015 | P7 (Basic fibroblast growth factor- binding peptide) | 7 | Free | Free | Linear | L | None | Basic Fibroblast growth factor 2- binding peptide | Anti-proliferative and anti-angiogenic | 37 °C for 1-48hours | 0.3478μM | 1.5 | Human plasma proteases | HPLC | Human plasma | in vitro | 20414975 | None | Not reported | |||
| 25594223 | 2015 | ENF(Enfuvirtide) | 36 | Acetylation | Amidation | Linear | L | None | Enfuvirtide | Anti-viral (Anti-HIV activity) | 0.5-24 hours | 1.7μM/Kg | 1.5 | Rat plasma proteases | HPLC | Sprague-Dawey (SD) rats Plasma | in vivo | None | None | EC50 = 3nM for Anti-viral potency | |||
| 25594223 | 2015 | SL-ENF(Sialic acid Enfuvirtide) | 37 | Sialic acid | Amidation | Linear | L | None | Synthetic derived from glycosylated ENFs | Anti-viral | 0.5-24 hours | 1.7μM/Kg | 23.1 | Rat plasma proteases | HPLC | Sprague-Dawey (SD) rats Plasma | in vivo | None | None | EC50 = 2nM for Anti-viral potency | |||
| 25594223 | 2015 | Lac-ENF (Lactic acid Enfuvirtide) | 37 | Lactic acid | Amidation | Linear | L | None | Synthetic derived from glycosylated ENFs | Anti-viral | 0.5-24 hours | 1.7μM/Kg | 4.2 | Rat plasma proteases | HPLC | Sprague-Dawey (SD) rats Plasma | in vivo | None | None | EC50 = 2nM for Anti-viral potency | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 37 C, 48 Hours | 10 µM | 4.18 | Fxa(Facor Xa) and DPP-IV | HPLC-ESI/MS/MS | Protein Sample +HAS + Fxa +DPP IV | in vitro | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | ~ 5 | db/db mice plasma proteases | LC-MS/MS | db/db Mice plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | BAY55-9837 (VPAC2 receptor agonist) | 31 | Free | Free | Linear | L | None | Pituitary adenylate cyclase-activating peptides (PACAPs) derived peptide | Insulin secretion stimulant | 0.5-24 hours | 0.5 mg/kg | ~ 5 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in BAY55-9837-treated mice (20nmol/kg) is 0.79 fold higher than control | |||
| 25771000 | 2015 | 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 | |||
| 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 | 16.31 | Fxa(Facor Xa) | HPLC-ESI/MS/MS | Peptide sample + HAS | 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 | |||
| 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 | 0.5-24 hours | 0.5 mg/kg | 16.72 | Fxa(Facor Xa) and DPP-IV | LC-MS/MS | Peptide sample + HSA +Fxa + DPP IV(Dose i/v injected) | 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 | |||
| 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 | 0.5-24 hours | 0.5 mg/kg | 12.19 | db/db mice plasma proteases | LC-MS/MS | (Dose i/v injected)Mice plasma | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control | |||
| 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 | 0.5-24 hours | 0.5 mg/kg | >12 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in MHDBAY-treated mice (20nmol/kg) is 2.26 fold higher than control | |||
| 25771000 | 2015 | Exendin-4 | 39 | Free | Free | Linear | L | None | GLP-1 derived peptide | Regulate blood glucose | 0.5-24 hours | 0.5 mg/kg | 3.03 | db/db mice plasma proteases | LC-MS/MS | db/db Mice plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in Exendin-4 -treated mice (20nmol/kg) is 1.62 fold higher than control | |||
| 25771000 | 2015 | Exendin-4 | 39 | Free | Free | Linear | L | None | GLP-1 derived peptide | Regulate blood glucose | 0.5-24 hours | 0.5 mg/kg | >3 | Rabbit plasma proteases | LC-MS/MS | New Zealand White Rabbit plasma (Dose i/v injected) | in vivo | None | None | AUC for glucose -stimulated 1st phase insulin secretion in Exendin-4 -treated mice (20nmol/kg) is 1.62 fold higher than control | |||
| 25900863 | 2015 | TRI-1144 | 38 | Acetylation | Amidation | Linear | L | None | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 4.2 | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG-TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with PEG(40KDa) thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 34 | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG-TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with PEG(40KDa) thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Not mentioned | Not mentioned | 70 | Human plasma proteases | LC-MS/MS | Human Plasma | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG40kDa[ClPhSO2]TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with ClPhSO2 conjugate thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Not mentioned | Not mentioned | 150 (t1/2β) | Human plasma proteases | LC-MS/MS | Human Plasma | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG40kDa[ClPhSO2]TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with ClPhSO2 conjugate thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 150 (t1/2 linker cleavage) | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 25900863 | 2015 | PEG40kDa[MorphSO2]TRI-1144 | 38 | Acetylation | Amidation | Linear | L | Conjugated with MorphSO2 conjugate thro µgh Lys-30 | Synthetic derived from SPPS with an acetylated N-terminus and amidated C-terminus. | HIV-fusion inhibitor | Blood sample collected after 1-168 hours after the infusion of peptide | 800nmol/Kg dose injected | 44 (t1/2β of releasable PEG-TRI-1144 conjugate) | Rat plasma proteases | LC-MS/MS | Intravenously administered to Sprague €“Dawley rats | in vivo | None | None | Not reported | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 3.4 ±0.2 | Pig blood proteases | Radioimmunoassay and HPLC | Female pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 10.8 ±0.8 | Pig blood proteases | Radioimmunoassay and HPLC | Female pigs blood + Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotinin | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 6.2 ±0.2 | Pig plasma proteases | Radioimmunoassay and HPLC | Female pigs plasma+ Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | Porcine-PYY(1-36) | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | 37 °C for 24 hours | Not mentioned | 11.9 ±0.7 | Pig plasma proteases | Radioimmunoassay and HPLC | Female pigs plasma+ Peptide sample+ DPP-IV inhibitor (valine pyrrolidide) + aprotinin | in vitro | None | None | Human PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.5nmol/L | |||
| 26197931 | 2015 | PYY(3-34) [Peptide YY] | 34 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Blood sample collected after 15minutes of the infusion of peptide | 100 pmol/kg | 3.6 ±0.5 | Pig blood proteases | Radioimmunoassay | Female pigs blood | in vivo | None | None | Porcine PYY 3 €“36 signaled through the Y-2 receptor in COS-7 cells with potency with EC50 = 3.9nmol/L | |||
| 26197931 | 2015 | PYY(1-36) [Peptide YY] | 36 | Free | Free | Linear | L | None | Synthetic peptide hormone released from enteroendocrine cells | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Blood sample collected after 15minutes of the infusion of peptide | 100 pmol/kg | 7.3 ±0.8 | Pig blood proteases | Radioimmunoassay | Female pigs blood | in vivo | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 13 ±0.7 | Human plasma proteases + DPP IV | MS | Human Plasma+ Heparin | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 4 ±0.2 | Human plasma proteases + DPP IV | MS | Citrate + Human plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 4 ±0.2 | Human serum proteases + DPP IV | MS | Serum | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp and on Ice | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P700 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp and on Ice | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P800 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | Apr-24 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 12 ±3 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 2 ±0.4 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | Apr-14 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 10 ±0.5 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G36A or [GLP-1(7-36A)] | 30 | Free | Amidation | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 37-96 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 04 to 18 | Human plasma proteases + DPP IV | MS, ELISA | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P700 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS, ELISA | P800 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 1 ±0.3 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 5 ±1.0 | Human blood proteases + DPP IV | MS | EDTA whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | 12 ±1.0 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | G 37 or [GLP-1(7 €“37)] | 31 | Free | Free | Linear | L | None | Glucagon-like peptide 1 (GLP-1) | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | On ice | 0.4 µM | 41 ±5.0 | Human blood proteases + DPP IV | MS | P800 whole blood | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | GIP (1-42) (Glucosedependent insulinotropic polypeptide) | 42 | Free | Free | Linear | L | None | Proprotein of gastrointestinal tract | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | May-20 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | GIP (1-42) (Glucosedependent insulinotropic polypeptide) | 42 | Free | Free | Linear | L | None | Proprotein of gastrointestinal tract | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | May-20 | Human serum proteases + DPP IV | MS | Serum | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | GIP (1-42) (Glucosedependent insulinotropic polypeptide) | 42 | Free | Free | Linear | L | None | Proprotein of gastrointestinal tract | Antihyperglycemic or incretin effect(Stimulate Insulin release in glucose dependent manner) | Room Temp | 0.4 µM | >96 | Human plasma proteases + DPP IV | MS | P800 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | OXM(1-37) (Oxyntomodulin) | 37 | Free | Free | Linear | L | None | Peptide Hormone of colon | Anti-apetizer | Room Temp | 0.4 µM | <24 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | OXM(1-37) (Oxyntomodulin) | 37 | Free | Free | Linear | L | None | Peptide Hormone of colon | Anti-apetizer | Room Temp | 0.4 µM | >72 | Human plasma proteases + DPP IV | MS | P800 plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | Glucagon | 29 | Free | Free | Linear | L | None | Peptide hormone of pancrease | Regulates hypoglycemia | Room Temp | 0.4 µM | May-20 | Human plasma proteases + DPP IV | MS | EDTA plasma | in vitro | None | None | Not reported | |||
| 26222180 | 2015 | Glucagon | 29 | Free | Free | Linear | L | None | Peptide hormone of pancrease | Regulates hypoglycemia | Room Temp | 0.4 µM | 45 | Human plasma proteases + DPP IV | MS | P800 plasma | in vitro | None | None | Not reported | |||
| 26308095 | 2015 | Exenatide | 39 | Free | Amidation | Linear | L | None | Saliva of Gila monster | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after7-288 hours after the injection of peptide | 5nmol/Kg | 02-Mar | Proteases from mini-pig plasma | ELISA, LC/MS | Mini-pigs plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | Exenatide | 39 | Free | Amidation | Linear | L | None | Saliva of Gila monster | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 30 | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | Acylation of peptide at K-26 with C-18(palmitic acid) fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Upregulates intracellular cAMP resulting in the release of insulin | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 8-10 hours | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | Acylation of peptide at K-26 with C-18(palmitic acid) fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Upregulates intracellular cAMP resulting in the release of insulin | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 14.4 hours | Rat plasma proteases | ELISA, LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Not reported | |||
| 26308095 | 2015 | semaglutide | 36 | Free | Amidation | Linear | L | Alpha-aminoisobutyric acid at 8th position, Acylation of peptide at K-26 with C-18 fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after7-288 hours after the injection of peptide | 1 -2 nmol/Kg | 165 | Human plasma proteases | ELISA, LC/MS | Human plasma (Dose s/c injected) | in vivo | 25475122 | None | Semaglutide was the most potent with an ED50 of < 2 nmol/kg | |||
| 26308095 | 2015 | semaglutide | 36 | Free | Amidation | Linear | L | Acylation of peptide at K-26 with C-18 fatty di-acid chain | Glucagon-like peptide 1 (GLP-1) analogue | Regulates blood glucose by upregulating the insulin secretion | Blood sample collected after 1-96 hours after the injection of peptide | 5nmol/Kg | 46 | Mini-pig plasma proteases | ELISA, LC/MS | Mini-pigs plasma (Dose s/c injected) | in vivo | 25475122 | None | Semaglutide was the most potent with an ED50 of < 2 nmol/kg | |||
| 26325323 | 2015 | Endogenous LHRH | 10 | Free | Amidation | Linear | L | Pyro-Glutamate at 1st position | Hypothalamus | Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH) | Blood sample collected after0.5-24 hours after the injection of peptide | 2.5mg/Kg | 4-8min | Human plasma proteases | LC/MS | Human plasma (Dose s/c injected) | in vivo | None | None | Not reported | |||
| 26325323 | 2015 | Compound 1(lactose [Q1][w6]LHRH ) | 10 | Lactose | Amidation | Linear | L | Lactose at N-ter, pyro-Glutamine at n-ter, D-Trp at 6 pos | Hypothalamus | Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH) | Blood sample collected after0.5-24 hours after the injection of peptide | 2.5mg/Kg | 2.9 ±0.63 | Rat plasma proteases | LC/MS | Rat Plasma (Dose i/v injected) | in vivo | None | None | Increase in the level of LH was observed i.e. nAUC = 11.33 ± 1.65 ng/24 hafter oral administration of 20 mg/kg of compound 1 compared to the control nAUC = 4.45 ± 1.028 ng/24 h | |||
| 26325323 | 2015 | Compound 1(lactose [Q1][w6]LHRH ) | 10 | Lactose | Amidation | Linear | L | Lactose at N-ter, pyro-Glutamine at n-ter, D-Trp at 6 pos | Hypothalamus | Stimulates pitutiary gland to secretes to release gonadotropins(LH, FSH) | Blood sample collected after0.5-24 hours after the injection of peptide | 10mg/Kg | 2.6 ±0.84 | Rat plasma proteases | LC/MS | Rat Plasma (Dose i/p injected) | in vivo | None | None | Increase in the level of LH was observed i.e. nAUC = 11.33 ± 1.65 ng/24 hafter oral administration of 20 mg/kg of compound 1 compared to the control nAUC = 4.45 ± 1.028 ng/24 h | |||
| 26337231 | 2015 | P16 [TNF α (75 €“94)] | 20 | Free | Free | Linear | L | None | Tumor necrosis factor-derived (TNF) | Tumor growth inhibitor and anti-angiogenic | Blood sample collected after0.5-24 hours after the injection of peptide | 5mg/kg | 0.096 ±0.008 | BALB/c mice plasma proteases | LC/MS | BALB/c mice plasma (Dose i/v injected) | in vivo | None | None | Growth inhibition effect of RMP16 was observed in DU145 cells (IC50 = 17.20 ± 1.95 nM, Tumor inhibition rates of P16-treated mice was 21.81% | |||
| 26337231 | 2015 | RMP-16 (Recombinant slow-release TNF α-derived peptide) | 32 | Free | Free | Linear | L | None | Recombinant slow-release TNF α-derived peptide | Tumor growth inhibitor and anti-angiogenic | Blood sample collected after0.5-24 hours after the injection of peptide | 5mg/kg | 13.11 ±1.49 | BALB/c mice plasma proteases | LC/MS | BALB/c mice plasma (Dose i/v injected) | in vivo | None | None | Growth inhibition effect of RMP16 was observed in DU145 cells (IC50 = 17.20 ± 1.95 nM, the tumor inhibition rates of RMP16-treated mice was 78.11% | |||
| 26400022 | 2015 | Hirulog-1 | 20 | Free | Free | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 20-25 | Human plasma proteases | HPLC, MS-MS | Human plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 20.50 ± 0.62nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.77 ± 0.09nM | |||
| 26400022 | 2015 | Hirulog-1 | 20 | Free | Free | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 15 ±1.3 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 20.50 ± 0.62nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.77 ± 0.09nM | |||
| 26400022 | 2015 | Peptide 1 (Hirudin mimetic peptide) | 22 | Free | Amidation | Linear | Mix | None | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 13+-2.6 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 13.40 ± 0.46 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 5.80 ± 0.55nM | |||
| 26400022 | 2015 | Peptide S2 (Hirudin mimetic peptide) | 22 | Free | Amidation | Linear | Mix | Stearic acid at Lys | Hirudin derived | Anti-coagulant | Not mentioned | 1.0μM/Kg | 212.2 ±58.4 | Rat plasma proteases | HPLC, MS-MS | Sprague-Dawley (SD) rats plasma (Dose i/v injected) | in vivo | None | None | Inhibition constant for peptides (Ki, nM) in rat thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 15.24 ± 0.18 nM; Inhibition constant for peptides (Ki, nM) in human thrombin €“catalyzed hydrolysis of Chromozym TH with Ki 11.75 ± 0.46nM | |||
| 21459096 | 2011 | ANP (Atrial natriuretic peptide) | 28 | Free | Free | Cyclic (C7-C23) | L | None | Derived from parotid gland | Vasorelaxing | 37 °C for 0-125 minutes | Not mentioned | 1.3 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 21459096 | 2011 | BNP(B-type natriuretic peptide) | 32 | Free | Free | Cyclic (C10-C26) | L | None | Brain natriuretic peptide | Cardiac fibrosis Inhibitor | 37 °C for 0-125 minutes | Not mentioned | 8 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 21459096 | 2011 | CNP(C-type natriuretic peptide) | 22 | Free | Free | Cyclic (C6-C22) | L | None | Secreted from vascular endothelium | Vasodialator | 37 °C for 0-125 minutes | Not mentioned | 4.3 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | 19395584 | None | Not reported | |||
| 21459096 | 2011 | DNP (Dendroaspis natriuretic peptide) | 39 | Free | Free | Cyclic (C7-C23) | L | None | Dendroaspis natriuretic peptide | Natriuretic and hypotensive activities | 37 °C for 0-125 minutes | Not mentioned | 159 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | 19395584 | None | Not reported | |||
| 21459096 | 2011 | CD-NP (C-terminal tail of DNP) | 37 | Free | Free | Cyclic (C6-C22) | L | None | Chimeric peptide derived from CNP and DNP | Natriuretic and aldosterone suppressor | 37 °C for 0-125 minutes | Not mentioned | 17-22.9 | Human kidney proteases | Not mentioned | Human kidney membrane extract | in vitro | None | None | Not reported | |||
| 25625650 | 2015 | Liraglutide | 31 | Free | Free | Linear | L | γ-Glu-palmitoyl at 21 st position | Analog of human GLP-1 | GLP-1 receptor agonist | 0.25-84 hours | 0.6mg s/c injected | 12 ±2.8 | Cat blood proteases | ELISA | Healthy cat blood (Dose s/c injected) | in vivo | None | None | Insulin secretion increased 760.8 ± 350.7 (449 €“1,493) ng/L on Liraglutide administration as compared to normal 455.5 ±115.8 (411 €“660) in hyperglycemic patients | |||
| 21903490 | 2011 | cTP6( Cyclic thymic hexapeptide) | 6 | Free | Free | Cyclic (Amide bond between C1-Y6) | L | None | Synthetic analog of TP5(Thymopentin) | Immunomodulatory drug | Blood collected after 5 minutes-8 hours after peptide delivery | 100 µg/ml | 2.24 ±0.423 | Rhesus monkey plasma proteases | LC-MS | Rhesus monkey plasma | in vivo | None | None | Not reported | |||
| 21903490 | 2011 | cTP6( Cyclic thymic hexapeptide) | 6 | Free | Free | Cyclic (Amide bond between C1-Y6) | L | None | Synthetic analog of TP5(Thymopentin) | Immunomodulatory drug | Blood collected after 5 minutes-8 hours after peptide delivery | 200 µg/ml | 2.95 ±0.157 | Rhesus monkey plasma proteases | LC-MS | Rhesus monkey plasma | in vivo | None | None | Not reported | |||
| 21903490 | 2011 | cTP6( Cyclic thymic hexapeptide) | 6 | Free | Free | Cyclic (Amide bond between C1-Y6) | L | None | Synthetic analog of TP5(Thymopentin) | Immunomodulatory drug | Blood collected after 5 minutes-8 hours after peptide delivery | 300 µg/ml | 2.56 ±0.27 | Rhesus monkey plasma proteases | LC-MS | Rhesus monkey plasma | in vivo | None | None | Not reported | |||
| 21903490 | 2011 | TP5(Thymopentin) | 5 | Free | Free | Linear | L | None | Thymopentin | Immunomodulatory drug | Not mentioned | Not mentioned | 30 | Human plasma proteases | Not mentioned | Human plasma | 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 | |||
| 24139844 | 2013 | Conjuagte 2(conjugates of 4-aminocyclophosphamide (4-NH2-CPA)) | 6 | Succinylation | Amidated CPA | Linear | L | None | Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA) | Anti-cancer | Not mentioned | Not mentioned | 12 | PSA(Prostate-specific antigen ) | HPLC | Conjuagte 2+PSA(Prostate-specific antigen) | in vitro | None | None | pEC50-8.59 ±0.9minutes, Emax 9.30 ±0.26nmol/well | |||
| 24139844 | 2013 | Conjuagte 3(conjugates of 4-aminocyclophosphamide (4-NH2-CPA)) | 5 | Bn-glutarylation | Amidated CPA | Linear | L | None | Synthetic peptide derived from conjugates of 4-aminocyclophosphamide (4-NH2-CPA) | Anti-cancer | Not mentioned | Not mentioned | 55 | PSA(Prostate-specific antigen ) | HPLC | Conjuagte 3+PSA(Prostate-specific antigen) | in vitro | None | None | pEC50-8.19 ±1.0minutes, Emax 9.44 ±0.3 nmol/well | |||
| 24874704 | 2014 | AM(adrenomedullin) | 52 | Free | Amidation | Cyclic (Ringed structure formed by C16-C21) | L | None | Isolated from Human pheochromocytoma | Vasodilator and cardiovascular protection | Not mentioned | 3nmol/kg Dose | 0.62 ±0.02 (1st plasma half life) | Rat plasma proteases | ELISA | Male Wistar rats plasma | in vivo | http://www.genscript.com/peptide/RP11288-Adrenomed | None | Native human AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.59 ± 0.90 and9.30 ± 0.26 nmol/well | |||
| 24874704 | 2014 | AM(adrenomedullin) | 52 | Free | Amidation | Cyclic (Ringed structure formed by C16-C21) | L | None | Isolated from Human pheochromocytoma | Vasodilator and cardiovascular protection | Not mentioned | 3nmol/kg Dose | 15.2 ±1.9 min (2nd plasma half life) | Rat plasma proteases | ELISA | Male Wistar rats plasma | in vivo | http://www.genscript.com/peptide/RP11288-Adrenomed | None | Native human AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.59 ± 0.90 and9.30 ± 0.26 nmol/well | |||
| 24874704 | 2014 | PEGylated AM | 52 | Pegylation | Amidation | Cyclic (Ringed structure formed by C16-C21) | L | None | Isolated from Human pheochromocytoma | Vasodilator and cardiovascular protection | Not mentioned | 3nmol/kg Dose | 4.87 ±0.68(1st plasma half life) | Rat plasma proteases | ELISA | Male Wistar rats plasma | in vivo | http://www.genscript.com/peptide/RP11288-Adrenomed | None | PEGylated AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.519 ± 0.10 and9.44 ± 0.30 nmol/well | |||
| 24874704 | 2014 | PEGylated AM | 52 | Pegylation | Amidation | Cyclic (Ringed structure formed by C16-C21) | L | None | Isolated from Human pheochromocytoma | Vasodilator and cardiovascular protection | Not mentioned | 3nmol/kg Dose | 108 ±12 min (2nd plasma half life) | Rat plasma proteases | ELISA | Male Wistar rats plasma | in vivo | http://www.genscript.com/peptide/RP11288-Adrenomed | None | PEGylated AM peptide elevated intracellular cAMP levels in a dose-dependent manner with pEC50 and Emax values of 8.519 ± 0.10 and9.44 ± 0.30 nmol/well | |||
| 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 | 2 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum(Subcutaneous 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 sterile phosphate buffered saline(PBS, pH 7.2) at a concentration of 0.1 mg | 4.5 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intraperitoneal 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 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 | 28.9 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Oral 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 | |||
| 25453979 | 2014 | (D-Leu-4)OB3 | 7 | Free | 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 | 34 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum(Subcutaneous 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 | (D-Leu-4)OB3 | 7 | Free | 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 | 49 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intraperitoneal 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 | (D-Leu-4)OB3 | 7 | Free | 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 | 36 | 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 | (D-Leu-4)OB3 | 7 | Free | 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 | 20 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Oral 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 | (D-Leu-4)OB3 | 7 | Free | 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 | 41 | Mice serum proteases | Competitive ELISA | Male Swiss Webster mice serum (Intranasal route of delivery) | in vivo | None | None | Stimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS | |||
| 24462899 | 2014 | APTEDB-DTX (Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate) | 27 | Free | Free | Linear | L | Modified Gly at 16th postion i.e. propargylglycine and peptide conjugated with drug DTX at this position | Fibronectin extra domain B (EDB)-specific aptide docetaxel conjugate | Drug(anticancer agent i.e. DTX) Delivery vehicle | Not mentioned | 5 mg DTX/kg Dose | 0.491 | Mice serum proteases | HPLC | C57BL6 mice Serum | in vivo | None | None | Stimulates TLR3 signaling and Inhibits TLR4 signaling by seqsteting LPS | |||
| 5092290 | 2014 | LL-37 (Antimicrobial Peptide) | 37 | Free | Free | Linear | L | None | Human epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein) | Antimicrobial | 15-720 minutes hour | 3 µM | ~1 | Cathepsin | Proteolysis assay, (confirmed by Western blotting) | Western Blotting | in vitro | 16716248 | None | Not reported | |||
| 5092290 | 2014 | LL-37 (Antimicrobial Peptide) | 37 | Free | Free | Linear | L | None | Human epithelial cells(proteolytic cleavage of c-ter portion of hCAP-18 protein) | Antimicrobial | 15-720 minutes hour | 3 µM | >12 | Cathepsin | Proteolysis assay, (confirmed by Western blotting) | Western Blotting | in vitro | 16716248 | None | Not reported | |||
| 26308095 | 2015 | Semaglutide | 31 | Free | Free | Linear | L | Aib =2-Aminoisobutyric acid; Acylation of peptide at K-26 with fatty acid side chain i.e. N6-[N-(17-carboxy-1-oxoheptadecyl-L-c-glutamyl[2- (2-aminoethoxy)ethoxy]acetyl[2-(2 aminoethoxy)ethoxy]acetyl | GLP-1 (Glucagon like peptide-1) analogue | Regulate blood glucose level | Blood samples collected upto 96 hous | 1 -2 nmol/Kg | 165 | Proteases from Human plasma | ELISA, LC/MS | (Dose s/c injected)Human plasma | in vivo | 23743288 | None | Semaglutide was the most potent to lower blood glucose with an ED50 of < 2 nmol/kg | |||
| 26308095 | 2015 | Semaglutide | 31 | Free | Free | Linear | L | Aib =2-Aminoisobutyric acid; Acylation of peptide at K-26 with fatty acid side chain i.e. N6-[N-(17-carboxy-1-oxoheptadecyl-L-c-glutamyl[2- (2-aminoethoxy)ethoxy]acetyl[2-(2 aminoethoxy)ethoxy]acetyl | GLP-1 (Glucagon like peptide-1) analogue | Regulate blood glucose level | Blood samples collected upto 96 hous | 5nmol/Kg | 46 | Proteases from mini-pig plasma | ELISA, LC/MS | (Dose i/v injected)Mini-pigs plasma | in vivo | 23743288 | None | Semaglutide was the most potent to lower blood glucose with an ED50 of < 2 nmol/kg | |||
| 24361089 | 2014 | Teriparatide | 34 | Free | Free | Linear | L | None | Parathyroid Hormone derivative | Increase the concentration of ionic calcium (Ca2+) in the blood | Not mentioned | Not available | 5 (Elimination half life) | Proteases from human plasma(Severe renal impairment patients) | Not mentioned | Human plasma (Severe renal impairment patients) | in vivo | None | None | Not reported | |||
| 24361089 | 2014 | Teriparatide | 34 | Free | Free | Linear | L | None | Parathyroid Hormone derivative | Increase the concentration of ionic calcium (Ca2+) in the blood | Not mentioned | Not available | 1.5 (Elimination half life) | Proteases from human plasma(Normal) | Not mentioned | Human plasma (Normal) | in vivo | None | None | Not reported | |||
| 21210710 | 2011 | Linear chlorotoxin(CTX) | 36 | Free | Free | Linear | L | N-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 27 | Scorpion venom | Identify tumor foci with high sensitivity | 24 hours | 50μl of 40μM | 14 | Mice serum proteases | Imaging system to measure fluorescent intensity | Intravenous injection in two month old wild-type C57BL/6 mice | in vivo | http://www.drugbank.ca/drugs/DB00140 | None | Fluorescent efficiency (cm2) in the tumor compared with control mice=2.49 ±1 | |||
| 21210710 | 2011 | Cyclic chlorotoxin(CTX) | 43 | Free | Free | Cyclic (C2-C19, C5-C28, C16-C33, C20-C35) | L | N-hydroxysuccinimide ester(NHS-ester)modified Cy5.5 at Lysine 15,23 and 28 | Analog of CTX | Identify tumor foci with high sensitivity | 24 hours | 50μl of 40μM | 11 | Mice serum proteases | Imaging system to measure fluorescent intensity | Intravenous injection in two month old wild-type C57BL/6 mice | in vivo | http://www.drugbank.ca/drugs/DB00141 | None | Fluorescent efficiency (cm2) in the tumor compared with control mice=3.3 ±1.81 | |||
| 21986100 | 2011 | DALCE [(D-Ala2, Leu5, Cys6)-enkephalin] | 6 | Free | Free | Linear | Mix | None | Enkephalin derative | Treatment of ischemia | Not mentioned | 1mg/Kg | 9.1 ±2.4 | Rats plasma proteases | LC-MS | Intravenous injection in male Sprague €“Dawley rats | in vivo | http://www.drugbank.ca/drugs/DB00142 | None | Not mentioned | |||
| 21986100 | 2011 | DADLE [(D-Ala2, Leu5)-enkephalin] | 5 | Free | Free | Linear | Mix | None | Opoid peptide | Neuromodulator | Not mentioned | 1mg/Kg(200-250μl) | 4.6 | Rats plasma proteases | HPLC with tandem LC/MS/MS | Rat plasma | in vivo | http://www.drugbank.ca/drugs/DB00143 | None | Not mentioned | |||
| 21986100 | 2011 | CMD-Cys-DALCE | 6 | Free | Thiolated carboxymethyl dextran(CMD) cysteine conjugated via disulfide bond | Linear | Mix | None | Enkephalin derative | Treatment of ischemia | Not mentioned | 4.5 mg/kg corresponding to 1 mg/kg of DALCE | 56 ±6.0 | Rats plasma proteases | LC-MS | Intravenous injection in male Sprague €“Dawley rats | in vivo | http://www.drugbank.ca/drugs/DB00144 | None | Not mentioned | |||
| 22770564 | 2012 | HR2 (wild type) [HR2 regions of the HIV-1 envelope glycoprotein gp41] | 41 | Free | Free | Linear | L | None | HR2 regions of the HIV-1 envelope glycoprotein gp41 | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 37.2 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00145 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=1.5 ± 0.1nM | |||
| 22770564 | 2012 | N-terminus of HR2 | 42 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.6 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00146 | None | Not mentioned | |||
| 22770564 | 2012 | N-terminus-PEG750 of HR2 | 42 | Pegylation-PEG750 | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 40 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00147 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=7.2 ± 0.7nM | |||
| 22770564 | 2012 | N-terminus-PEG2000 of HR2 | 42 | Pegylation-PEG2000 | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 79.3 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00148 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=11.2 ± 1.9nM | |||
| 22770564 | 2012 | R4C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 37.4 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00149 | None | Not mentioned | |||
| 22770564 | 2012 | R4C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 4th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 44.1 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00150 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.1 ± 1.1nM | |||
| 22770564 | 2012 | R4C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at 4th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 67.4 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00151 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=8.7 ± 1.3nM | |||
| 22770564 | 2012 | S11C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.9 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00152 | None | Not mentioned | |||
| 22770564 | 2012 | S11C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 11th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 50.2 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00153 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.4 ± 0.8nM | |||
| 22770564 | 2012 | S11C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at 11th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 91 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00154 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.9 ± 0.5nM | |||
| 22770564 | 2012 | S15C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 39.9 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00155 | None | Not mentioned | |||
| 22770564 | 2012 | S15C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 15th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 53.7 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00156 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.1 ± 1.0nM | |||
| 22770564 | 2012 | S15C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at 15th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 82.4 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00157 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.0 ± 0.5nM | |||
| 22770564 | 2012 | E18C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.4 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00158 | None | Not mentioned | |||
| 22770564 | 2012 | E18C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 18th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 50.3 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00159 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.5 ± 1.0nM | |||
| 22770564 | 2012 | E18C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at 18th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 81.3 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00160 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.9 ± 0.6nM | |||
| 22770564 | 2012 | N22C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.9 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00161 | None | Not mentioned | |||
| 22770564 | 2012 | N22C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 22nd position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 51.8 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00162 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=4.2 ± 0.9nM | |||
| 22770564 | 2012 | N22C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at22nd position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 80.7 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00163 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.1 ± 0.5nM | |||
| 22770564 | 2012 | Q29C derivative of HR2 | 41 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.6 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00164 | None | Not mentioned | |||
| 22770564 | 2012 | Q29C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 29th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 58.1 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00165 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.2 ± 0.8nM | |||
| 22770564 | 2012 | Q29C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at 29th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 84.1 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00166 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=5.5 ± 0.5nM | |||
| 22770564 | 2012 | C terminus derivative of HR2 | 42 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 39 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00167 | None | Not mentioned | |||
| 22770564 | 2012 | C terminus-PEG750 derivative of HR2 | 42 | Free | Free | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 81.2 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00168 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=10.9 ± 2.2nM | |||
| 22770564 | 2012 | C terminus-PEG2000 derivative of HR2 | 42 | Free | Pegylation (PEG750) | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 126 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00169 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)=43.3 ± 14.8nM | |||
| 22770564 | 2012 | S20C derivative of HR2 | 41 | Free | Pegylation (PEG2000) | Linear | L | None | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 38.6 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00170 | None | Not mentioned | |||
| 22770564 | 2012 | S20C-PEG750 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG750 of cysteine at 20th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 42 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00171 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)>400 | |||
| 22770564 | 2012 | S20C-PEG2000 derivative of HR2 | 41 | Free | Free | Linear | L | Pegylation-PEG2000 of cysteine at 20th position | Modified HR2 wild type peptide | Inhibitor to prevent virus ˆ’host cell membrane fusion | Not mentioned | 20μM | 76.3 | Bovine Trypsin | Trypsin degradation assay, Analytical reverse phase HPLC | Solutions of bovine trypsin and the peptide or PEG ˆ’peptide conjugate in 10 mM PBS (pH 7.4) | in vitro | http://www.drugbank.ca/drugs/DB00172 | None | Cell ˆ’Cell Fusion Inhibition Efficacy (IC50)>401 | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 6 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 100 μg/kg of the body weight | 0.14 ±0.03(t1/2α) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00173 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 7 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 100 μg/kg of the body weight | 2.96 ±1.12(t1/2β) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00174 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 8 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 200 μg/kg of the body weight | 0.15 ±0.06(t1/2α) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00175 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 9 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 200 μg/kg of the body weight | 3.27 ±2.07(t1/2β) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00176 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 10 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 400 μg/kg of the body weight | 0.09 ±0.01(t1/2α) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00177 | None | Not mentioned | |||
| 23099431 | 2012 | GHRP-6 (Growth Hormone-Releasing Peptide-6) | 11 | Free | Amidation | Linear | Mix | None | Synthetic molecule structurally related to Met-enkephalin | Cytoprotective,antioxidant in nature | Not mentioned | 400 μg/kg of the body weight | 1.15 ±0.17(t1/2β) | human plasma proteases | LC-MS | Intravenous bolus administartion in 9 healthy male subjects | in vivo | http://www.drugbank.ca/drugs/DB00178 | None | Not mentioned | |||
| 23196806 | 2012 | TAMRA-TAT [5-(and-6)-carboxytetramethylrhodamine labeled HIV transactivator protein TAT] | 11 | 5-(and-6)-carboxytetramethylrhodamine(TAMRA) | Free | Linear | L | None | HIV | Cell penetrating peptide | Not mentioned | 60 μg/g | 6.7 | Modified simulated intestinal fluid with pancreatic enzymes | HPLC with fluorescence detection | Modified simulated intestinal fluid | in vitro | http://www.drugbank.ca/drugs/DB00179 | None | Fluorescence intensity (intestinal delivery)=4.0×105 in Duodenum, 6.0×105 in Jejunum, 4.0×105 in Ileum, 1×105 in Colon | |||
| 23196806 | 2012 | TAMRA-TAT microemulsion | 11 | 5-(and-6)-carboxytetramethylrhodamine(TAMRA) | Free | Linear | L | None | HIV | Cell penetrating peptide | Not mentioned | Microemulsion composition: Miglyol 812/Capmul MCM/Tween 80/TAMRA-TAT solution at the weight ratio of | 19.4 | Modified simulated intestinal fluid with pancreatic enzymes | HPLC with fluorescence detection | Modified simulated intestinal fluid | in vitro | http://www.drugbank.ca/drugs/DB00180 | None | Fluorescence I ntensity (intestinal delivery)< 1.0×105 in Duodenum, Jejunum, Ileum, Colon | |||
| 23696181 | 2013 | Cx43MP (Connexin43 mimetic peptides) | 12 | Free | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 145.57 ±14.57 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00181 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 90% approx. after 48 hours | |||
| 23696181 | 2013 | C12-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | C12-Laa | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 301.34 ±18.93 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00182 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 85% approx. after 48 hours | |||
| 23696181 | 2013 | C12-C12-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | Two C12-Laa | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 353.39 ±13.63 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00183 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 80% approx. after 48 hours | |||
| 23696181 | 2013 | GlcNS-Cx43 MP (Connexin43 mimetic peptide derivative) | 12 | N-β-D-glucosamine succinamic acid(GlcNS) | Free | Linear | L | None | Synthetic, matching amino acids 199-210 on the extracellular loop 2 of Cx43 | Blocking Cx43 hemichannel mediated vascular leakage in case of retinal ischemia | Aliquots were collected at 0, 5, 30, 60, 120, and 240 min | 500μM | 318.04 ±75.13 | Bovine vitreous proteases | RP-HPLC | 500 μL of freshly collected bovine vitreous | in vitro | http://www.drugbank.ca/drugs/DB00184 | None | Cell viability of NT2/ D1 cells at 100μM of peptide= 85% approx. after 48 hours | |||
| 24133142 | 2013 | GLP2-2G-XTEN (Glucagon like peptide-2-2G-XTEN) | 34 | Free | Ahx-6-aminohexanoic acid, Mpa-3-maleimidopropionic acid conjugated to the amino group of Ahx,XTEN protein | Linear | L | None | Glucagon-like peptide 2 variant | Treatment of short bowel syndrome | Aliquots were collected at 0.08, 4, 8, 24, 48, 72, 96, 120 and 168 h | 2mg/kg of rats | 38.5 ±7.4 | Rats blood proteases | ELISA,RP-HPLC | Subcutaneous injection in female Sprague €“ Dawley strain rats | in vivo | http://www.drugbank.ca/drugs/DB00185 | None | GPCR Ca2+ flux mobilization assay, relative activity=1.43% |