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 has efficacy for mouse GCGR, GIPR, and GLP-1R with EC50 values of 2.32, 0.191 and 0.794 nM, respectively.
Retatrutide (LY3437943) acetate engages GCGR in vivo and can improve glucose tolerance in an ipGTT through either the GIP or GLP-1 receptors. Retatrutide acetate causes great body weight loss and increases energy expenditure through glucagon receptor activatio. Retatrutide acetate can be used for the research of obesity.
| Molecular Weight | 4791.38 |
| Formula | C221H342N46O68.C2H4O2 |
| CAS Number | 2381089-83-2 (free base) |
| Form | Solid |
| Solubility (25°C) | Water 10 mg/mL |
| Storage | Store at ≤ -20°C, protect from light, dry, sealed |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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