Tolazamide

Tolazamide is a first generation sulfonylurea that inhibits sulfonylurea receptor 1 (SUR1) linked to the inwardly rectifying potassium channel (KIR6.2, IC50 = 4.2 µM in HEK293 cells transfected with the human receptor). It has no effect on glucose uptake in L6 rat skeletal muscle cells when used at a concentration of 0.6 mg/mL but enhances glucose uptake two-fold when used in combination with insulin. In vivo, tolazamide (128 mg/kg) reduces glomerulosclerosis and albumin excretion in a rat model of insulin-dependent diabetes induced by streptozotocin (Cay-13104). Formulations containing tolazamide have been used in the treatment of type 2 diabetes.Formal Name: N-[[(hexahydro-1H-azepin-1-yl)amino]carbonyl]-4-methyl-benzenesulfonamide. CAS Number: 1156-19-0. Synonyms: NSC 70762. Molecular Formula: C14H21N3O3S. Formula Weight: 311.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 0.25 mg/ml. lambdamax: 229 nm. SMILES: CC1=CC=C(S(NC(NN2CCCCCC2)=O)(=O)=O)C=C1. InChi Code: InChI=1S/C14H21N3O3S/c1-12-6-8-13(9-7-12)21(19,20)16-14(18)15-17-10-4-2-3-5-11-17/h6-9H,2-5,10-11H2,1H3,(H2,15,16,18). InChi Key: OUDSBRTVNLOZBN-UHFFFAOYSA-N.