CB1 inverse agonist 1

Research use only, not for human use.

CB1 inverse agonist 1 (MRL-650) is an orally active and selective CB1 agonist. The IC50s for CB1 and CB2 are 7.5 nM and 4100 nM, respectively.

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.

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MRL-650 (Compound 14; 0.3, 1, or 3 mg/kg）inhibits feeding in a dose-dependent manner. 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.Animal Model:Rat Dosage:0.3, 1, or 3 mg/kg Administration:PO Result:Inhibited feeding in a dose-dependent manner. 3 mg/kg decreased cumulative food intake from 2 h post-dosing. Decreased overnight body weight gain compared to vehicle treatment at all dosing levels.

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GPCR/G Protein

Cannabinoid Receptor

Cannabinoid Receptor

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852315-00-5

514.79

C25H18Cl3N3O3

>98% (HPLC)

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N(C(C)=O)C=1C=2C(=NC(=C(C2)C3=CC=C(Cl)C=C3)C4=C(Cl)C=C(Cl)C=C4)N(C)C(=O)C1C(C)=O

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(-20℃)

With Ice Pack

≥ 2 years