| Bioactivity | MRL-650 (CB1 inverse agonist 1) is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects[1]. |
| In Vivo | MRL-650 (Compound 14; 0.3, 1, or 3 mg/kg)inhibits feeding in a dose-dependent manner[1]. The pharmacokinetic profile of CB1 inverse agonist 1 is evaluated in Sprague-Dawley rats, C57BL/6 mice, beagles, and rhesus macaques with t1/2 of >8, >8, >24, and 22 h, respectively[1]. Animal Model: |
| Name | MRL-650 |
| CAS | 852315-00-5 |
| Formula | C25H18Cl3N3O3 |
| Molar Mass | 514.79 |
| 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]. Debenham JS, et al. Synthesis of functionalized 1,8-naphthyridinones and their evaluation as novel, orally active CB1 receptor inverse agonists.Bioorg Med Chem Lett. 2006 Feb;16(3):681-5. |