Sitagliptin phosphate

SKU: orb1305654

Description

Sitagliptin phosphate is a selective DPP-4 inhibitor used in diabetes research. It is widely applied in both in vitro enzymatic assays and in vivo models to study glycemic control and beta-cell function.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 654671-78-0
• MW: 505.31
• Purity: 99.91% (May vary between batches)
• Formula: C₁₆H₁₈F₆N₅O₅P
• SMILES: N[C@@H](CC(N1Cc2nnc(C(F)(F)F)n2CC1)=O)Cc(c(F)c1)cc(F)c1F.OP(O)(O)=O
• Target: Autophagy,DPP-4
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.96 mM);DMSO:50 mg/mL (98.95 mM)

Bioactivity

• Target IC50:
  DPP4:19 nM
• 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.
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• 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 .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, DPP, DPP4, DPP-4, Dipeptidyl Peptidase, Inhibitor, Januvia, inhibit, MK0431, MK-0431, MK0431 Phosphate, MK-0431 phosphate, MK-0431 Phosphate, MK 0431, MK 0431 Phosphate, Sitagliptin, Sitagliptin (phosphate), Sitagliptin Phosphate, Sitagliptin phosphate

Compound Identifiers

PubChem CID

6451150