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| ID | PMID | YEAR | Sequence | Name | Length | N-ter MOD | C-ter MOD | Linear/Cyclic | Chirality | Chem-MOD | Origin | Nature | Incubation Time | Concentration | Half Life | Units Half Life | Protease | Assay | Test Sample | Vivo/Vitro | Reference | Patent No. | Activity |
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 15322125 | 2004 | Aβ(1 €“ 42) | 42 | Free | Free | Linear | L | None | Derivative of human Aprecursor protein APP771 | Neurodegenerative | 121 minutes | 2x107 cpm of 125I-Aβ40 peptide | 2.8 | Mouse plasma proteases | Radioactivity measured by scintillation counter | Intravenouly injected into male B6SJLF1/J mice and blood samples collected from tail vein to prepare plasma samples | in vivo | None | None | Neurodegeneration caused by oligomerization | |||
| 11553691 | 2001 | APP-C59 | 59 | Free | Free | Linear | L | None | Amyloid precursor protein derivative | Regulator of synapse formation | 2 hours | Not mentioned | ~5 | Fetal calf serum proteases | Pulse chase experiment | BHK cell line | in vitro | None | None | Not reported | |||
| 11553691 | 2001 | APP-C59 | 59 | Free | Free | Linear | L | None | Amyloid precursor protein derivative | Regulator of synapse formation | 2 hours | Not mentioned | ~5 | Fetal calf serum proteases | Pulse chase experiment | Primary cultures of neurons from PS1 knockout mice's 14 day embryos | in vitro | None | None | Not reported | |||
| 15246869 | 2004 | GIP | 42 | Free | Free | Linear | L | None | Gastrointestinal incretin hormone | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 6 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | 8446620 | None | cAMP EC50=21.8 ±1.5nM | |||
| 15246869 | 2004 | (Abu2)GIP | 42 | Free | Free | Linear | L | 2-aminobutyric acid (Abu) | Synthetic | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | 7.1 | Human plasma protease | Radioimmunoassay | Human plasma | in vitro | None | None | cAMP EC50=36.8 ±1.6nM | |||
| 15246869 | 2004 | GIP | 42 | Free | Free | Linear | L | None | Gastrointestinal incretin hormone | Potentiate postprandial insulin secretion and glucose clearance | 12 hours | 2mM | >12 | Human plasma proteases except DPP | Radioimmunoassay | Human plasma+DPA (DPA is DPP inhibitor) | in vitro | 8446620 | None | cAMP EC50=21.8 ±1.5nM | |||
| 20593470 | 2010 | Peptide 1 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.9 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 2 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 1.1 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 3 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.7 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 4 | 41 | Free | Amidation | Linear | Mix | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.9 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 5 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 4.7 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 6 | 41 | Free | Amidation | Linear | Mix | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 5.1 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 7 | 41 | Free | Amidation | Linear | L | tBu=tertiary butyl | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | >168 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 8 | 41 | Free | Amidation | Linear | L | PhG=phenylglycine | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.5 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 9 | 41 | Free | Amidation | Linear | L | Aib=α-aminoisobutyric acid | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 0.8 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 10 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 20.4 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 11 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 2.5 | None | HPLC | PBS | in vitro | None | None | EC50=0.23 ±0.10nM | |||
| 20593470 | 2010 | Peptide 12 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 2.8 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 13 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 2.4 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 14 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 33.3 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 15 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 7.7 | None | HPLC | PBS | in vitro | None | None | EC50=0.77 ±0.25 | |||
| 20593470 | 2010 | Peptide 16 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | >168 | None | HPLC | PBS | in vitro | None | None | Not reported | |||
| 20593470 | 2010 | Peptide 17 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 50.6 | None | HPLC | PBS | in vitro | None | None | EC50=0.04 ±0.06nM | |||
| 20593470 | 2010 | Peptide 18 | 41 | Free | Amidation | Linear | L | None | Synthetic dipeptide extended GLP-analogs | Regulate blood glucose | 168 hours | Not mentioned | 64 | None | HPLC | PBS | in vitro | None | None | EC50=2.07 ±0.41nM | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 8 | γ-secretase | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 1 | γ-secretase (protease) Lactacystin(protease inhibitor) | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 9822665 | 1998 | H26-57C | 74 | Free | Free | Linear | L | None | Amyloid precursor protein | Not mentioned | 40 minutes | Not mentioned | 10 | γ-secretase (protease) ALLN(protease inhibitor) | Pulse chase experiment | Human embryonic kidney cells | in vitro | None | None | Not mentioned | |||
| 8222093 | 1993 | Recombinant hirudin | 65 | Free | Free | Linear | L | None | Not available | Anticoagulant | Not reported | 1000ng/ml | 2 to 3 | Not mentioned | ELISA | Human blood sample | in vivo | None | None | Not mentioned | |||
| 16099941 | 2005 | proADM 45 €“92 (Adrenomedullin) | 48 | Free | Free | Linear | L | None | Synthetically synthesised proADM 45 €“92 | Vasodilatory peptide | Not reported | 0.29nmol/L | 22 | Human blood proteases | Sandwich immunoluminometric Assay | Human blood plasma | in vitro | None | None | Not given | |||
| 18553094 | 2008 | NT-proBNP | 76 | Free | Free | Linear | L | None | Pro-Brain natriuretic peptide | Vasodilator | Not reported | Not mentioned | ~120 | Human blood proteases | ELISA | Human plasma | in vitro | None | None | Not available | |||
| 17292492 | 2007 | NT-ANP | 98 | Free | Free | Linear | L | None | ANP (A- type natriuretic peptide) | Natriuretic, diuretic and vasorelaxant | Not reported | 650fmol/ml | 1 | Human blood proteases | Radioimmunoassay | Human blood | in vitro | None | None | Not mentioned | |||
| 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 | |||
| N.A. | 2009 | DX-890 | 56 | Free | Free | Linear | L | None | Kunitz domain peptide | Protease inhibitor | N.A. | Not mentioned | 165 | Rabbit blood proteases | I-125 radiolabelling method | Rabbit plasma (Intravenous) | in vivo | None | EP2090589A1 | Inhibition constt (Ki) 6 ±1 pM | |||
| N.A. | 2009 | Human Serum Albumin-DX-890 | 56 | Human serum albumin | Free | Linear | L | None | Kunitz domain peptide | Protease inhibitor | N.A. | Not mentioned | 3500 | Rabbit blood proteases | I-125 radiolabelling method | Rabbit plasma (Intravenous) | in vivo | None | EP2090589A1 | Inhibition constt (Ki) 7 ±1 pM | |||
| N.A. | 2009 | DX-890 | 56 | Free | Free | Linear | L | None | Kunitz domain peptide | Protease inhibitor | N.A. | Not mentioned | 79.44 | Mouse blood proteases | I-125 radiolabelling method | Mouse plasma (Intravenous) | in vivo | None | EP2090589A1 | Not mentioned | |||
| N.A. | 2009 | DX-890-Human Serum Albumin | 56 | Free | Human serum albumin | Linear | L | None | Kunitz domain peptide | Protease inhibitor | N.A. | Not mentioned | 380 | Mouse blood proteases | I-125 radiolabelling method | Mouse plasma (Intravenous) | in vivo | None | EP2090589A1 | Not mentioned | |||
| N.A. | 2011 | Chimeric CNP-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 | 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. | 2009 | Human Corticotropic releasing factor (hCRF) | 41 | Free | Free | Linear | L | None | Hypothalamus | Inhibitor of edema and inflammation | N.A. | 100 micro g/ Kg | 62.6 | Not mentioned | ELISA | Rat plasma (Subcutaneous) | in vivo | None | WO2009027844 | Not mentioned | |||
| N.A. | 2009 | Human Corticotropic releasing factor (hCRF) | 41 | Free | Free | Linear | L | None | Hypothalamus | Inhibitor of edema and inflammation | N.A. | 1000 micro g/ Kg | 72.1 | Not mentioned | ELISA | Rat plasma (Subcutaneous) | in vivo | None | WO2009027844 | Not mentioned | |||
| 1418002 | 1992 | Somatomedin c | 70 | Free | Free | Linear | L | None | Human liver | Growth hormone | Not given | 129.4 ng | 20 | Human serum proteases | Peptide specific immunoassay | Human serum sample | in vitro | PMID 632300 | None | Somatomedin C is a prerequisite for normal muscle homeostasis which is disrupted in fibromyalgia. Regression analysis shows that ~7 % low level of somatomedin c in case of fibromyalgia patients. | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 76 μg | 16.2 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 85 μg | 13.3 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 75 μg | 12.4 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 75 μg | 12.7 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 90 μg | 5.6 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 80 μg | 9.4 (t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 80 μg | 11.6 (mean t1/2 fast) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 76 μg | 70.8 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 85 μg | 49.5 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 75 μg | 95.4 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 75 μg | 90.8 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 90 μg | 47.9 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 80 μg | 83.5 (t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 6605972 | 1984 | Ovine corticotropic releasing factor | 41 | Free | Free | Linear | L | None | Paraventricular nucleus (PVN) of the hypothalamus | Used as a diagnostic test in disease affecting the Hypothalamic pituitary axis | 0, 2, 5, 7,10,15, 20, 25, 30, 45, 60, 90, 120, 150, and 180 min. | 80 μg | 73.0 (mean t1/2 slow) | Human blood plasma proteases | Radioimmunoassay and HPLC analysis | Intravenous administration to human plasma | in vivo | http://www.anaspec.com/products/product.asp?id=322 | None | Not reported | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.033 ±0.004 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 1.22 ±0.237 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Insulin like growth factor 1 (IGF-1) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 5.88 ±0.374 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.064 ±0.052 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.971 ±0.336 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 8.97 ±4.50 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.032 ±0.005 (t1/2 α) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 0.321 ±0.0.091 (t1/2 β) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 11145579 | 2001 | Analogue of Insulin like growth factor 1 (E3A/F49A) | 70 | Free | Free | Linear | L | I125 radiolabeling | Human IGF-1 | Regulate somatic growth and cellular proliferation | 1, 5, 15, and 30 min and at 1, 2, 4, 8, and 24 h | 15 μCi(0.2 ml) | 6.23 ±1.47 (t1/2 Î¥) | Rat blood proteases | TCA precipitation | Intravenous injection into rat | in vivo | PMID:7758431 | None | Human articular cartilage explant is taken and cultured in humidified environment, explant is treated with 40ng/ml of IGF-1, E3A,F49A for 5 days. Proteoglycan synthesis(matrix) synthesis is increased ~ 3 times in E3A/F49A treated sampleas compare to control as measured by scientillation counter. | |||
| 1824807 | 1991 | naP-2 (Neutrophil-activatingprotein-2) | 70 | Free | Free | Linear | L | None | beta- thromboglobulin | Inflammatory peptide | 48 hours | 20 pmol/site | 65-75 | Rabbit blood proteases | Not mentioned | Intradermal injection in rabbit | in vivo | None | None | P- 2 elicited inflammatory responses (neutrophil emigration, edema formation at 20 pmol/l | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 8 | Rat Stomach luminal flushing proteases | TCA precipitation | Rat Stomach luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 5 | Rat Stomach luminal flushing proteases | Antibody assay | Rat Stomach luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 2.5 | Rat Stomach luminal flushing proteases | Receptor-precipitable radioactivity | Rat Stomach luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | TCA precipitation | Rat Duodenum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | Antibody assay | Rat Duodenum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | Receptor-precipitable radioactivity | Rat Duodenum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | TCA precipitation | Rat Ileum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | Antibody assay | Rat Ileum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | Receptor-precipitable radioactivity | Rat Ileum luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 38 | Rat Colon luminal flushing proteases | TCA precipitation | Rat Colon luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 33 | Rat Colon luminal flushing proteases | Antibody assay | Rat Colon luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 16 | Rat Colon luminal flushing proteases | Receptor-precipitable radioactivity | Rat Colon luminal flushing | in vitro | 632300 | None | Stimulate gut growth and repair | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 50 | Rat Stomach luminal flushing proteases | TCA precipitation | Rat Stomach luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Duodenum luminal flushing proteases | TCA precipitation | Rat Duodenum luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 2-5, 5, 7-5, 10 or 20min | 8.6ng | 2 | Rat Ileum luminal flushing proteases | TCA precipitation | Rat Ileum luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 7561632 | 1995 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | 13 amino acid extension peptide at the N-terminus of IGF-I | Free | Linear | L | I125 labeling | Analogue of IGF-I | Growth Hormone | 5, 10, 20, 30 or 60 min | 8.6ng | 60 | Rat Colon luminal flushing proteases | TCA precipitation | Rat Colon luminal flushing | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | Protect the growth factor by steric hindrance of cleavage sites. | |||
| 8194082 | 1993 | Epidermal Growth Factor (EGF) | 53 | Free | Free | Linear | L | I125 labeling | Epidermal Growth Factor | Growth factor | 135 minutes | 1420 Ci/mmol | 12.4 (dissociation t1/2) | Proteases present in human meningioma | Autoradiography | Fresh surgically excised human meningioma specimens | in vitro | 4636327 | None | High concentrations (10-4-10 -2 M) of suramin inhibited 125I-EGF binding to meningioma sections with ICs0's of 3.2 + 0.4 × 1 0 - 4 M | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 50 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 1.05 ±0.04 | Rat blood proteases | Radioimmunoassay | Spontaneously hypertensive rats (SHR) | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg. | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 51 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 1.19 ±0.09 | Rat blood proteases | Radioimmunoassay | Wistar-Kyoto rats | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were - 12.4, -46.6, -61.6 mmHg. | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 52 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 18.1 ±1.4 | Rat blood proteases | Radioimmunoassay | Spontaneously hypertensive rats (SHR) | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg. | |||
| 8542672 | 1995 | Adrenomedullin (AM) | 53 | Free | Amidation | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 1.0 nmol/kg, dissolved in saline | 16.3 ±1.2 | Rat blood proteases | Radioimmunoassay | Wistar-Kyoto rats | in vivo | None | None | The mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were - 12.4, -46.6, -61.6 mmHg. | |||
| 19165353 | 2009 | NT pro-BNP (N-terminal Pro-Brain natriuretic Peptide) | 76 | Free | Free | Linear | L | None | Brain Natriuretic Peptide | Diuretic,natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 60-120 | Human plasma proteases | Not mentioned | Human plasma | in vitro | http://www.phoenixpeptide.com/catalog/product_info | None | NT-pro-BNP is an independent predictor of postoperative myocardial injury in patients undergoing vascular surgery | |||
| 15740458 | 2005 | Rat AM (Adrenomedullin) | 50 | Free | Free | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 200 μl | 2 (distribution t1/2) | Rat blood proteases | Competitive Radioimmunoassay | Intravenous administration in Rat | in vivo | http://www.anaspec.com/products/product.asp?id=304 | None | Not reported | |||
| 15740458 | 2005 | Rat AM (Adrenomedullin) | 50 | Free | Free | Linear | L | None | Human pheochromocytoma | Hypotensive peptide | 30 minutes | 200 μl | 15.9 (elimination t1/2) | Rat blood proteases | Competitive Radioimmunoassay | Intravenous administration in Rat | in vivo | http://www.anaspec.com/products/product.asp?id=304 | None | Not reported | |||
| 3871610 | 1985 | Rat α1- proteinase inhibitor | 60 | Free | Free | Linear | L | Glycosylation | Rat serum | Protelytic activities regulating peptide | 5 minutes, 30 minutes, 1 hour, 4 hour and 7 hour | Not mentioned | 170 (for glycosylated α1- proteinase inhibitor) | Rat serum proteases | Radioimmunoassay | Wistar rats | in vivo | http://www.uniprot.org/uniprot/Q9JMK6 | None | Protect tissue against proteolytic attack by leukocyte elastase | |||
| 3871610 | 1985 | Rat α1- proteinase inhibitor | 60 | Free | Free | Linear | L | None | Rat serum | Protelytic activities regulating peptide | 5 minutes, 30 minutes, 1 hour, 4 hour and 7 hour | Not mentioned | 30 (for unglycosylated α1- proteinase inhibitor) | Rat serum proteases | Radioimmunoassay | Wistar rats | in vivo | http://www.uniprot.org/uniprot/Q9JMK6 | None | Protect tissue against proteolytic attack by leukocyte elastase | |||
| 18586440 | 2008 | NT pro-BNP (N-terminal pro B-type natriuretic peptide) | 76 | Free | Free | Linear | L | None | B-type Natriuretic peptide | Diuretic, Natriuretic and vasodilatory peptide | Not mentioned | Not mentioned | 120 | Human serum proteases | Not mentioned | Humans | in vivo | http://www.phoenixpeptide.com/catalog/product_info | None | NT-pro-BNP (using a cutoff value of >308 pg/mL) is an independent predictor of postoperative myocardial injury in patients undergoing vascular surgery | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 3.2 ±0.1 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 4.9 ±0.02 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 2.8 ±0.1 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 4.6 ±0.5 (t1/2α) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 203 ±10.2 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | Insulin-like growth factor-I (IGF-I) | 70 | Free | Free | Linear | L | I125 labeling | Human IGF-1 | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 185.4 ±4.7 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | 632300 | None | infusion of 125I-IGF-I into rats, 0 ·003 ±0 ·001% (mean ±S.E.M, n=6) of total infused, intact 125I-IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 111.1 ±3.9 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid. | |||
| 10607940 | 2000 | LR(3) insulin-like growth factor-I (IGF-I) | 83 | Free | Free | Linear | L | I125 labeling | Analogue of IGF-I | Promotes formation and repair of bone, stimulates body protein and glucose metabolism and increases glomerular filtration rate and renal plasma flow | 5, 30, 120 and 240 min | 100 μl | 140.2 ±2.5 (t1/2β) | Rat blood proteases | Radioimmunoassay and bi-exponential equation that describes a two-compartment model | Intravenous bolus administration in Rat | in vivo | http://www.cellsciences.com/content/p-detail.asp?r | None | At 5 min 0 ·01 ± 0 ·001% (mean ± S.E.M, n = 6, P < 0 ·001) of total infused intact 125I-LR3IGF-I had appeared per milliliter of wound fluid. | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 0.138 mg/kg | 23.1 ±4.3 | Rat plasma proteases | Competitive ELISA | Rat plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 0.69mg/kg | 21.5 ±3.6 | Rat plasma proteases | Competitive ELISA | Rat plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 1.38 mg/kg | 22.2 ±1.7 | Rat plasma proteases | Competitive ELISA | Rat plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 6.9 mg/kg | 27.5 ±3.7 | Rat plasma proteases | Competitive ELISA | Rat plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 13.8 mg/kg | 30.7 ±2.6 | Rat plasma proteases | Competitive ELISA | Rat plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 9.87 mg/kg | 47.8 | Rat plasma proteases(rat chronic renal insufficiency (CRI) model) | Competitive ELISA | Rat(rat chronic renal insufficiency (CRI) model) plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 0.02 mg/kg | 14.6 ±4.3 | Monkey plasma proteases | Competitive ELISA | Monkey plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 0.1 mg/kg | 16.4 ±1.7 | Monkey plasma proteases | Competitive ELISA | Monkey plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 0.475 mg/kg | 29.9 ±9.4 | Monkey plasma proteases | Competitive ELISA | Monkey plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 16982323 | 2006 | Hematide | 42 | Acetylation | Beta-alanine-PEG | Linear | L | X1-Napthyl-alanine, X2-Sarcosine | Synthetic dimeric peptide | Erythropoiesis stimulating agent | Not mentioned | 1.35 mg/kg | 59.7 ±2.9 | Monkey plasma proteases | Competitive ELISA | Monkey plasma (Dose i/v adminstered) | in vivo | None | None | IC50 = 37pM for HuEPOr/125I-EPO competition binding assay, EC50 =460 pM for cell proliferation stimulation | |||
| 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 | |||
| 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. | |||
| 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 | |||
| 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 | |||
| 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 | |||
| 1319455 | 1992 | hCRH(Human Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 30.5 ±3.3 | Human plasma proteases | IRM(Immunoradiometric assays) | Human plasma | in vivo | 12379493 | None | 22.4 ± 8.1 ng/hour (ACTH response) | |||
| 1319455 | 1992 | hCRH(Human Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 46.5 ±7.2 | Sheep plasma proteases | IRM(Immunoradiometric assays) | Human plasma | in vivo | 12379493 | None | 46.5 ± 6.4 ng/hour (ACTH response) | |||
| 1319455 | 1992 | oCRH(Ovine Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 42.8 ±6.4 | Human plasma proteases | IRM(Immunoradiometric assays) | Sheep plasma | in vivo | 6603620 | None | 39.9 ± 11.7 ng/hour (ACTH response) | |||
| 1319455 | 1992 | oCRH(Ovine Corticotropin Releasing Hormone) | 41 | Free | Free | Linear | L | None | Derived from Pre-hormone | Hormone causes Adrenocorticotropin secrection and neurotransmitter | 2.5-180 minutes | 100μg | 39.8 ±10.1 | Sheep plasma proteases | IRM(Immunoradiometric assays) | Sheep plasma | in vivo | 6603620 | None | 40.2 ± 8.4 ng/hour (ACTH response) | |||
| 1646465 | 1991 | iso-rANP(1-45) (Recombinant atrial natriuretic peptide) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | 1 x 106 cpm | 130 ±13 | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 1646465 | 1991 | iso-rANP(1-45) (Recombinant atrial natriuretic peptide) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | 1 x 106 cpm | 23.7 + 1.7 (α- t1/2) | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 1646465 | 1991 | iso-rANP(1-45) (Recombinant atrial natriuretic peptide) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Derived from ANP (Atrial natriuretic peptide) | Natriuretic and vasodilator | Blood samples collected at 5-1800 seconds after peptide injecteion | 1x 106 cpm | 164.3 ±9.0(β- t1/2) | Rat plasma proteases | Radioimmunoassay | Male Wistar rats plasma (Dose i/p injected) | in vivo | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 45 ±5 | Normal Human plasma proteases | Radioimmunoassay and HPLC | Normal Human plasma | in vitro | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 69 ±8 | Normal Human blood proteases | Radioimmunoassay and HPLC | Normal Human blood | in vitro | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 10.4 ±1.1 | Pancreatitis patients blood proteases | Radioimmunoassay and HPLC | Pancreatitis patient plasma | in vitro | None | None | Not reported | |||
| 1889124 | 1991 | CCK58 (Cholecystokinin 58) | 58 | Free | Amidation | Linear | L | None | Peptide hormone of the gastrointestinal system | Stimulates digestion of fat & protein | 37 °C for 30-180 minutes | 1.6pmol | 11.1 ±1 | Pancreatitis patients plasma proteases | Radioimmunoassay and HPLC | Pancreatitis patient blood | in vitro | None | None | Not reported | |||
| 2162275 | 1990 | PHV (Peptide histidine valine) | 42 | Free | Free | Linear | L | None | Peptide derived from Prepro-VIP | Vasodilator | Not mentioned | 5 pmol min-1 kg-1 | 37.5 | Human plasma proteases | Radioimmunoassay | Human plasma | in vivo | None | None | It increases heart rate but not significantly | |||
| 2966345 | 1988 | rANF(Asn1-Arg98) [Rat atrial natriuretic factor] | 98 | Free | Free | Linear | L | Radioiodinated peptide at Tyr-4 | Rat ANF derivative [Rat atrial natriuretic factor] | Natriuretic, diuretic and vasorelaxant peptide | Not mentioned | 10 X106 CPM | 54.8 ±3.9(2nd component) | Rat plasma proteases | Radioimmunoassay | Male Sprague-Dawley rats plasma | in vivo | http://www.uniprot.org/uniprot/P01161 | None | Not reported | |||
| 2966345 | 1988 | rANF(Asn1-Arg98) [Rat atrial natriuretic factor] | 98 | Free | Free | Linear | L | Radioiodinated peptide at Tyr-4 | Rat ANF derivative [Rat atrial natriuretic factor] | Natriuretic, diuretic and vasorelaxant peptide | Not mentioned | 10 X106 CPM | 2.5 ±0.3(1st compent) | Rat plasma proteases | Radioimmunoassay | Male Sprague-Dawley rats plasma | in vivo | http://www.uniprot.org/uniprot/P01162 | None | Not reported | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 10 µg/kg peptide injected to rhesus monkey | 4.0 ±1.2 (t1/2fast) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1035 ± 226 %, cortisol increased by 123 ± 34% on 10 µg/kg dose | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 100 µg/kg peptide injected to rhesus monkey | 1.5 ±0.5 (t1/2fast) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1858 ± 452 %, cortisol increased by 231 ± 28% on 10 µg/kg dose | |||
| 2988919 | 1985 | oCRF(Ovine corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 1 µg/kg peptide injected to rhesus monkey | 3.6 ±1.1 (t1/2 fast) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 161 ± 40 %, cortisol increased by 78 ± 22 % on 10 µg/kg dose | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 10 µg/kg peptide injected to rhesus monkey | 29.0 ±2.0(t1/2 slow) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1858 ± 452 %, cortisol increased by 123 ± 28% on 10 µg/kg dose | |||
| 2988919 | 1985 | r/hCRF(Human/rat corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 100 µg/kg peptide injected to rhesus monkey | 32.7 ±10.1 (t1/2 slow) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 1858 ± 452 %, cortisol increased by 231 ± 28% on 10 µg/kg dose | |||
| 2988919 | 1985 | oCRF(Ovine corticotropin-releasing factor) | 41 | Free | Free | Linear | L | None | Peptide hormone secreted by hypothalamus | Stimulates corticotropes to secrete adrenocorticotropic hormone (ACTH) | Blood samples collected at 1-180 minutes after peptide injection | 1 µg/kg peptide injected to rhesus monkey | 44.3 +/= 6.7 (t1/2 slow) | Rhesus monkey proteases | Radioimmunoassay | Rhesus monkey plasma | in vivo | None | None | ACTH increased by 161 ± 40 %, cortisol increased by 78 ± 22 % on 10 µg/kg dose | |||
| 3379352 | 1988 | IGF-1 (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | Labelled with 125I | Purified from bovine colostrum | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 6.0-7.0 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 3379352 | 1988 | Reduced IGF-1(Free form) (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | Labelled with 125I, Disulphide bond is reduced | Bovine IGF-1 | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 0.8 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 3379352 | 1988 | Reduced IGF-1(bound form) (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | Labelled with 125I, Disulphide bond is reduced | Bovine IGF-1 | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 6 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 3379352 | 1988 | S-CM IGF-1 (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | S-CM=S-carboxymethylated | Bovine IGF-1 | Mediates growth and development | Blood collected 10 minutes to 30 hours after peptide infusion | 10mM/L | 0.8-0.9 | Lamb plasma proteases | Radioimmunoassay, Binding protein radioactivity assay and IGF-region radioactivity | Eight merino lambs plasma | in vivo | None | None | Not reported | |||
| 2454805 | 1988 | [125I]IGF-I | 70 | Free | Free | Linear | L | None | Human Recombinant peptide | Stmulates glycogen synthesis | Blood collected 10 minutes to 6 hours after peptide injection | 1 µCi peptide injected to rhesus monkey | 100 | Proteases from Rat serum | Radioimmunoassay | Rat Serum | in vivo | None | None | Stimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm | |||
| 2454805 | 1988 | [125I]B-chain mutant IGF-1 | 71 | Free | Free | Linear | L | None | Human Recombinant peptide | Stmulates glycogen synthesis | Blood collected 10 minutes to 6 hours after peptide injection | 2 µCi peptide injected to rhesus monkey | 27.5 | Proteases from Rat serum | Radioimmunoassay | Rat Serum | in vivo | None | None | Stimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm | |||
| 2454805 | 1988 | [125I] [Gln3,Ala4,Tyr15,Leu16]IGF-1 | 70 | Free | Free | Linear | L | None | Human Recombinant peptide | Stmulates glycogen synthesis | Blood collected 10 minutes to 6 hours after peptide injection | 3 µCi peptide injected to rhesus monkey | 26.9 | Proteases from Rat serum | Radioimmunoassay | Rat Serum | in vivo | None | None | Stimulates glycogen synthesis by the incorporation of [14C]glucose into glycogen in rat diaphragm | |||
| 3108068 | 1987 | IGF-1 (Insulin-like growth factor-I) | 70 | Free | Free | Linear | L | None | Purified from bovine colostrum | Mediates growth and development | Blood collected 12hours after peptide injection | 6 - 10 µg/Kg | <15 | Proteases from chicken plasma | Radioimmunoassay | (Dose i/v injected)Chicken plasma | in vivo | None | None | GH concentrations subsequent to TRH injection were significantly depressed45.1 and 48.2% in IGF-l-treated as compared with control chicks; and GRF-stimulated GH secretion was significantly decreased by IGF-I administration in (41.3%) | |||
| 1664804 | 1991 | Rat BNP-45 ( Brain natriuretic peptide-45) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Isolated from rat heart and shown to be a circulating form of rat BNP | Cardiac Natriuretic Peptide | Blood samples collected at 0.5-10 minutes post peptide injection | 2 µg/150ul saline | 45 (t1/2 alpha or initial phase t1/2) | Proteases from Mice (WKY)plasma | Radioimmunoassay | (Dose i/v injected)Mice (WKY) plasma | in vivo | None | None | Urinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.1 | |||
| 1664804 | 1991 | Rat BNP-45 ( Brain natriuretic peptide-45) | 45 | Free | Free | Cyclic (C23-C39) | L | None | Isolated from rat heart and shown to be a circulating form of rat BNP | Cardiac Natriuretic Peptide | Blood samples collected at 0.5-10 minutes post peptide injection | 2 µg/150ul saline | 6.95 (t 1/2 beta or 2nd phase t1/2) | Proteases from Mice (WKY)plasma | Radioimmunoassay | (Dose i/v injected)Mice (WKY) plasma | in vivo | None | None | Urinary sodi µM excretion (uEq/min per kg)= 0.43 ± 0.13, mean arterial pressure (mmHg) = 129 ± 1, Urinary cGMP excretion (pmol/min) = 27.0 ± 3.2 | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 1.05 ±0.04 (1st phase elimination life) | Proteases from SHR rat plasma | Radioimmunoassay | Rat(SHR) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 1.19 ±0.09 (1st phase elimination life) | Proteases from WKY rat plasma | Radioimmunoassay | Rat(WKY) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 18.1 ±1.4 (2nd phase elimination life) | Proteases from SHR rat plasma | Radioimmunoassay | Rat(SHR) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 8542672 | 1995 | Rat adrenomedullin (AM) | 50 | Free | Amidation | Cyclic (C14-C19) | L | None | Member of the calcitonin family of peptides | Hypotensive effect | Blood sample collected after 0.5-20 minutes after drug administration | 1.0nmol/Kg | 16.3 ±1.2 (2nd phase elimination life) | Proteases from WKY rat plasma | Radioimmunoassay | Rat(WKY) plasma | in vivo | None | None | Mean maximal changes in MBP at doses of 0.3, 1.0 and 3.0nmol/kg of AM were -24.0, -78.5, -92.3mmHg for SHR, and - 12.4, -46.6, -61.6 mmHgfor WKY, respectively | |||
| 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 | |||
| 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 | |||
| 1213660 | 1975 | Procine Proinsulin | 84 | Free | Free | Cyclic (C7-C70,C19-C83,C69-C74) | L | None | Proinsulin | Not mentioned | Not reported | 5-8.6 µg/kg were injected. | 8.2 ±0.3 | Porcine blood proteases | Radioimmunoassay | Porcine blood | in vivo | http://www.drugbank.ca/drugs/DB00186 | None | Not reported | |||
| 8035644 | 1994 | Adrenomedullin (ADM) | 52 | Free | Free | Linear | L | None | Synthetic | Hormone in circulation control | Not reported | Intraarterial doses of 0.01-0.3 nmol | 55 to 80 | Cat blood proteases | HPLC | Hind limb vascular bed of the cat | in vivo | http://www.drugbank.ca/drugs/DB00197 | None | Not reported | |||
| 38807146 | 2024 | TG103 | 62 | Free | Fc region of IgG joined through (CH2-CH3) IgD | Linear | L | GLP-1 dimerization | GLP-1 analogs | Antiobesity | Blood sampling time points:(1) Within 2 h before dosing on day 1 and day 8,(2) 6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 15) after dosing on day 8 (3)Within 2 h before dosing on day 64, day 71 and day 78 (4)6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78. | 15.0 mg | 116 ± 10.8 (Terminal Half Life) | Human serum protease | Double-antibody sandwich assay | Human serum | In Vivo | None | None | N.A. | |||
| 38807146 | 2024 | TG103 | 62 | Free | Fc region of IgG joined through (CH2-CH3) IgD | Linear | L | GLP-1 dimerization | GLP-1 analogs | Antiobesity | Blood sampling time points:(1) Within 2 h before dosing on day 1, day 8 and day 15, (2) 6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 22) after dosing on day 15 (3)Within 2 h before dosing on day 64, day 71 and day 78 (4) 6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78. | 22.5 mg | 110 ± 11.9 (Terminal Half Life) | Human serum protease | Double-antibody sandwich assay | Human serum | In Vivo | None | None | N.A. | |||
| 38807146 | 2024 | TG103 | 62 | Free | Fc region of IgG joined through (CH2-CH3) IgD | Linear | L | GLP-1 dimerization | GLP-1 analogs | Antiobesity | Blood sampling time points: (1) Within 2 h before dosing on day 1, day 8, day 15 and day 22, (2)6, 12, 24, 36, 48, 72, 96, 144 and 168 h (before dosing on day 29) after dosing on day 22,(3)Within 2 h before dosing on day 64, day 71 and day 78 (4) 6, 12, 24, 36, 48, 72, 96, 144, 168, 336 and 504 h after dosing on day 78. | 30.0 mg | 116 ± 9.34 (Terminal Half Life) | Human serum protease | Double-antibody sandwich assay | Human serum | In Vivo | None | None | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 36 Hours | 4.06 nmol/kg | 68 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 386.4 nmol/kg | 64 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 350.4 nmol/kg | 77 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 352.5 nmol/kg | 76 | Dogs plasma protease | LC-MS | Dogs plasma | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 375.7 nmol/kg | 46 | Dogs plasma protease | LC-MS | Dogs plasma after food is provided 1 min post dose | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Compound 1 | 43 | Free | Amidation | Linear | Mix | Aib2, aMeF(2F)6, 4PallO, aMeL13, Ornl6, K17, Aib20, D-Glu24 aMeY25, and Ser39 substituitions, Lys17 linked with chemical group ((2-[2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(y-Glu)-CO-(CH2)16-CO2H) | Incretin Analog | Antidiabetes | Blood sample collected over 168 Hours | 377.1 nmol/kg | 55 | Dogs plasma protease | LC-MS | Dogs plasma after food is provided 30 min post dose | In Vivo | None | US 2023/0072968 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 0.1 mg/kg | 3.49 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 1 mg/kg | 3.34 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 10 mg/kg | 7.64 (Initial Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 0.1 mg/kg | 18.8 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 1 mg/kg | 10 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood sample were collected at 2,5,10,20,40,60 Minutes After Dosing And For Animals Receiving 10 Mg/Kg, Additional Samples Were Taken At 90 And 120 Minutes After Dosing | 10 mg/kg | 10.2 (Terminal Elimination Phase) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rat plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 8.4 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.33 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.66 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 14 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 7.11 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 14 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 7 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 8 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma after day 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.67 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma after Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples were collected at 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.85 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.8 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.16 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.31 (Elimination Half Life) | Male wistar rats plasma protease | LC-MS/MS | Male wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 7.04 (Elimination Half Life) | Female wistar rats plasma protease | LC-MS/MS | Female wistar rats plasma After Day 14 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.68 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.83 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 6.59 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 1 mg/kg | 4.66 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.01 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 5.7(Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.05 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 3 mg/kg | 6.13 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.09 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.41 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 6 (Elimination Half Life) | Male dogs plasma protease | LC-MS/MS | Male dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Samples Were Collected At 2,5,10,20,40 Minutes After Dosing On Days 1 Or 14 | 10 mg/kg | 5.9 (Elimination Half Life) | Female dogs plasma protease | LC-MS/MS | Female dogs plasma After Day 1 Repeated Dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 25 μg/kg | 0.79 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 50 μg/kg | 0.92 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 100μg/kg | 1.15 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected At The Following Time Points: Pre-Dose, Then, 10 Min,20 Min,30Min,0.75,1,1.5,2,2.5,3,4,6,8,12,16 And 24 H After Infusion Start | 150 μg/kg | 1.15 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 50 μg/kg | 1.38 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 100μg/kg | 2.18 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 140 μg/kg | 1.94 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 200 μg/kg | 1.94 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| N.A. | 2024 | Peptide 1 | 47 | Free | Amidation | Linear | L | V24L modifications | Annexin A1 Derivative | Antiinflammatory | Blood Samples Were Collected For Pk Purpose For Peptide 1 Determinations On Day 1 At The Following Time Points: Pre-Dose, Then 10 Min, 20 Min, 30 Min = 0.5, 0.75, 1.0, 1.5, 2.0, 2.5, 3.0, 4.0, 6.0, 8.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 8.16, 8.32, 8.5, 8.75, 9.0, 9.5, 10.0, 10.5, 11.0, 12.0, 14.0, 16.0, Then 10 Min, 20 Min, 30 Min After The Second Infusion Start, I.E. 16.16, 16.32, 16.5, 16.75, 17.0, 17.5, 18.0, 18.5, 19.0, 20.0, 22.0 And 24 Hours After The First Infusion Start | 250 μg/kg | 1.88 (Elimination Half Life) | Human plasma protease | LC-MS/MS | Human plasma received three 8 hours apart 30-min peptide 1 repeated dose | In Vivo | None | EP 2023067975 W | N.A. | |||
| 37874823 | 2023 | MDK1472 | 42 | Acetylation | Free | Cyclic (Disulphide Bond Bw C7-C16, C32-C41) | L | IL-7Ra binding domain linked with yc binding domain with the help of linker GGS linker | Synthetic | IL-7R agonist peptide | 37 °C | 10 mM | 60 | Human Plasma Protease | LC-MS/MS | Human plasma | In Vitro | None | None | IC50(nM) = 340 (IC50 values in a competition ELISA for compound binding to human IL-7Rα) | |||
| 37874823 | 2023 | MDK1472 | 42 | Acetylation | Free | Cyclic (Disulphide Bond Bw C7-C16, C32-C41) | L | IL-7Ra binding domain linked with yc binding domain with the help of linker GGS linker | Synthetic | IL-7R agonist peptide | 37 °C | 10 mM | 104 | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vitro | None | None | IC50(nM) = 190 (IC50 values in a competition ELISA for compound binding to Cyno IL-7Rα) | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 200 nmol/kg | 36.4 (Terminal Half Life) | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC 50 (nM) = 109 ± 24 of LY3540378 in Rat RXFP2 | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 100 nmol/kg | 124 (Terminal Half Life) | Cynomolgus monkeys plasma protease | LC-MS | Cynomolgus monkeys plasma | In Vivo | None | None | EC 50 (nM) = 19.3 ± 4.0 of LY3540378 in Cynomolgus monkey RXFP2 | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 100 nmol/kg | 45.7 (Terminal Half Life) | Cynomolgus monkeys plasma protease | LC-MS | Cynomolgus monkeys plasma | In Vivo | None | None | EC 50 (nM) = 19.3 ± 4.0 of LY3540378 in Cynomolgus monkey RXFP2 | |||
| 36780899 | 2023 | LY3540378 | 64 | Free | Relaxin-A chain linked with albVHH domain at C terminus, A and B chain linked by linker | Linear | L | None | relaxin-2 analog | Treatment of Chronic Heart Failure | N.A. | 30 nmol/kg | 39.7 ± 1.8 (Terminal Half Life) | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | None | EC 50 (nM) = 109 ± 24 of LY3540378 in Rat RXFP2 | |||
| N.A. | 2023 | Non-converting compound 1 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Aib at position 4, Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.8 mg | 137 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 2 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Aib at position 4,Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.5 mg | 130 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 3 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 , | Free | Linear | L | Aib at position 4,Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys 16 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 115 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 4 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl attached to Lys1 | Amidation | Linear | L | Aib at position 4,Chem. 11[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19-carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys20 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 136 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 1 | 41 | D-Lys conjugated with [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] | Free | Linear | Mix | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 , Sar2, Aib modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.1 mg | 146 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 2 | 41 | Free | Free | Linear | L | Aeg = N-(2-aminoethyl)glycine, Chem.16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Aeg2, Chem.8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 142 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 3 | 41 | Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modification | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3 mg | 139 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 5 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to L-Aeg | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.8 mg | 106 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 12 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modfications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.7 mg | 143 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 13 | 41 | Chem. 17[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.8 mg | 121 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 14 | 41 | Chem. 22[(2S)-2,6-bis[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]hexanoyl] attached to Lys1 | Free | Linear | L | Chem. 10[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.2 mg | 119 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 15 | 41 | Chem. 17[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4- carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 mg | 124 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 16 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys 16, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 96 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 17 | 41 | Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to G-Aeg | Free | Linear | L | Chem.7[(2S)-2-amino-6-[[(2S)-2-amino-6-[[(4S)-4-carboxy-4-(17- carboxyheptadecanoylamino)butanoyl]amino]hexanoyl]amino]hexanoyl] attached to Lys16, Aib modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 3.2 mg | 105 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 18 | 41 | Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Amidation | Linear | L | Chem.11 [2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(19- carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys20, Sar2 modification | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2.9 mg | 88 (Terminal Half Life) | Beagle dogs plasma protease | LC-MS | Beagle dogs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Non-converting compound 1 | 41 | Lys side chain conatins Chem. 16[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Aib at position 4, Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 nmol/kg | 170 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 1 | 41 | D-Lys conjugated with [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] | Free | Linear | Mix | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 , Sar2 modification | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 20 nmol/kg | 118 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 3 | 41 | Chem. 16 [(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl] attached to Lys1 | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 2 nmol/kg | 119 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 9 | 41 | Chem. 19[2-[[(4S)-4-carboxy-4-(15-carboxypentadecanoylamino)butanoyl]amino]acetyl] attached to Lys1 | Free | Linear | L | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33, Sar2 modifications | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 20 nmol/kg | 102 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| N.A. | 2023 | Compound 10 | 41 | Chem. 21[2-[2-[2-[[2-[2-[2-[[(4S)-4-carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to D-Lys1 | Free | Linear | Mix | Chem. 8[2-[2-[2-[[2-[2-[2-[[(4S)-4- carboxy-4-(15- carboxypentadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy] acetyl] attached to Lys33 | Synthetic | GLP-1/GIP receptor co-agonist | N.A. | 20 nmol/kg | 118 (Terminal Half Life) | Minipigs plasma protease | ELISA or similar antibody based assay or LC-MS | Minipigs plasma | In Vivo | None | EP 2023051315 W | N.A. | |||
| 36997003 | 2023 | Compound 15 | 41 | Free | Terminal Lys side chain linked to C16 fatty acid via linker yE-C16 at C terminal | Linear | Mix | D-Ser2 substiuition | GLP-1 analogs | Dual GLP-1/Glucagon receptor agonist | The mice were sacrificed, and blood samples were collected after 0.083, 0.25, 1, 2, 4, 8, 16, and 24 h after application | 1 mg/kg | 2.2 | C57/B16 female mice plasma protease | LC−MS/MS | C57/B16 female mice plasma | In Vivo | https://www.nature.com/articles/s41598-022-21251-y | None | GLP-1 receptor : EC50 = 5.2 pM | |||
| 36101452 | 2022 | IgG1 S-AM (6-52) | 47 | IgG1 Fc linked with hAM using linker (GGGGS)3 | Amidation | Cyclic (C16-C21 Disulfide Bond In Ham) | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 2.11 | Wistar rats plasma protease | ELISA (measure mAM) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | IgG4 S-AM (6-52) | 47 | IgG4 Fc linked with hAM using linker (GGGGS)3 | Amidation | Linear | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 2.37 | Wistar rats plasma protease | ELISA (measure mAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | IgG1 S-AM (6-52) | 47 | IgG1 Fc linked with hAM using linker (GGGGS)3 | Amidation | Cyclic (C16-C21 Disulfide Bond In Ham) | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 2.885 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | IgG4 S-AM (6-52) | 47 | IgG4 Fc linked with hAM using linker (GGGGS)3 | Amidation | Linear | L | None | hAM-IgG Fc fusion protein | AntiiInflammatory | Blood was collected before injection (day 0), and then 1, 2, 4, 6, 8, 10, 12, and 14 days after administration | 30 nmol/kg | 3.23 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | AM | 52 | Free | Amidation | Cyclic (C16-C21 Disulfide Bond) | L | None | Isolated from Human pheochromocytoma | Vasodilator and Cardiovascular Protection | Blood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration | 50 nmol/kg | 32.3 | Wistar rats plasma protease | ELISA (measure mAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 36101452 | 2022 | AM | 52 | Free | Amidation | Cyclic (C16-C21 Disulfide Bond) | L | None | Isolated from Human pheochromocytoma | Vasodilator and Cardiovascular Protection | Blood was collected before injection (0 min), and then 15, 30, 60 and 120 min after administration | 50 nmol/kg | 27.5 | Wistar rats plasma protease | ELISA (measure tAM ) | Wistar rats plasma | In Vivo | None | None | After treatment with IgG4-AM (6-52), SBP (Systolic Blood Pressure) decreased significantly over time, showing reductions of 24.3 ± 4.8 mmHg on day 3, 32.2 ± 6.9 mmHg on day 6, 40.7 ± 3.1 mmHg on day 9, and 56.6 ± 4.5 mmHg on day 12, compared to the control group | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | Blood samples were collected before RA15127343 administration (baseline) and 1–4 times per day until study end. | 10 nmol/kg | 47 | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | Blood samples were collected before RA15127343 administration (baseline) and 1–4 times per day until study end. | 10,30,45,60 nmol/kg | 48 - 59 | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | N.A. | 200 nmol/kg | 11 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35892256 | 2022 | RA15127343 | 51 | Free | Free | Linear | L | Albumin binding fatty-acid side chain is coupled to lysine (B29) | Insulin analogue | Antidiabetes | N.A. | 200, 400 nmol/kg | 21 - 22 | Rats plasma protease | LC-MS/MS | Rats plasma | In Vivo | https://sci-hub.st/10.1016/j.jpba.2018.07.009 | None | (Activity values of RA15127343) IC50 for IR-A: 19.9 μM, IC50 for IR-B: 6.31 μM, EC50 for IR-A: 2.054 μM, EC50 for IR-B: 669.6 nM | |||
| 35150805 | 2022 | Exenatide-4aa-ABNF | 43 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 4 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 19.6 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 1.387 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-7aa'-ABNF | 46 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 7 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 20.8 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.5785 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-7aa-ABNF | 46 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 7 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 19.3 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.7459 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-12aa-ABNF | 51 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 12 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 400 nmol/kg | 21.9 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.8065 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-25aa-ABNF | 64 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 25 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 370 nmol/kg | 18.7 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.4903 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| 35150805 | 2022 | Exenatide-Exenatide-4aa-ABNF | 82 | Free | Albumin binding Nanofitins (ABNF) linked at C terminus by 4 aa | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sampling was performed at 0.083, 0.5, 4, 24, 48 and 72 h after injection | 300 nmol/kg | 20.5 (Terminal Half Life) | Male CDR1 mice plasma protease | ELISA | Male CDR1 mice plasma | In Vivo | PDB id: 7MLL | None | EC50 = 0.3708 nM ( in the classical in vitro GLP1R cell based assay based on cAMP) | |||
| N.A. | 2022 | Streptavidin-[e9-XPLGLAG-r9-k(cy5)]4 | 100 | Streptavidin | Cy5 linked with Lys side chain at C terminus | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Strep=Streptavidin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 4 nmol | 4 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | G5-PAMAM4-[e9-XPLGLAX-r9-k(cy5)]2[PEG]126 | 48 | G5-PAMAM4 | Cy5 linked with Lys side chain at C terminus, PEGylation | Linear | Mix | e=D-Glutamic acid, r=D-Aspartic acid, k=D-Lys, Strep=Streptavidin, Cy5 = indocarbocyanine dye conjugated with Lys at C terminal, X=linker | Synthetic | Transport molecule | Blood was collected in a heparinized capillary tube at 30 minutes and 1, 2 And 6 hour time points | 3 nmol | 20 | Mice blood plasma protease | N.A. | Mice blood plasma | In Vivo | None | US 201916457763 A | N.A. | |||
| N.A. | 2022 | Example 12 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modification, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 46 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13 | |||
| N.A. | 2022 | Example 1 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG), B3E, B27E, B28E modifications, , A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 103 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 66.3 | |||
| N.A. | 2022 | Example 7 | 51 | Free | B29R, desB30 modificaiton | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 86 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 124.4 | |||
| N.A. | 2022 | Example 10 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 97 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3 | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 987 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 713 pmol/kg | 182 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1714 pmol/kg | 148 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 720 pmol/kg | 153 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 706 pmol/kg | 158 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 45 | 51 | Free | B29R, desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu-2×OEG), B3E, B26E modifications | Insulin Derivative | Antidiabetes | Blood sample taken at the following time points: Predose (-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1735 pmol/kg | 219 | Lyd pig plasma protease | ELISA | Lyd pig plasma | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 4 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A14E, A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B27E, B28E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 24 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 28.6 | |||
| N.A. | 2022 | Example 10 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B28D modification, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 28 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 77.3 | |||
| N.A. | 2022 | Example 11 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E, B28E modificatino, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 28 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13.6 | |||
| N.A. | 2022 | Example 12 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 25 | SD rats plasma protease | LC-MS | SD rats plasma | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 13 | |||
| N.A. | 2022 | PA2 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-gGlu-2×OEG) modifications | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 24 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | PA3 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)tetradecanedioyl-4×gGlu), B28D modifications | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 26 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 33 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B28D modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 58 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 85.1 | |||
| N.A. | 2022 | Example 31 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B27E, B28E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 79 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | hIGF1R 0.1% HSA (% rel to HI) Ex48 = 55 | |||
| N.A. | 2022 | Example 41 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-4×gGlu), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 57 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | Example 42 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG), B3E, B26E modifications, A and B chain linked with disulfide bond | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 41 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| N.A. | 2022 | PA1 | 51 | Free | B29R, desB30 modification | Cyclic (C7-C12 disulfide bond in A chain) | L | A22K(N(eps)hexadecanedioyl-gGlu-2×OEG) modification | Insulin Derivative | Antidiabetes | Plasma collected at time points 0,3,7,15,30,60,120,180 Minutes After Dosing | 25 nmol/kg | 41 | SD rats plasma protease | LC-MS | SD rats plasma with 3 Zn/Hexamer Of Insulin Derivative | In Vivo | None | US 201615754395 A | N.A. | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 3.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 2.48 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 2.48 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 7.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.32 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 7.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.32 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 9.76 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 6.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 9.76 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 2.2 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.52 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 2.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.52 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 9.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 32.87 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C6 (N-[ε-maleimidocaproyloxy] sulfosuccinimide ester, EMCS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 11.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 32.87 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 11.01 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 11.01 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.29 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 4.4 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.29 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 14 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 86.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with chondroitin [CH] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 12.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 86.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 7.3 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 6.1 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 0.93 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | K29(B) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 16.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 24.16 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) withheparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 5.6 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 8.68 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (LysB29) | 50 | Free | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 6.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 1.25 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1/LysB29) | 50 | Gly1(A) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) withheparosan [HPN] | K29(B) Maleimide modified linked using linker C11 (N-[κ-maleimidoundecanoyloxy]- sulfosuccinimide ester, KMUS) with heparosan [HPN] | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 12.9 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 88.23 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 5.7 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with chondroitin [CH] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 340 nmol/kg | 9.5 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 4.84 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 8 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 35259149 | 2022 | CH-/HPN-Conjugated Insulins (GlyA1) | 50 | Gly1(A) Maleimide modified linked using linker C3 (N-[β-maleimidopropyloxy] succinimide ester, BMPS) with heparosan [HPN] | Free | Cyclic (C6-C11 disulfide bond in A chain) | L | C7-C7 and C20-C19 disulfide bond between A and B chain | Human insulin analog | Antidiabetes | Blood samples were collected immediately before injection and at various time points up to 48 h after injection | 100 nmol/kg | 11.7 | Mice serum protease | Sandwich ELISA | Mice serum | In Vivo | https://pubs.acs.org/doi/10.1021/acsomega.9b00059, https://pubmed.ncbi.nlm.nih.gov/28365509/ | None | EC50(nM) = 6.54 | |||
| 33825469 | 2021 | FITC-labeled Ex4−DNP 9 | 44 | FITC-Ahx | Ex4 linked to DNP9 = Dinitro phenol by (PEG)n spacer | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 2.07 ± 0.05 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33825469 | 2021 | FITC-labeled Ex4−DNP 10 | 44 | FITC-Ahx | Ex4 linked to DNP10 = Dinitro phenol by (PEG)n spacer | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 3.55 ± 0.33 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33825469 | 2021 | FITC-labeled Ex4−DNP 11 | 44 | FITC-Ahx | Ex4 linked to DNP11 = Dinitro phenol by (PEG)n spacer | Linear | L | None | GLP-1 analogs | Antidiabetes | Blood sample (20 μL) was obtained from the leg veins and using a pipette added into 80 μL of PBS solution (containing EDTA) at 40 s, 25 min, 50 min, 1.2 h, 1.6 h, 2 h, 4.8 h, 6.5 h, 8.5 h, 10 h, and 24 h after injection. | 75 nmol/kg | 2.62 ± 0.17 | C57Bl/6 mice plasma protease | Fluorescence assay | C57BL/6 mice plasma | In Vivo | None | None | EC50 values = 0.99 nM for Ex4 (GLP-1 Receptor Activation Potency) | |||
| 33245951 | 2021 | GIP(1–42) | 42 | Free | Free | Linear | L | None | Secreted by entero-endocrine K cells located in the proximal intestine | Insulinotrophic Effect | Blood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min | 25 nmol/kg | 93 ± 2 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type= | None | N.A. | |||
| 33245951 | 2021 | GIP(1–42) | 42 | Free | Free | Linear | L | None | Secreted by entero-endocrine K cells located in the proximal intestine | Insulinotrophic Effect | Blood samples (50 μL) were drawn from the retro-orbital plexus at t = 0, 1, 3, 5, 10 and 20 min and then co-incubation with Val-Pyr | 25 nmol/kg | 5 ± 0.6 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://pdf.sciencedirectassets.com/271102/1-s2.0-S0014579300X09702/1-s2.0-0014579381802888/main.pdf?X-Amz-Security-Token=IQoJb3JpZ2luX2VjEIr%2F%2F%2F%2F%2F%2F%2F%2F%2F%2FwEaCXVzLWVhc3QtMSJHMEUCIQD62SR4A%2B4hs8dyDimRd8i4eqjFdUt5lDROOjPQfQfVdAIgCzazhyIQYpOf0Ptr2TaxQcJ0gfc0tFJSvp00rqp72KMqsgUIExAFGgwwNTkwMDM1NDY4NjUiDFKOQuOPiilKRo0IGiqPBYnEsqS8aZVPDGyG07f6LcX2zV6C1BU1jQ%2BiYzudplRLnaMGn2dzKqD0IgA3jsmhp7CPygQevWTs4Ed1E%2FEvWjuhN8AOvlXEs2Af0t7zL6%2Ba6LtjwN7ZRUIgQGtEhxXKjkWXm9SbXNXu%2FW%2B0ZCHb36rhKfxxcw6e3m0TTTQ5VBU5YtjFRc9KPiAZsUvrVg42y6wbkYdoImtbRueY2e67MmEBizqQ12ayvDeaiudwbYmOGBGr%2BGvimIbEui5OYl1NgebT3Q8%2F%2F5MQ6z0bJxhTQQvplmdG7ymlRrCWfaYdi6ama4%2FpLbZKNVGuU9hscZNpcQUayR82zK3CBh9HRLr%2BTXe6OyFGBRn56BpJ1b%2Bh7qQZYMWBDZGMQdNungv743HpUHMuIxKAt3%2B8SEJ1WkfsIsptsTXEJ%2Fe5Pe2WTSkejT7b9WNpvYncidJCF2lT8NW9RfAw8mc7boYYiFuzqfjULjJV2W6KiXDtf%2F3yQmIV8VRa6hHVovZEQlYpMNpkWgqXznwKL5Lf%2FVUx09SOMK8MoHIWUbF8kgKRM9zGxSs3lPKU7g5gnTqcLwgUKBTnYjjS%2Bm0kz5A4Y4PRE0NI5L4Uy4iF0moVtD6fcXJ7uceU5ofMjnk4jTbla86W0LkLEI6VxBLN2vyWJ%2BkiKXE0GmT7xerhOiY%2FJt74ImPgZVDf6nKzoNAKgoEW5yIBW8X8eRQhNQgbPrCSTSwcAW%2BCoULg4xS3aG87frYuj3ZSUb1DOHzkIRq5G9yj7EjgVbroxu2hh3g9YytLb2PpbvOVSTe%2B%2F2zm04ZibPDOd9UEZQPhgDMGQLnEQ0oKpHU3xaThRzRdTnF%2B6Va%2F7nTk9HXfj3MLfKH3vRbkHVcuODJZVomDO2Awq9mnuQY6sQFg6uBpRDSJbdGuJM4MBWHMJAuiWcghOQq8RAfYeWwCKcdeeLjIPYYpXygg22s0S36%2BiClhIk6QXuPZWihQ%2BbG2PEAcUOIXqLpPHTWwmjGIGrKcTPHPEJKRYKb6HCmW5yCqSEXiKCKgJXX2OzfABfGdtJxraYtj94rVu3tUZ2J1%2Bp4icKKPMKSJaHNBTuKzqNmpvnDyVRDiT0L2iJhacy9SB9TOXT9U0gMzOfOZeQk%2Famo%3D&X-Amz-Algorithm=AWS4-HMAC-SHA256&X-Amz-Date=20241105T104258Z&X-Amz-SignedHeaders=host&X-Amz-Expires=300&X-Amz-Credential=ASIAQ3PHCVTY7EKIR4FY%2F20241105%2Fus-east-1%2Fs3%2Faws4_request&X-Amz-Signature=da086866fd5ae7aa1850a8ed33269fdcc94d601135b6ec16e293756e1d2b3045&hash=fbb1651e9188cb1c761d3e5215af03584aadf82583c0ccbb7e874e4504a450ee&host=68042c943591013ac2b2430a89b270f6af2c76d8dfd086a07176afe7c76c2c61&pii=0014579381802888&tid=spdf-dbd1ce2d-f820-4e78-8534-eac97584de70&sid=5ffdcf685136184f4559b673ec8c38454df3gxrqb&type= | None | N.A. | |||
| 33049303 | 2021 | GLP-GA3-GS-L3 | 94 | Free | Free | Linear | L | GLP-1 linked with GA3 through L3 linker, FITC labeled | Synthetic | Antidiabetes | 8 h at 4 ◦C | 50 μg | 36.3 ± 7.8 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50) | |||
| 33049303 | 2021 | GLPABD035-GS-L3 | 93 | Free | Free | Linear | L | GLP-1 linked with ABD035 through L3 linker, amino acid subsituitions with F,R,K,E,K,L,H, FITC labeled | Synthetic | Antidiabetes | 8 h at 4 ◦C | 50 μg | 31.3 ± 1.0 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50) | |||
| 33049303 | 2021 | GLP-ABDCon-GS-L3 | 93 | Free | Free | Linear | L | GLP-1 linked with ABDCon through L3 linker, amino acid subsituitions with K,E,K,I,E,K,I,T,F,D,K,N,K,K, FITC labeled | Synthetic | Antidiabetes | 8 h at 4 ◦C | 50 μg | 38.3 ± 2.7 | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | Based on the ELISA method, we also found that the fusion proteins containing GA3, ABD035 and ABDCon showed no significant difference in apparent affinity for HSA (P > 0.50) | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | Conventional unsubstituted β-eliminative linker, linked by a GDM linker and Mod = (CH3)2NSO2− | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | ~2020 (Release Half Life) | N.A. | N.A. | N.A. | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | Conventional unsubstituted β-eliminative linker | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | 900 (Release Half Life) | Rats | N.A. | Rats | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | with GDM linker and Mod = (CH3)2NSO2− | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | ~1800 (Release Half Life) | N.A. | N.A. | N.A. | In Vitro | PDB id: 7MLL | None | N.A. | |||
| 33822591 | 2021 | MS−[Gln28]exenatide | 87 | Free | Free | Linear | L | Conventional unsubstituted β-eliminative linker | Exendin-4 analogs | Antidiabetes | pH 7.4, 37 °C | N.A. | 750 (Release Half Life) | Rats | N.A. | Rats | In Vivo | PDB id: 7MLL | None | N.A. | |||
| 33284103 | 2020 | Mouse ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 0 to 5 hr at 37°C | 100 ng/mL | ~120 | Mouse plasma protease | ELISA | Mouse plasma | In Vitro | None | None | N.A. | |||
| 33284103 | 2020 | Mouse O-glycosylated ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | O-glycosylation likely at Ser8 in SVPSPDP, Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 0 to 5 hr at 37°C | 100 ng/mL | >5 | Mouse plasma protease | ELISA | Mouse plasma | In Vitro | None | None | N.A. | |||
| 33284103 | 2020 | Mouse O-glycosylated ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | O-glycosylation likely at Ser8 in SVPSPDP, Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 2 hours at 37°C | 40 ng/g | ~182 | Mice serum protease | OCN ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 33284103 | 2020 | Mouse ucOCN | 46 | Free | Free | Cyclic (C19-C25 Disulfide bond) | L | Uncarboxylation at all glutamic acid | Osteoblast Derived hormone | Antidiabetes | 2 hours at 37°C | 40 ng/g | ~108 | Mice serum protease | OCN ELISA | Mice serum | In Vivo | None | None | N.A. | |||
| 33125843 | 2020 | 5a | 45 | Free | Either or nonsulfated gastrin-6 were coupled to the C-terminus of 2d and 2k through two OEG spacers, affording 5a−5d | Linear | L | Aib substiuition at position 2, Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 1.7 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.040 ± 0.011 (Effects of 5a on GLP-1R) | |||
| 33125843 | 2020 | 5b | 45 | Free | Either or nonsulfated gastrin-6 were coupled to the C-terminus of 2d and 2k through two OEG spacers, affording 5a−5d | Linear | L | Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 1.9 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.048 ± 0.018 (Effects of 5b on GLP-1R) | |||
| 33125843 | 2020 | 6a | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | C1 = structure given in paper, Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 4.6 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.022 ± 0.008 (Effects of 6a on GLP-1R) | |||
| 33125843 | 2020 | 6b | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | C1 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 5 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R) | |||
| 33125843 | 2020 | 7a | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | Modification of 6a and 6b with the introduction of C2 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 2.9 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R) | |||
| 33125843 | 2020 | 7b | 45 | Free | 4c, 4d, 4m, and 4n were next C-terminally modified with the sequence Tyr-Gly-Trp-Leu-Asp-Phe-NH2 using two OEGs as the linker to generate 6a−6d | Linear | L | Modification of 6a and 6b with the introduction of C2 = structure given in paper,Aib substiuition at position 2,Ser39 linked with fatty acid | GLP-1 analogs | Antidiabetes | At 0, 1, 2, 4, 8, 16, and 24 h, blood samples (~100 μL) were collected from fundus venous plexus | 50 nmol/kg | 3.1 | SD rats plasma protease | LC−MS/MS | SD rats plasma | In Vivo | None | None | EC50 (nM) = 0.041 ± 0.017 (Effects of 6b on GLP-1R) | |||
| 33057063 | 2020 | ALM6 | 75 | Free | Free | Linear | L | None | Synthetic | Her4-Selective Agonism | Overnight at 4 °C | 10 μg/mL | 1.4 | Mouse serum protease | ELISA | Mouse serum | In Vitro | None | None | HER4 binding KD = 440 nM | |||
| 32841660 | 2020 | XFL6 | 43 | Free | Free | Linear | L | Modifcation of lysine site at position at 16 with C16 fatty acid | GLP-1/GIP/Gcg receptor triagonist | Antidiabetes, Antiobesity | N.A. | 10 nmol/kg | 41.35 ± 1.42 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R) | |||
| 32841660 | 2020 | XFL6 | 43 | Free | Free | Linear | L | Modifcation of lysine site at position at 16 with C16 fatty acid | GLP-1/GIP/Gcg receptor triagonist | Antidiabetes, Antiobesity | N.A. | 30 nmol/kg | 58.23 ± 2.17 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R) | |||
| 32841660 | 2020 | XFL6 | 43 | Free | Free | Linear | L | Modifcation of lysine site at position at 16 with C16 fatty acid | GLP-1/GIP/Gcg receptor triagonist | Antidiabetes, Antiobesity | N.A. | 90 nmol/kg | 75.81 ± 3.58 | SD rats serum protease | N.A. | SD rats serum | In Vivo | None | None | EC50 (nM) = 0.12 (In vitro receptor activation profiles of XFL peptides for GLP-1R) | |||
| 32736262 | 2020 | EX-AFF | 84 | Free | AFF | Linear | L | None | Synthetic | Antiobesity | Blood was withdrawn at 0, 5 min, 30 min, 1 h, 2 h, 4 h, 6 h, and 8 h post-administratio | 50 nmol/kg | 1.5 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32736262 | 2020 | EX-ABD | 84 | Free | ABD | Linear | L | None | Synthetic | Antiobesity | Blood was withdrawn at 0, 10 min, 1 h, 3 h, 8 h, 1 day, 2 day, 3 day, 4 day, 7 day, 10 day, and 14 day post-administratio | 50 nmol/kg | 84.02 | ICR mice plasma protease | ELISA | ICR mice plasma | In Vivo | None | None | Kd(M) = 6.97 * 10-8(binding affinities of EX-ABD-AFF to glucagon-like peptide-1 receptor (GLP-1)) | |||
| 32387412 | 2020 | DIG-2 | 62 | Free | bisMal-PEG(10KDa) | Linear | L | Radioiodinated , A8G, G31C modification in GLP-1 | DIG conjugates | Antidiabetes | The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C | 50 nmol/kg | 62.6 | Cynomolgus monkeys plasma protease | RP-HPLC | Cynomolgus monkeys plasma | In Vivo | None | None | kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD | |||
| 32387412 | 2020 | DIG-2 | 62 | Free | bisMal-PEG(10KDa) | Linear | L | Radioiodinated , A8G, G31C modification in GLP-1 | DIG conjugates | Antidiabetes | The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C | 100 nmol/kg | 97.2 | Cynomolgus monkeys plasma protease | RP-HPLC | Cynomolgus monkeys plasma | In Vivo | None | None | kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD | |||
| 32387412 | 2020 | DIG-2 | 62 | Free | bisMal-PEG(10KDa) | Linear | L | Radioiodinated , A8G, G31C modification in GLP-1 | DIG conjugates | Antidiabetes | The collected samples at predose, 0.5, 1, 2, 4, 8, 24, 36, 48, 96, 144 and 168 h were stored at −80 °C | 150 nmol/kg | 120.4 | Cynomolgus monkeys plasma protease | RP-HPLC | Cynomolgus monkeys plasma | In Vivo | None | None | kd (1/s) = 6.54 × 10−3 (binding results for DIG conjugates 2 with human GLP-1R ECD | |||
| 35496622 | 2020 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | Exendin-4 analogs | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 7.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.076 ± 0.013 for Lixisenatide (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1a | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 13.2 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.19 ± 0.02 for Lixisenatide 1a (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1b | 44 | Free | Amidation | Linear | L | (X2) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 19.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.49 ± 0.11 for Lixisenatide 1b (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1c | 44 | Free | Amidation | Linear | L | (X3) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 30 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.98 ± 0.24 for Lixisenatide 1c (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1d | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 13.1 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.085 ± 0.021 for Lixisenatide 1d (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1e | 44 | Free | Amidation | Linear | L | (X2) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 21.2 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.13 ± 0.03 for Lixisenatide 1e (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1f | 44 | Free | Amidation | Linear | L | (X3) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 33.4 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.32 ± 0.13 for Lixisenatide 1f (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1g | 44 | Free | Amidation | Linear | L | (X1) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 11.9 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 0.59 ± 0.16 for Lixisenatide 1g (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1h | 44 | Free | Amidation | Linear | L | (X2) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 17.8 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 1.97 ± 0.53 for Lixisenatide 1h (in vitro GLP-1 receptor activation potency) | |||
| 35496622 | 2020 | Lixisenatide 1i | 44 | Free | Amidation | Linear | L | (X3) MPAs modification on Lys12 | lixisenatide analogues | Antidiabetes | incubated at 37 °C for 6, 12, 24, and 48 h | 1000 ng/mL | 31.6 | Rats blood plasma protease | LC-MS/MS | Rats blood plasma | In Vitro | None | None | EC50(nM) = 4.68 ± 0.85 for Lixisenatide 1i (in vitro GLP-1 receptor activation potency) | |||
| 31654685 | 2019 | Off-target repebody-fused GLP-1 | 50 | Repebody | GLP-1(7-36) (A8G) fused to the off-target repebody through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis | 25 nmol/kg | 1.3 (Initial Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases | |||
| 31654685 | 2019 | Repebody-fused GLP-1 in complex with HSA | 50 | Repebody | GLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis | 25 nmol/kg | 4.2 (Initial Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases | |||
| 31654685 | 2019 | Repebody-fused GLP-1 in complex with HSA | 50 | Repebody | GLP-1(7-36) (A8G) fused to the repebody in complex with HSA through linker (A(EAAAAK)3A) at C terminus | Linear | L | None | Synthetic | Antidiabetes | Mice were euthanized at predetermined time points (n = 5 mice each at 0.05, 0.5, 1, 3, 6, 12 and 24 h post-injection) to collect whole blood from the aorta abdominalis | 25 nmol/kg | 10.7 (Terminal Half Life) | Mice plasma protease | Sandwich ELISA | Mice plasma | In Vivo | PDB id: 5VAI | None | C57BLKS/J lar- Leprdb/Leprdb mice (n = 5 per group, 6 weeks) were intravenously injected with the repebody-fused GLP-1 in complex with HSA, an off-target repebody-fused GLP-1, native GLP-1, and PBS. The blood glucose levels were analyzed at each time point for 24 h. The HSA-specific repebody-fused GLP-1 showed a significant decrease (**p < 0.005) in blood glucose level compared to other cases | |||
| 31615671 | 2019 | Free-ADI | 100 | Free | Free | Linear | L | None | Purified from the mycelia of A. nidulan | Anticancer | 20 days | 100 μl | 50.14 | Mice serum protease | HPLC | Mice serum | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 100 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Purified from the mycelia of A. nidulan | Anticancer | 20 days | 100 μl | 66.8 | Mice serum protease | HPLC | Mice serum | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31389463 | 2019 | PP18 | 49 | Free | Free | Linear | L | Ser23 linked with X3 = Structure givven in paper | OXM analogs | Antidiabetes, Antiobesity | blood was sampled pre-dose and at 0.5, 1, 2, 4, 8, 24, 48, 72, and 96 h post-dose | 30 nmoL/kg | 38.5 ± 5.9 | SD rats plasma protease | LC-MS, ELISA | SD rats plasma | In Vivo | None | None | EC50(nM) = 0.487 for Human GLP-1R | |||
| 31278957 | 2019 | Ex-(EBP)10-6xHis | 96 | Free | Ten repeats of EBP without a linker sequence, (EBP)10 fused at the C-terminus of the exenatide for Ex-(EBP)10, 6xHis tag | Linear | L | Inserting valine to the X amino acid position in the EBP (VPGXG) sequence, labeled with Flamma® 675 vinylsulfone | Fusion protein of exenatide and elastin-based polypeptide from recombinant Saccharomyces cerevisiae | Antidiabetes | The fluorescence images of the mice were measured at 0, 1, 2, 4, 8, 12, 24, 48, 72, 96, and 147 h after injection | 20 μg | 7.7 | Mouse body protease | In vivo imaging system | Mouse body | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 10 µg/kg | 5.4 ± 0.3 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 10 µg/kg | 5.8 ± 0.4 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 30 µg/kg | 5.4 ± 0.3 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 100 µg/kg | 5.2 ± 0.2 (Elimination Half Life) | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 17.4 µ/kg | 9.0 ± 1.8 (Elimination Half Life) | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 17.4 µ/kg | 11.4 ± 1.0 (Elimination Half Life) | Cynomolgus monkeys plasma protease | LC-MS/MS | Cynomolgus monkeys plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72h for intravenous | 17.4 µ/kg | 12.9 ± 1.0 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 31083740 | 2019 | SKL-18287 | 41 | Free | Amidation | Linear | L | 3H labeling at Tyr, Ser8 modification | GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein for rats, the cephalic vein for monkeys, and the jugular venous or femoral venous catheter for mini-pigs, using a heparinized syringe at 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12, 24, 48, and 72 h for subcutaneous administration | 17.4 µ/kg | 15.4 ± 0.3 (Elimination Half Life) | Göttingen minipigs plasma protease | LC-MS/MS | Göttingen minipigs plasma | In Vivo | None | None | N.A. | |||
| 35520704 | 2019 | Di-GLP-1 | 62 | Free | Bis-maleimide-NH2 | Linear | L | None | GLP-1 analogs | Antidiabetes | At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected | 50 nmol/kg | 1.8 ± 0.2 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | PDB id: 5VAI | None | EC50 = 0.039 ± 0.007 nM | |||
| 35520704 | 2019 | Lip-Di-GLP-1 | 62 | Free | Bis-maleimide-C16 conjugation at C terminal | Linear | L | None | GLP-1 analogs | Antidiabetes | At each predetermined times (1, 2, 3, 4, 6, 12, 24 and 36 h), there mice were sacrificed and ∼200 μL of blood samples were collected | 50 nmol/kg | 7.0 ± 0.7 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | PDB id: 5VAI | None | EC50 = 0.056 ± 0.018 nM | |||
| 30756483 | 2019 | ABD–Dox | 47 | Free | Dox conjugation | Linear | L | None | Derived from streptococcal protein G | Anticancer | Blood samples were collected at 40 s, 15 and 30 min, and 2, 4, 8, 24, 48, 72, and 96 h post injection | 5 mg/kg | 29.4 ± 0.8 (Elimination Half Life) | Mice plasma protease | Flurorescence assay | Mice plasma | In Vivo | None | None | (IC50) of ABD–Dox was 6.4 × 10−6 for C26 cell | |||
| 30543420 | 2019 | R2 | 53 | Free | Free | Linear | L | B-D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 0.3 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.025 ± 0.004 | |||
| 30543420 | 2019 | R2 | 53 | Free | Free | Linear | L | B-D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 7 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.025 ± 0.55 | |||
| 30543420 | 2019 | R3-01 | 53 | Free | FA-01 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | N.A. | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 4.3 ± 0.005 | |||
| 30543420 | 2019 | R3-02 | 53 | Free | FA-02 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role in Hemodynamics and Renal function and has shown preclinical efficacy in multiple disease models, including Acute Heart Failure, Fibrosis, Preeclampsia, and Corneal Wound Healing | N.A. | 0.3 mg/kg | 1 | Mouse plasma protease | LC-MS | Mouse plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.18 | |||
| 30543420 | 2019 | R3-02 | 53 | Free | FA-02 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | 1 | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.10 | |||
| 30543420 | 2019 | R3-08 | 53 | Free | FA-08 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | N.A. | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 1.5 | |||
| 30543420 | 2019 | R3-09 | 53 | Free | FA-09 | Linear | L | B-S29C,D1A Cys mutation | R3 based relaxin analogs | Role In Hemodynamics And Renal Function And Has Shown Preclinical Efficacy In Multiple Disease Models, Including Acute Heart Failure, Fibrosis, Preeclampsia, And Corneal Wound Healing | N.A. | 0.3 mg/kg | N.A. | Mouse plasma protease | LC-MS | mouse plasma | In Vivo | None | None | EC50(nM) = 0.8 | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 4°C | N.A. | 1445 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 4°C | N.A. | 2440 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 30 °C | N.A. | 23.5 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 30 °C | N.A. | 40.2 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 37°C | N.A. | 17.3 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 37°C | N.A. | 34.2 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Free-ADI | 85 | Free | Free | Linear | L | None | Isolated from Thermophilic Aspergillus nidulans | Anticancer | 45°C | N.A. | 3.4 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 6.3 ± 0.6(μmol/mg/min) in HepG-2 cells | |||
| 31615671 | 2019 | Dextran-ADI | 85 | Free | Free | Linear | L | ADI was conjugated to dextran- reactive aldehyde groups via the formation of aldimine linkage | Synthetic | Anticancer | 45°C | N.A. | 8.4 (Activity Half Life) | Mice plasma protease | Standard assay | Mice plasma | In Vivo | None | None | IC50 = 4.7 ± 0.9 (μmol/mg/min) in HepG-2 cells | |||
| 31281949 | 2019 | FUD | 49 | Free | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 0.81 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 10K PEG-FUD | 49 | 10K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 3.28 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 20K PEG-FUD | 49 | 20K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 6.77 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 40K PEG-FUD | 49 | 40K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 10.09 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | mFUD | 49 | Free | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 0.86 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 10K PEG-mFUD | 49 | 10K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 3.06 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 20K PEG-mFUD | 49 | 20K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 5.25 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 31281949 | 2019 | 40K PEG-mFUD | 49 | 40K PEG | Free | Linear | L | Sulfo-Cy5 fluorophore | Synthetic | Therapeutic candidate for disorders linked with hyperdeposition of fibronectin-modulated ECM proteins | At time points of 30 min and 1, 3, 6, 12, 24, 36, and 48 h | 12.5 mg/kg | 8.36 (Abosrption Half Life) | N.A. | Fluorescence in vivo imaging | Mice | In Vivo | https://pmc.ncbi.nlm.nih.gov/articles/PMC5705399/ | None | N.A. | |||
| 30096651 | 2018 | Analogue 6 | 80 | Free | C terminal Cys extension for bis-maleimide linkage | Linear | L | Conjugation of Palmitic acid at Lys20 (single monomer) , dimerization | Dimeric lipidated Xenopus GLP-1 analogues | Antidiabetes | At 1, 2, 3, 4, 6, 12, 24 and 48 h after injection, three Kunming mice were sacrificed at each time point and blood samples (~200 mL) were collected through extracting eyeball | 50 nmol/kg | 10.8 ± 0.8 | Kunming mice plasma protease | LC-MS/MS | Kunming mice plasma | In Vivo | None | None | EC50 = 1.4 ± 0.5 nM in HEK293 cells | |||
| 30096651 | 2018 | Analogue 6 | 80 | Free | C terminal Cys extension for bis-maleimide linkage | Linear | L | Conjugation of Palmitic acid at Lys20 (single monomer) , dimerization | Dimeric lipidated Xenopus GLP-1 analogues | Antidiabetes | Blood samples (100e150 mL) were obtained from fundus venous plexus and stored in polyethylene tubes containing heparin | 50 nmol/kg | 12.9 ± 3.6 | SD rats plasma protease | LC-MS/MS | SD rats plasma | In Vivo | None | None | EC50 = 1.4 ± 0.5 nM in HEK293 cells | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 1 µM | <0.5 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | > 4 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 3.43 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | 0.56 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 50 µM | > 4 | Rats SCT protease | LC-HRMS | 1 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 50 µM | > 4 | Rats SCT protease | LC-HRMS | 2 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | HI | 51 | Free | Free | Cyclic (3 S-S Bond) | L | None | Synthetic | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 50 µM | > 4 | Rats SCT protease | LC-HRMS | 4 mg/ml rats SCT protein | In Vitro | https://sci-hub.st/10.1016/j.jpba.2018.07.009, PDB id: 1SF1 | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | Human SCT protease | LC-HRMS | 1 mg/ml human SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | SD rats SCT protease | LC-HRMS | 1 mg/ml SD rats SCT protein | In Vitro | None | None | N.A. | |||
| 30041153 | 2018 | Lixisenatide | 44 | Free | Amidation | Linear | L | None | GLP-1 analogs | Antidiabetes | At each time point (0, 0.5, 1, 2, 4 h), 50 µL of SCts were collected from the incubation mixture | 10 µM | <0.5 | Göttingen minipigs SCT protease | LC-HRMS | 1 mg/ml göttingen minipigs SCT protein | In Vitro | None | None | N.A. | |||
| 29799205 | 2018 | 4m | 43 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 18.8 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.18 ± 0.06 | |||
| 29799205 | 2018 | 4n | 43 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 26.6 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.44 ± 0.11 | |||
| 29799205 | 2018 | 4o | 43 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 36.4 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.98 ± 0.18 | |||
| 29799205 | 2018 | 4p | 43 | Free | Free | Linear | L | X1 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 16.9 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.14 ± 0.02 | |||
| 29799205 | 2018 | 4q | 43 | Free | Free | Linear | L | X2 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 27.2 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.48 ± 0.08 | |||
| 29799205 | 2018 | 4r | 43 | Free | Free | Linear | L | X3 = structure given in paper | Xenopus GLP-1 analogs | Antidiabetes | 37°C over 72 h | 1000 ng/mL | 38.7 | Rats plasma protease | LC-MS/MS. | Rats plasma | In Vitro | None | None | EC50(nM) = 0.61 ± 0.24 | |||
| 29550018 | 2018 | DTβ4 | 88 | Free | Free | Linear | L | Dimerization using GS linker | Dimeric Tβ4 | Protects post-ischemic cardiac function | N.A. | 50 μg | 59.1 | Mouse serum protease | HPLC | Mouse serum | In Vivo | Uniprot id: P62328 | None | In scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration | |||
| 29550018 | 2018 | Tβ4 | 43 | Free | Free | Linear | L | None | Synthetic | Protects post-ischemic cardiac function | N.A. | 50 μg | 53.3 | Mouse serum protease | HPLC | Mouse serum | In Vivo | Uniprot id: P62328 | None | In scratch wound and Boyden chamber assays, the migration of HUVECs induced by DTβ4 was significantly higher than that induced by wild-type Tβ4 at each applied concentration | |||
| 29528634 | 2018 | GLP-2 analog 8 | 42 | Free | Amidation | Cyclic (C17-C24 Stapled Using Linker L3) | L | None | GLP-2 analogues | Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 2.7 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.068 ± 0.003 | |||
| 29528634 | 2018 | GLP-2 analog 9 | 42 | Free | Amidation | Cyclic (C9-C16 Stapled Using Linker L3) | L | None | GLP-2 analogues | Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 3.1 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.041 ± 0.005 | |||
| 29528634 | 2018 | GLP-2 analog 10 | 42 | Free | Amidation | Cyclic (C11-C18 Stapled Using Linker L3) | L | None | GLP-2 analogues | Efficacy in Dextran Sodium Sulfate induced Mouse Colitis Models | Plasma levels of the peptides at various time points (5 min, 30 min, 1 h, 3 h, 7 h, and 24 h) | 10 nmol/kg | 4.7 | Mice plasma protease | In vitro cell based activity assay | Mice plasma | In Vivo | None | None | EC50(nM) = 0.028 ± 0.002 | |||
| 29436835 | 2018 | PIE 12-trimer | 48 | Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 0.6 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 2.1 ± 0.28 (antiviral potency) | |||
| 29436835 | 2018 | PIE 12-trimer | 48 | Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 0.8 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 2.1 ± 0.28 (antiviral potency) | |||
| 29436835 | 2018 | Palm-PIE12-trimer | 48 | Palm-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1.2 mg/kg | 1.8 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.54 ± 0.029 (antiviral potency) | |||
| 29436835 | 2018 | Palm-PIE12-trimer | 48 | Palm-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1.2 mg/kg | 2.2 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.54 ± 0.029 (antiviral potency) | |||
| 29436835 | 2018 | C16-PIE12-trimer | 48 | C16-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 0.9 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.11 ± 0.012 (antiviral potency) | |||
| 29436835 | 2018 | C16-PIE12-trimer | 48 | C16-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 1.2 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.11 ± 0.012 (antiviral potency) | |||
| 29436835 | 2018 | C18-PIE12-trimer | 48 | C18-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 1.1 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.087 ± 0.012(antiviral potency) | |||
| 29436835 | 2018 | C18-PIE12-trimer | 48 | C18-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 1.4 | Rats plasma protease | LC-MS/MS using an Agilent HPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.087 ± 0.012(antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 1.8 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 2.7 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 1.6 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PIE12-trimer | 48 | Chol-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 3.9 | Rats plasma protease | UHPLC coupled with Quadrupole Time-of-Flight (Q-TOF) Mass Spectrometry | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.022 ± 0.0018 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PEG5k-PIE12-trimer | 48 | Chol-PEG5K-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 5.6 | Rats plasma protease | UHPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.030 ± 0.0010 (antiviral potency) | |||
| 29436835 | 2018 | Chol-PEG5k-PIE12-trimer | 48 | Chol-PEG5K-Maleimide joined by linker PEG24 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 7.2 | Rats plasma protease | UHPLC | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.030 ± 0.0010 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 5 min to 24 h | 1 mg/kg | 3.3 | Rats plasma protease | Ultra-High Performance Liquid Chromatography (UHPLC) | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | 15 min to 48 h | 1 mg/kg | 5.4 | Rats plasma protease | Ultra-High Performance Liquid Chromatography (UHPLC) | Rats plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | One ml blood samples were collected by venipuncture of a femoral vein at 0.083, 0.167, 0.25, 0.5, 1, 2, 4, 8, 16 and 24 h | 1 mg/kg | 7.4 | Male cynomolgus monkeys plasma protease | LC-MS | Male cynomolgus monkeys plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29436835 | 2018 | CPT31 | 48 | Chol-Maleimide joined by linker PEG31 | Free | Linear | Mix | All D-amino acids except Gly | Synthetic | Antiviral (HIV Entry Inhibitor) | Plasma samples were collected pre-dose and 0.25, 0.5, 1, 2, 4, 8, 16, 24, 48 and 72 h post-dose | 3 mg/kg | 18.8 | Male cynomolgus monkeys plasma protease | LC-MS | Male cynomolgus monkeys plasma | In Vivo | None | None | JRFL(nM) = 0.015 ± 0.0062 (antiviral potency) | |||
| 29391187 | 2018 | Peptide 6 | 41 | Free | ABD domain from Streptococcal G strain , Amidation | Linear | L | None | [Ser8]-GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein using a heparinised syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h postdose | 0.01 mg/kg | 5.8 ± 0.4 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC50(nM) = 1.7 | |||
| 29391187 | 2018 | Peptide 6 | 41 | Free | ABD domain from Streptococcal G strain , Amidation | Linear | L | None | [Ser8]-GLP-1 analogs | Antidiabetes | Blood samples were collected via the jugular vein using a heparinised syringe at 0.083, 0.25, 0.5, 1, 2, 4, 6, 8, 10, 12 and 24 h postdose | 0.01 mg/kg | 5.4 ± 0.3 | Rats plasma protease | LC-MS | Rats plasma | In Vivo | None | None | EC50(nM) = 1.7 | |||
| N.A. | 2018 | Example 7 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, B3E, desB27, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 44 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 10.5 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27 modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 45 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27 modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 52 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D,modifications | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 121 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Blood sample was collected at predose(-10,0),3,6,9,12,15,20,30,45,60,90,120,150,180,240,300,360,420,480,540,600 And 720 Minutes | 1 nmol/kg | 159 | Pig plasma protease | ELISA | Pig plasma | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Example 8 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27,modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 29 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 11.8 | |||
| N.A. | 2018 | Example 5 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 35 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 7.6 | |||
| N.A. | 2018 | Example 9 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, A21A, B3Q, desB27, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 30 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 16.7 | |||
| N.A. | 2018 | Example 7 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-4×gGlu), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, B3E, desB27, modififcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 30 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 10.5 | |||
| N.A. | 2018 | Example 4 | 49 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2×OEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B3E, desB27,modificaitons | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 31 | SD rats plasma protease | ELISA | SD rats plasma with zinc ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 9.3 | |||
| N.A. | 2018 | Prior Art analogue 2 | 50 | Free | B29K(N(Eps)Tetradecanedioyl-gGlu-2xOEG), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,B28D, modifcations | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 45 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Prior Art analogue 3 | 50 | Free | B29K(N(Eps)Tetradecanedioyl), desB30 modifications | Cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond, modifications | Insulin Derivative | Treatment of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 50 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| N.A. | 2018 | Example 15 | 49 | Free | B29K(N(Eps)Hexadecanedioyl-gGlu-2×OEG), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3E, desB27, modificaitons | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 67 | SD rats plasma protease | ELISA | SD rats plasma with Zinc Ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 1.8 | |||
| N.A. | 2018 | Example 23 | 49 | Free | B29K(N(Eps)Hexadecanedioyl-4×gGlu), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,A21A, B3Q, desB27, modifications | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 55 | SD rats plasma protease | ELISA | SD rats plasma with Zinc Ion | In Vivo | None | US 201615754342 A | Lipogenesis 1% HSA (%rel to HI) = 1.54 | |||
| N.A. | 2018 | Prior Art analogue 7 | 50 | Free | B29K(N(Eps)Hexadecanedioyl-gGlu), desB30 modifications | cyclic (C7-C12 disulfide bond in A chain) | L | A and B chain linked with disulfide bond,modifications | Insulin Derivative | Treatment Of Hypoglycaemia | Plasma was collected at the time points 0, 3,7,15,30,60,120,180 minutes after dosing | 25 nmol/kg | 200 | SD rats plasma protease | ELISA | SD rats plasma with 3 Zinc Ion Per Hexamer | In Vivo | None | US 201615754342 A | N.A. | |||
| 29464007 | 2018 | 99mTc-F4A | 72 | Free | Free | Cyclic (PEG2000 Linkage) | L | Tetramerization using PEG2000 | Fibrin-specific natural peptide analogue | 99mTc-F4A is a high-avidity prototype probe for characterizing thrombus in LVADs | serial blood samples were obtained at 0, 2, 5, 10, 15, 20, 30, 60, 120, and 180 min via an indwelling jugular catheter | N.A. | 5.0 ± 1.9 (T1/2A Distribution Half Life) | Mice plasma protease | Radioactivity assay | Mice plasma | In Vivo | None | None | N.A. | |||
| 28899838 | 2017 | Ghrelin(12-28)CNP(6-22)ghrelin(12-28) | 51 | Free | Ghrelin(12-28) | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 15 nmol/kg | 18.40 ± 2.05 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | Agonist activity of ghrelin(12-28)CNP(6-22)ghrelin(12-28) was also the lowest | |||
| 28899838 | 2017 | Ghrelin(28-12)CNP(6-22)ghrelin(12-28) | 51 | Reversed sequence ghrelin(28-12) fused to the N-terminal side of CNP(6-22) | Free | Cyclic (C18-C34 Disulfide Bond) | L | None | Natriuretic peptide derivatives | Treatment of Growth Failure and Short Stature Disorders such as Achondroplasia | N.A. | 16 nmol/kg | 17.38 ± 1.00 | Rats plasma protease | RIA | Rats plasma | In Vivo | None | None | Ghrelin(28-12)CNP(6-22)ghrelin(12-28) exhibited lower potency than that of ghrelin(28-12)CNP(6-22) and CNP(6-22)ghrelin(12-28) | |||
| 28464043 | 2017 | KP-54 | 54 | Free | Amidation | Linear | L | None | kisspeptin analogue | Treatment of Specific Human Reproductive Disorders | 100 μl of blood was collected from the lateral tail vein from groups of mice (n = 4) for each time point (0, 1min, 2 min, 5 min, 10 min, 30 min, 60 min and 120 min) | 1 nmol | 32 | Mouse plasma protease | RIA | Mouse plasma | In Vivo | https://www.jbc.org/article/S0021-9258(19)77047-1/fulltext | None | N.A. | |||
| 28457895 | 2017 | Exenatide-APTHSA | 83 | Free | C-terminal part of exenatide was connected to the N-terminal part of APTHSA using a long (18-mer) linker | Linear | L | None | Exendin-4 analogs | Antihyperglycemic | 1 hour | 25 nmol/kg | ~1.3 | ICR mice retro-orbital sinus protease | Exenatide ELISA | ICR mice retro-orbital sinus | In Vivo | PDB id: 7MLL | None | both exenatide and exenatide-APTHSA groups at an equal dose effectively cleared glucose from the bloodstream, showing similar anti-hyperglycemic activity | |||
| 27115755 | 2016 | HSA-dTMP | 63 | HSA joined using a linker | Free | Linear | L | None | Fusion protein of dTMP and HSA | Treatment of Thrombocytopenia | Serum was sampled from mice eyes at 5 min, 30 min, 1 h,1.5 h, 2 h, 4 h, 12 h, 24 h, and 48 h after dosing | 300 μg/kg | 17.1 | Mice serum protease | Immunoenzymetric assay | Mice serum | In Vivo | None | None | both HSA-dTMP and dTMP-HSA could significantly increase peripheral platelet counts in a dose-dependent manner in normal mice | |||
| 27115755 | 2016 | dTMP-HSA | 63 | Free | HSA joined using a linker | Linear | L | None | Fusion protein of dTMP and HSA | Treatment of Thrombocytopenia | Serum was sampled from mice eyes at 5 min, 30 min, 1 h,1.5 h, 2 h, 4 h, 12 h, 24 h, and 48 h after dosing | 300 μg/kg | 16.1 | Mice serum protease | Immunoenzymetric assay | Mice serum | In Vivo | None | None | both HSA-dTMP and dTMP-HSA could significantly increase peripheral platelet counts in a dose-dependent manner in normal mice | |||
| 28989813 | 2016 | 54.6 kDa EG9 | 43 | Free | AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(54.6KDa) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-4 analogs | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 42.4 ± 2.9 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50(nM) = 1.91 ± 0.35 | |||
| 28989813 | 2016 | 55.6 kDa EG3 | 43 | Free | AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(55.6KDa) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-4 analogs | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 61.2 ± 5.0 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50(nM) = 4.17 ± 0.13 | |||
| 28989813 | 2016 | 71.6 kDa EG3 | 43 | Free | AEBMP: N-(2-(2-(2-(2-aminoacetamido)acet-amido)acetamido) ethyl)-2-bromo-2-methylpropanamide, OEGMA(71.6KDa) | Linear | L | Fluorescently labeled with Alexa Fluor | Exendin-4 analogs | Antidiabetes | 10 μL of blood samples were collected from the tail vein into 100 μL of a heparin solution (1kU/ml in PBS, Sigma Aldrich) at 40 s, 40 min, 2.5 h, 4.5 h, 8 h, 24 h, 48 h, 72 h, 96 h and 120 h after injection | 75 nmol/kg | 61.5 ± 3.2 (T1/2 Elimination Half Life) | Mice plasma protease | Fluorescence assay | Mice plasma | In Vivo | None | None | EC50(nM) = 5.11 ± 0.23 | |||
| 138-792-131-275-411 | 2017 | HRS (1-60) | 67 | Free | Free | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 0.5 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 138-792-131-275-411 | 2017 | HRS (1-60) | 67 | Free | Free | Linear | L | None | Synthetic | Therapeutic | 1.5 hr | 8 mg/kg | 0.7 | NA | ELISA | mice | in vivo | https://lens.org/138-792-131-275-411 | US 9587235 B2 | NA | |||
| 159-909-893-044-968 | 2017 | adrenomedullin | 44 | lipid | free | Linear | D | None | human adrenomedullin peptide | agonistic | NA | NA | 1.5 | NA | ELISA | SHR rat | in vivo | https://lens.org/159-909-893-044-968 | US 9694051 B2 | NA | |||
| 034-343-155-162-302 | 2017 | Ex4 | 87 | Free | Free | Linear | L | None | NA | NA | NA | NA | 38 | chymotrypsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA | |||
| 034-343-155-162-302 | 2017 | exenatide | 87 | Free | Free | Linear | L | None | NA | NA | NA | NA | 13 | pepsin | ELISA | NA | in vitro | https://lens.org/034-343-155-162-302 | US 9695224 B2 | NA |