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Gosogliptin is a potent, orally active, highly selective and competitive inhibitor of DPP-4 (dipeptidyl peptidase 4), increasing the levels of intestinal glucagon peptide (GLP-1) and glucose-dependent proinsulinotropic polypeptide (GIP), thereby enhancing insulin secretion and lowering blood glucose levels. In animal studies, Gosogliptin rapidly, orally and reversibly inhibits plasma DPP-4 activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $139 | In Stock | |
5 mg | $347 | In Stock | |
10 mg | $556 | In Stock | |
25 mg | $1,160 | In Stock | |
50 mg | $1,870 | In Stock | |
100 mg | $2,500 | In Stock |
Description | Gosogliptin is a potent, orally active, highly selective and competitive inhibitor of DPP-4 (dipeptidyl peptidase 4), increasing the levels of intestinal glucagon peptide (GLP-1) and glucose-dependent proinsulinotropic polypeptide (GIP), thereby enhancing insulin secretion and lowering blood glucose levels. In animal studies, Gosogliptin rapidly, orally and reversibly inhibits plasma DPP-4 activity. |
In vitro | Gosogliptin (PF-00734200) is a potent, oral, selective, and competitive DPP-IV inhibitor that rapidly and reversibly inhibits plasma DPP-4 activity when administered orally to rats, dogs, and monkeys.[2] |
In vivo | Methods: Gosogliptin (PF-00734200) was administered (orally) to intact SD rats (5 mg/kg), beagle dogs (5 mg/kg), and humans (20 mg) to investigate metabolism, pharmacokinetics, and excretion in Dawley (SD) rats, beagle dogs, and humans. Results: Gosogliptin recovered a mean of 97.1% of the administered radioactivity in urine, feces, and cage wash fluids within 168 hours after dosing. The mean cumulative dose recovered in feces was 66.0%. The mean cumulative excretion in urine was 30.8%. Approximately 95% of the excreted radioactivity was recovered within the first 48 hours. [2] |
Alias | PF-734200, PF734200, PF-00734200, PF00734200 |
Molecular Weight | 366.41 |
Formula | C17H24F2N6O |
Cas No. | 869490-23-3 |
Smiles | C(=O)([C@@H]1C[C@@H](CN1)N2CCN(CC2)C=3N=CC=CN3)N4CC(F)(F)CC4 |
Relative Density. | 1.36 g/cm3 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 80 mg/mL (218.33 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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