Tolbutamide-d9 is intended for use as an internal standard for the quantification of tolbutamide by GC- or LC-MS. Tolbutamide is an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.9 µM).1 It is selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 85 and 88 µM, respectively). Tolbutamide increases glucose-induced insulin secretion and calcium influx in isolated mouse pancreatic islets.2 In vivo, tolbutamide (80 mg/kg) reduces blood glucose levels in a mouse model of diabetes induced by streptozotocin .3 Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.
1.Proks, P., Reimann, F., Green, N., et al.Sulfonylurea stimulation of insulin secretionDiabetes51(3)S368-S376(2002) 2.Ishiyama, N., Ravier, M.A., and Henquin, J.-C.Dual mechanism of the potentiation by glucose of insulin secretion induced by arginine and tolbutamide in mouse isletsAm. J. Physiol. Endocrinol. Metab.290(3)E540-E549(2006) 3.Rerup, C., and Tarding, F.Streptozotocin- and alloxan-diabetes in miceEur. J. Pharmacol.7(1)89-96(1969)