| Name | Sitagliptin phosphate |
| Description | Sitagliptin phosphate (MK-0431 phosphate) is a dipeptidyl peptidase-4 (DPP4) inhibitor. |
| 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]. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.96 mM), Sonication is recommended.
DMSO : 50 mg/mL (98.95 mM), Sonication is recommended.
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| Keywords | Sitagliptin Phosphate | Sitagliptin phosphate | Sitagliptin | MK-0431 Phosphate | MK0431 Phosphate | MK-0431 | MK0431 | MK 0431 Phosphate | MK 0431 | Inhibitor | inhibit | DPP-4 | DPP4 | DPP | Dipeptidyl Peptidase | Autophagy |
| Inhibitors Related | Stavudine | Aceglutamide | Cysteamine hydrochloride | Sodium 4-phenylbutyrate | Hydroxychloroquine | Guanidine hydrochloride | Curcumin | Valproic Acid | Paeonol | Naringin | Alginic acid | Gefitinib |
| Related Compound Libraries | FDA-Approved & Pharmacopeia Drug Library | Failed Clinical Trials Compound Library | Bioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | FDA-Approved Drug Library | Metabolism Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
