Tolbutamide

Tolbutamide is an inhibitor of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (IC50 = 4.9 µM). 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. In vivo, tolbutamide (80 mg/kg) reduces blood glucose levels in a mouse model of diabetes induced by streptozotocin (STZ, Cay-13104). Formulations containing tolbutamide have been used in the treatment of type 2 diabetes.Formal Name: N-[(butylamino)carbonyl]-4-methyl-benzenesulfonamide. CAS Number: 64-77-7. Synonyms: D 860, NSC 23813, NSC 87833, U-2043. Molecular Formula: C12H18N2O3S. Formula Weight: 270.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 30 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS (pH 7.2) (1:6): 0.14 mg/mL. lambdamax: 229 nm. SMILES: CC1=CC=C(S(NC(NCCCC)=O)(=O)=O)C=C1. InChi Code: InChI=1S/C12H18N2O3S/c1-3-4-9-13-12(15)14-18(16,17)11-7-5-10(2)6-8-11/h5-8H,3-4,9H2,1-2H3,(H2,13,14,15). InChi Key: JLRGJRBPOGGCBT-UHFFFAOYSA-N.