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AP3 is a GPR40 AgoPAM (Agonist/Positive Allosteric Modulator) small molecule developed by Merck & Co., Inc. as a potential oral antidiabetic therapeutic for type 2 diabetes. It functions by stimulating both insulin and incretin (GLP-1, GIP, PYY) secretion, leading to glucose lowering and body weight reduction. Uniquely, AP3 also causes a significant and sustained increase in glucagon secretion, a target-mediated effect requiring the GPR40 receptor. Its mechanism involves both direct stimulation of beta cells and indirect effects through GLP-1 secretion, contributing to enhanced glucose-dependent insulin secretion.
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