| Name | Gosogliptin |
| 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] |
| 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.
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| Keywords | PF 734200 | PF 00734200 | Gosogliptin | DPP-IV |
| Inhibitors Related | Trelagliptin | Trelagliptin succinate | Sitagliptin | Saxagliptin hydrate | Teneligliptin hydrobromide | Sitagliptin phosphate monohydrate | Picolamine | Anagliptin | Linagliptin | Vildagliptin | Saxagliptin | Sitagliptin phosphate |
United States
