(rel)-AM-6226

(rel)-AM-6226 is the relative stereoisomer of AM-6226 (HY-120493A). AM-6226 is a potent, orally active full agonist of G protein-coupled receptor 40 (GPR40) with an EC₅₀ value of 0.12 μM. AM-6226 activates GPR40 receptors on pancreatic β-cells and enteroendocrine L-cells, promotes insulin secretion in a glucose-dependent manner, and increases the release of incretin hormones (GLP-1, GIP), thus avoiding the risk of hypoglycemia. AM-6226 can be used in the research of metabolic diseases such as diabetes^[1]. In Vitro:AM-6226 (Compound 14) acts as a potent full agonist of GPR40 in transfected CHO cells with low GPR40 expression, with an EC₅₀ of 0.12 μM and a potency of 104% relative to AM-1638^[1]. In Vivo:AM-6226 (0.1-10 mg/kg; p.o.; single dose) significantly reduces plasma glucose levels in prediabetic cynomolgus monkeys during the oral glucose tolerance test (OGTT), with an 18% decrease in plasma glucose AUC_0-t at the 10 mg/kg dose^[1].