SAR441255 is a peptide triple agonist of the glucagon-like peptide 1 receptor (GLP-1R), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon receptor (GCGR).1 It induces cAMP accumulation in HEK293 cells expressing human GLP-1R, GIPR, or GCGR (EC50s = 1.03, 0.73, and 1.01 pM, respectively). SAR441255 (1-30 ?g/kg) reduces body weight in a mouse model of high-fat diet-induced obesity. It also reduces body weight and blood hemoglobin A1c (HbA1c) levels in high-fat diet-induced obese diabetic cynomolgus monkeys when administered at a dose of 11 ?g/kg.
References:
[1]. Bossart, M., Wagner, M., Elvert, R., et al.Effects on weight loss and glycemic control with SAR441255, a potent unimolecular peptide GLP-1/GIP/GCG receptor triagonistCell Metab.34(1)59-74(2022).
















