Retatrutide sodium salt is a potent triple agonist peptide for glucagon receptor (GCGR), glucose-dependent proinsulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R) Retatrutide sodium salt is used in the study of type 2 diabetes and obesity.

GIPR:0.191 nM (EC50, mouse), GIPR:0.0643 nM (EC50, human), GLP1R:0.794 nM (EC50, mouse), GLP1R:0.775 nM (EC50, human), GCGR:5.79 nM (EC50, human), GCGR:2.32 nM (EC50, mouse)

Retatrutide sodium salt exhibits activity against human GCGR, GIPR, and GLP-1R, with EC50 values of 5.79, 0.0643, and 0.775 nM, respectively[1].
In mouse models, Retatrutide sodium salt demonstrates activity against GCGR, GIPR, and GLP-1R, with EC50 values of 2.32, 0.191, and 0.794 nM, respectively[1].
The binding affinities of Retatrutide sodium salt for human GCGR, GIPR, and GLP-1R are characterized by Ki values of 5.6, 0.057, and 7.2 nM, respectively[1].
For mouse GCGR, GIPR, and GLP-1R, Retatrutide sodium salt exhibits binding affinities with Ki values of 73, 2.8, and 1.3 nM, respectively[1].

Retatrutide sodium salt, administered via subcutaneous injection at a single dose of 0.47 mg/kg, engages with the glucagon receptor (GCGR) in vivo and improves glucose tolerance in an intraperitoneal glucose tolerance test (ipGTT) through activation of GIP or GLP-1 receptors[1].
With subcutaneous injections at a dose of 10 mL/kg every 3 days for a cycle of 21 days, Retatrutide sodium salt induces significant weight loss and increased energy expenditure through activation of the glucagon-like peptide-1 (GLP-1) receptor[1].
Retatrutide sodium salt demonstrates safety and tolerability in these studies[1].