N-(3-Cyano-6-(1,1-dimethylpropyl)-4,5,6,7-tetrahydro-1-benzothien-2-yl)-2-ethylbutanamide hGCGR Antagonist White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable thienyl-amide compound that acts as a potent, selective, and competitive antagonist of the glucagon receptor. Shown to bind to hGCGR with high affinity and prevent its interaction with glucagon (IC50 = 181 nM, KDB = 81 nM, and pA2 = 7.1 in membranes prepared from CHO-hGCGR). Also suppresses glucagon-induced glycogenolysis in human primary hepatocytes and in mice (50 mg/kg, ip). Purity: ≥95% by HPLC. CAS 438618-32-7. Ref.: Qureshi, S.A., et al. 2004. Diabetes 53, 3267. |