Description
Retatrutide (LY3437943) is a triple agonist peptide of the Glukagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and Glukagon-like peptide-1 receptor (GLP-1R). Retatrutide inhibits human GCGR, GIPR, and GLP-1R with EC 50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide can be used for the research of obesityIn VitroRetatrutide (LY3437943) has efficacy for human GCGR, GIPR, and GLP-1R with EC 50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide has efficacy for mouse GCGR, GIPR, and GLP-1R with EC 50 values of 2.32, 0.191 and 0.794 nM, respectively. Retatrutide has binding affinity for human GCGR, GIPR, and GLP-1R with K i values of 5.6, 0.057 and 7.2 nM, respectively. Retatrutide has binding affinity for mouse GCGR, GIPR, and GLP-1R with K i values of 73, 2.8 and 1.3 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoRetatrutide (LY3437943) (s.c.; 0.47 mg/kg; single) engages GCGR in vivo and can improve glucose tolerance in an ipGTT through either the GIP or GLP-1 receptors. Retatrutide (s.c.; 10 mL/kg; cycle every 3 days; for 21 days) causes great body weight loss and increases energy expenditure through Glukagon receptor activatio. Retatrutide has safety and tolerability. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male CD-1 mice Dosage: 0.47 mg/kg Administration: Subcutaneous administration, single Result: AUC last, ng*h/mL AUC 0-∞, ng*h/mL C max, ng/mL T max, h t 1/2, h CLF, mL/h/kg 41135 41905 1680 12 21 11.22 Animal Model: Diet-induced obese (DIO) male C57/Bl6 mice (24-25 weeks, 40-51 g) Dosage: 10 mL/kg Administration: Subcutaneous (SC) injection, cycle every 3 days, for 21 days Result: Decreased body weight and improved glycemic control.Form:SolidIC50& Target:EC50 (for human): 5.79 (GCGR), 0.0643 (GIPR), 0.775 nM (GLP-1R),EC50 (for mouse): 2.32 (GCGR), 0.191 (GIPR), 0.794 nM (GLP-1R),Ki (for human): 5.6 (GCGR), 0.057 (GIPR), 7.2 nM (GLP-1R),Ki (for mouse): 73 (GCGR), 2.8 (GIPR), 1.3 nM (GLP-1R)