Retatrutide acetate (LY3437943) is a peptide and triple agonist for the glucagon receptor (GCGR), glucose-dependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R), exhibiting potent inhibitory effects on human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM respectively; it is utilized in obesity research [1].

Retatrutide acetate (LY3437943) exhibits activity against human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM, respectively [1]. In mice, the EC50 values are 2.32, 0.191, and 0.794 nM [1]. Additionally, retatrutide acetate demonstrates binding affinity to the human receptors with Ki values of 5.6, 0.057, and 7.2 nM [1], and to the mouse receptors with Ki values of 73, 2.8, and 1.3 nM [1].

Retatrutide (LY3437943) acetate, administered subcutaneously at a dosage of 0.47 mg/kg in a single injection, engages the GCGR and is capable of improving glucose tolerance in the ipGTT through interaction with GIP or GLP-1 receptors [1]. Additionally, when given at 10 mL/kg every third day over a 21-day period, Retatrutide acetate significantly reduces body weight and increases energy expenditure via the activation of the glucagon receptor [1]. Retatrutide acetate has been found to be safe and well-tolerated [1].