Sitagliptin phosphate is a dipeptidyl peptidase-4 (DPP4) inhibitor.
| Pack Size | Availability | Price/USD | Quantity |
|---|---|---|---|
| 100 mg | Inquiry | $ 102 | |
| 200 mg | Inquiry | $ 183 | |
| 400 mg | Inquiry | $ 274 | |
| 1 g | Inquiry | $ 552 | |
| 2 g | Inquiry | $ 861 |
| Description | Sitagliptin phosphate is a dipeptidyl peptidase-4 (DPP4) inhibitor. |
| Targets&IC50 | DPP-4:19 nM |
| In vitro | In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM. Sitagliptin inhibited DPP-8 (IC50: 48 μM). Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and aminopeptidase P . |
| In vivo | In free-fed Han-Wistar rats, the ED50 values ??for the inhibition of plasma DPP-4 activity by sitagliptin phosphate were calculated as 7 hours post-dose at 2.3 mg/kg and 24 hours post-dose at 30 mg/kg . A mouse model of streptozotocin-induced type 1 diabetes showed elevated plasma DPP-4 levels, which was significantly suppressed in mice on a sitagliptin phosphate diet. This is achieved through a positive effect on hyperglycemia regulation, possibly by prolonging islet graft survival. The plasma clearance and volume of distribution of sitagliptin phosphate in rats (40-48 mL/min/kg, 7-9 L/kg) were higher than those in dogs (9 mL/min/kg, 3 L/kg); its The half-life is shorter in rats, 2 hours in dogs and 4 hours in dogs. |
| Synonyms | Januvia, Sitagliptin (phosphate), MK-0431 phosphate |
| CAS No. | 654671-78-0 |
| Chemical Formula | C16H18F6N5O5P |
| Molecular Weight | 505.314 |
| Solubility | DMSO: 25 mg/mL(49.47 mM) |
| Storage | Powder: -20°C for 2 years In solvent: -80°C for 1 year |
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