Sitagliptin phosphate monohydrate ≥ 99% by HPLC

Sitagliptin phosphate monohydrate (MK-0431) is a highly selective, orally active dipeptidyl peptidase-4 (DPP-4) inhibitor (IC50 = 18 nM; >2,600-fold selectivity over DPP-8/9) that functions via reversible, competitive inhibition of the enzyme′s catalytic active site. By preventing the proteolytic inactivation of incretins (GLP-1 and GIP) with high specificity, MK-0431 achieves >90% DPP-4 inhibition within 2 hours (sustained ~80% at 24 hours), thereby enhancing glucose-dependent insulin secretion and suppressing glucagon. This pharmacodynamic profile yields a weight-neutral antidiabetic option with additive glycemic efficacy in combination with metformin or pioglitazone, while maintaining a significantly lower risk of hypoglycemia compared to sulfonylureas. Uniquely, Sitagliptin simultaneously targets hyperglycemia and systemic inflammation; it addresses metabolic syndrome-associated inflammation by suppressing intranuclear NF-κB binding and downregulating critical mediators (JNK-1, IKKβ, TLR-4, CCR-2), demonstrating distinct anti-atherogenic potential alongside metabolic control.

Hygroscopic, Store with desiccant