Trelagliptin-13C-d3 is intended for use as an internal standard for the quantification of trelagliptin by GC- or LC-MS. Trelagliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 4 nM).1 It is greater than 10,000-fold selective for DPP-4 over isopeptidases. Trelagliptin (7 mg/kg) inhibits plasma DPP-4 activity and reduces postprandial plasma insulin levels in Zucker fa/fa rats. Formulations containing trelagliptin have been used in the treatment of type 2 diabetes mellitus.
1.Kushwaha, R.N., Haq, W., and Katti, S.B.Discovery of 17 gliptins in 17-years of research for the treatment of type 2 diabetes: A synthetic overviewChemistry and Biology Interface4(3)137-162(2014)