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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 | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $132 | - | In Stock | |
| 5 mg | $328 | - | In Stock | |
| 10 mg | $529 | - | In Stock | |
| 25 mg | $1,090 | - | In Stock | |
| 50 mg | $1,780 | - | In Stock | |
| 100 mg | $2,380 | - | 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] |
| Synonyms | 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 |
| Color | White |
| Appearance | Solid |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 80 mg/mL (218.33 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (13.65 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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