Bioactivity | Retatrutide (LY3437943) acetate is a triple agonist peptide of the glucagon receptor (GCGR), glucosedependent insulinotropic polypeptide receptor (GIPR), and glucagon-like peptide-1 receptor (GLP-1R). Retatrutide acetate inhibits for human GCGR, GIPR, and GLP-1R with EC50 values of 5.79, 0.0643 and 0.775 nM, respectively. Retatrutide acetate can be used for the research of obesity[1]. |
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). |
Invitro | Retatrutide (LY3437943) acetate 对人 GCGR、GIPR 和 GLP-1R 具有活性,EC50 值分别为 5.79、0.0643 和 0.775 nM[1]。Retatrutide acetate 对小鼠 GCGR、GIPR 和 GLP-1R 具有活性,EC50 值分别为 2.32、0.191 和 0.794 nM[1]。Retatrutide acetate 对人 GCGR、GIPR 和 GLP-1R 具有结合亲和力,Ki 值分别为 5.6、0.057 和 7.2 nM[1]。Retatrutide acetate 对小鼠 GCGR、GIPR 和 GLP-1R 具有结合亲和力,Ki 值分别为 73、2.8 和 1.3 nM[1]。 |
In Vivo | Retatrutide (LY3437943) acetate (皮下注射;0.47 mg/kg;单次) 在体内参与 GCGR,并可通过 GIP 或 GLP-1 受体改善 ipGTT 中的葡萄糖耐量[1]。Retatrutide acetate (皮下注射;10 mL/kg;每 3 天一个周期;持续 21 天) 通过胰高血糖素受体激活导致体重显着减轻并增加能量消耗[1]。Retatrutide acetate 具有安全性和耐受性[1]。 |
Name | Retatrutide acetate |
Formula | C221H342N46O68.C2H4O2 |
Molar Mass | 4791.38 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. 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. |