|Description||LY3437943 is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). LY3437943 inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. LY3437943 can be used for the research of obesity.|
Research Areas >> Metabolic Disease
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).
|In Vitro||LY3437943 has inhibition for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. LY3437943 has inhibition for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively. LY3437943 has binding affinity for human GCGR, GIPR, and GLP-1R with Ki values of 5.6, 0.057 and 7.2 nM, respectively. LY3437943 has binding affinity for mouse GCGR, GIPR, and GLP-1R with Ki values of 73, 2.8 and 1.3 nM, respectively.|
|In Vivo||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. LY3437943 (s.c.; 10 mL/kg; cycle every 3 days; for 21 days) causes great body weight loss and increases energy expenditure through glucagon receptor activatio. LY3437943 has safety and tolerability. Animal Model: Male CD-1 mice Dosage: 0.47 mg/kg Administration: Subcutaneous administration, single Result: AUClast, ng*h/mL AUC0-∞, ng*h/mL Cmax, ng/mL Tmax, h t1/2, 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.|
. Tamer Coskun, et al. LY3437943, a novel triple glucagon, GIP, and GLP-1 receptor agonist for glycemic control and weight loss: From discovery to clinical proof of concept. Cell Metab. 2022 Sep 6;34(9):1234-1247.e9.