T0242

Sitagliptin (MK0431), a new oral hypoglycemic (anti-diabetic drug), is a new dipeptidyl peptidase-4 (DPP-4) inhibitor. This enzyme-inhibiting drug is used either alone or in combination with metformin or thiazolidinedione for treatment of type 2 diabetes mellitus. The drug can competitively inhibit a protein/enzyme and DPP-4, that leads to an incremental amount of active incretins (GLP-1 and GIP), the diminished amount of release of glucagon and increased release of insulin.

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) is a potent DPP-IV inhibitor with an IC50 of 19 nM in Caco-2 cell extracts.

5-Hydroxy saxagliptin-13C,d2-2 hydrochloride is a 13C and deuterium-labeled version of 5-Hydroxy saxagliptin hydrochloride. The latter is an active metabolite of Saxagliptin that functions as a potent and selective DPP-4 inhibitor. It exhibits Ki values of 2.6 nM in humans and 2.9 nM in cynomolgus monkeys. This compound is utilized in the study of type 2 diabetes.