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.
Reference:
| 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)
