产品描述:
Orforglipron is a nonpeptide agonist of the glucagon-like peptide 1 receptor (GLP-1R).{66609} It induces cAMP accumulation in HEK293 cells expressing human GLP-1R (EC50 = 3.05 nM) and is selective for GLP-1R over the glucagon receptor (GCGR), gastric inhibitory polypeptide (GIP) receptor, and GLP-2R at 100 nM. Orforglipron (0.1, 1, or 10 mg/kg) prevents increases in blood glucose levels in glucose-injected fasted mice expressing human GLP-1R but not in glucose-injected Glp1r-/- fasted mice. In vivo, orforglipron (5.4 mg/kg) decreases blood glucose and serum insulin levels in glucose-injected cynomolgus monkeys. It reduces mean food intake in cynomolgus monkeys when administered at doses of 0.05 or 0.1 mg/kg per day.