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Retatrutide 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 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.

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