(+-)-Sitagliptin-d4 (hydrochloride)

(+-)-Sitagliptin-d4 is intended for use as an internal standard for the quantification of sitagliptin by GC- or LC-MS. Sitagliptin is a mixture of the dipeptidyl peptidase 4 (DPP-4) inhibitor (-)-sitagliptin (Item No. 13252) and (+)-sitagliptin, also known as sitagliptin impurity E, a potential impurity found in commercial preparations of (-)-sitagliptin.{39742} (-)-Sitagliptin is a potent inhibitor of DPP-4 (IC50 = 18 nM).{26165} It is selective for DPP-4 over DPP-8 (IC50 = 48 µM) as well as several other peptidases, including DPP-9, DPP-2, and amino peptidase P.{26165,26164} (-)-Sitagliptin improves glucose tolerance in insulin-resistant Zucker fatty and high-fat diet fed rats as well as ob/ob and high-fat diet fed mice.{26071} It also reduces hyperglycemia in mice fed a high-fat diet with diabetes induced by streptozotocin (Item No. 13104). Formulations containing (-)-sitagliptin have been used in the treatment of type 2 diabetes mellitus.