Glucagon Receptor Antagonist I is a potent and selective cell-permeable thienyl-amide compound that acts as a competitive antagonist of the glucagon receptor. Exhibits binding to hGCGR with high affinity and prevents 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).
