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Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
50 mg | $33 | In Stock | |
100 mg | $47 | In Stock | |
200 mg | $57 | In Stock | |
500 mg | $94 | In Stock | |
1 mL x 10 mM (in DMSO) | $52 | In Stock |
Description | Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor. |
Targets&IC50 | DPP4:19 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 [1]. |
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 [1]. 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[2]. |
Alias | Sitagliptin (phosphate), MK-0431 phosphate, Januvia |
Molecular Weight | 505.31 |
Formula | C16H18F6N5O5P |
Cas No. | 654671-78-0 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (98.95 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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