| Retatrutide (LY3437943) is a triple agonist of the glucagonreceptor, glucose-dependent insulinotropic polypeptide receptor,and glucagon-like peptide-1 receptor (GLP-1R), and inhibits GCGR,GIPR, and GLP-1R.Retatrutide can be used to study obesity. | |
| 靶点活性 | GIPR:0.0643 nM (EC50, human), GIPR:0.057 nM (Ki, human),GLP1R:0.794 nM (EC50, mouse), GIPR:2.8 nM (Ki, mouse), GCGR:5.79 nM(EC50, human), GCGR:2.32 nM (EC50, mouse), GCGR:73 nM (Ki, mouse),GLP1R:7.2 nM (Ki, human), GIPR:0.191 nM (EC50, mouse), GLP1R:1.3 nM(Ki, mouse), GCGR:5.6 nM (Ki, human), GLP1R:0.775 nM (EC50,human) |
| 体外活性 | Retatrutide (LY3437943) exhibits activity against human GCGR, GIPR,and GLP-1R with EC50 values of 5.79, 0.0643, and 0.775 nM,respectively[1]. For mouse GCGR, GIPR, and GLP-1R, Retatrutide shows activity withEC50 values of 2.32, 0.191, and 0.794 nM, respectively[1]. In terms of binding affinity, Retatrutide has Ki values of 5.6,0.057, and 7.2 nM for human GCGR, GIPR, and GLP-1R,respectively[1]. Similarly, for mouse GCGR, GIPR, and GLP-1R, Retatrutide exhibitsbinding affinity with Ki values of 73, 2.8, and 1.3 nM,respectively[1]. |
| 体内活性 | In vivo, Retatrutide (LY3437943) engages with GCGR and, whenadministered through subcutaneous injection at a single dose of0.47 mg/kg, improves glucose tolerance in an ipGTT (intraperitonealglucose tolerance test) through activation of GIP or GLP-1receptors[1]. With subcutaneous injections at 10 mL/kg every 3 days in a cyclesustained for 21 days, Retatrutide leads to significant weightreduction and increased energy expenditure through activation ofglucagon receptor[1]. |
| 别名 | LY3437943 |
| 分子量 | 4731.33 |
| 分子式 | C221H342N46O68 |
| CAS No. | 2381089-83-2 |
