Retatrutide (C007B-415662)

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). Specification: 0.99 Molecular Formula: C221H342N46O68 Molecular Weight: 4731.33