2749855-96-5

(±)-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.1 (–)-Sitagliptin is a potent inhibitor of DPP-4 (IC50 = 18 nM).2 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.2,3 (–)-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.4 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.WARNING This product is not for human or veterinary use.

[1] De Souza, F.I., Zumiotti, A.V., and Da Silva, C.F. Neuregulins 1-α and 1-β on the regeneration the peripheral nerves[J]. Acta Ortop Bras.
[2] TESFAYE BIFTU  et al. et al. (3R)-4-[(3R)-3-Amino-4-(2,4,5-trifluorophenyl)butanoyl] -3-(2,2,2-trifluoroethyl)-1,4-diazepan-2-one, a Selective Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes.[J]. ChemInform, 2007, 38 20. DOI: 10.1002/chin.200720205
[3] DOOSEOP KIM . Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIA™ (sitagliptin phosphate)[J]. Bioorganic & Medicinal Chemistry Letters, 2007, 17 12: Pages 3373-3377. DOI: 10.1016/j.bmcl.2007.03.098
[4] MD B A, (PROFESSOR) P. DPP-4 inhibitors[J]. Best practice & research. Clinical endocrinology & metabolism, 2007, 21 4: Pages 517-533. DOI: 10.1016/j.beem.2007.07.005