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Sitagliptin | DPP-IV/DPP-4 inhibitor

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Catalog #:

Product Description

Sitagliptin (also named MK-0431 and marketed as Januvia) is a competitive inhibitor of the enzyme dipeptidyl peptidase 4 (DPP-4). Sitagliptin can increase incretin levels (GLP-1 and GIP), which inhibit glucagon release, which in turn increases insulin secretion, decreases gastric emptying, and decreases blood glucose levels.

Technical information:

Chemical Formula:   C16H15F6N5O
CAS #:   486460-32-6
Molecular Weight:   407.31
Purity:   >98%
Appearance:   White solid
Chemical Name:   (3R)-3-Amino-1-[3-(trifluoromethyl)-5,6,7,8-tetrahydro-1,2,4-triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one
Solubility:   Up to 100 mM in DMSO

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Herman GA, et al.Pharmacokinetics and pharmacodynamics of sitagliptin, an inhibitor of dipeptidyl peptidase IV, in healthy subjects: results from two randomized, double-blind, placebo-controlled studies with single oral doses. Clin Pharmacol Ther 2005; 78 (6): 675–88.
2. Herman GA, et al. Pharmacokinetics and pharmacodynamic effects of the oral DPP-4 inhibitor sitagliptin in middle-aged obese subjects. J Clin Pharmacol 2006;46 (8): 876–86.
3. Lee B, et al. Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. Eur J Pharmacol. 2008;589(1-3):306-14

Other Information:

Product Specification (pdf)
MSDS (pdf)

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