1219794-57-6

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 K_ir6.2 (IC₅₀ = 4.9 μM). It is selective for SUR1/K_ir6.2 over SUR2A/K_ir6.2 and SUR2B/K_ir6.2 channels (IC₅₀s = 85 and 88 μM, respectively). Tolbutamide increases glucose-induced insulin secretion and calcium influx in isolated mouse pancreatic islets. In vivo, tolbutamide (80 mg/kg) reduces blood glucose levels in a mouse model of diabetes induced by streptozotocin (STZ; ). Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.

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Labelled Tolbutamide (T535150). An antidiabetic, used as a hypoglycemic agent in veterinary medicine.

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