Repaglinide-d5 is intended for use as an internal standard for the quantification of repaglinide by GC- or LC-MS. Repaglinide is a metaglitinide antidiabetic agent that blocks ATP-dependent potassium (Kir6) channels in pancreatic β-cells (Kd = 0.42 nM for the sulphonylurea receptor SUR1 when co-expressed with Kir6.2).1 In vivo, repaglinide lowers blood glucose in fasted rats and dogs (ED50s = 10 and 28.3 μg/kg, respectively).2 Formulations containing repaglinide have been used to control blood sugar levels in patients with type 2 diabetes.
1.Hansen, A.M.K., Hansen, J.B., Carr, R.D., et al.Kir6.2-dependent high-affinity repaglinide binding to β-cell KATP channelsBr. J. Pharmacol.144(4)551-557(2005) 2.Mark, M., and Grell, W.Hypoglycaemic effects of the novel antidiabetic agent repaglinide in rats and dogsBr. J. Pharmacol.121(8)1597-1604(1997)