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Discover high-quality research tools to investigate GLP-1 mechanisms and next-generation metabolic targets.
OBESITY RESEARCH SOLUTIONSTolbutamide 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 (STZ; Item No. 13104).3 Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.
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1. Sulfonylurea stimulation of insulin secretion. Diabetes 51(3), S368-S376 (2002).
2. Dual mechanism of the potentiation by glucose of insulin secretion induced by arginine and tolbutamide in mouse islets. Am. J. Physiol. Endocrinol. Metab. 290(3), E540-E549 (2006).
3. Streptozotocin-