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Retatrutide (LY3437943) acetate is a triple agonist peptide for the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R).

Retatrutide acetate inhibits human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM, respectively. It exhibits activity on mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191, and 0.794 nM, respectively.

In vivo, Retatrutide (LY3437943) acetate engages with GCGR and enhances glucose tolerance in an ipGTT by acting through GIP or GLP-1 receptors. Activation via the glucagon receptor by Retatrutide acetate leads to significant weight reduction and increased energy expenditure. Retatrutide acetate can be utilized in research related to obesity.