URB447 

URB447 is a peripherally restricted CB₁ cannabinoid antagonist (IC₅₀: 313 nM and 41 nM for rat CB1 and human CB2 receptor respectively ). URB447 lowers food intake and body-weight gain in mice without entering the brain or antagonizing central CB₁-dependent responses. URB447 can be used for research of obesity^[1].

URB447 (100 nM-30 μM) inhibits GTPγS binding induced by the CB agonist WIN55,212-2 (1 μM), with an EC₅₀ of 4.9 μM in rat cerebellar membrane preparations^[1].
URB447 (1 μM) inhibits β-adrenergic agonist Isoproterenol (10 μM) induced cAMP accumulation in Hek-293 cells stably expressing mouse CB₂ receptors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

URB447 (20 mg/kg, i.p.) reduces total food consumption in Swiss mice, and shows a C_max of 596 nM^[1].
URB447 (20 mg/kg, i.p.) blocks the analgesic effects of Methanandamide in Swiss mice, indicating URB447 inhibits peripheral CB1-mediated analgesia^[1].
URB447 (20 mg/kg, i.p., once daily for 2 weeks) reduces food consumption and body-weight gain in obese ob/ob mice^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

400.90

C₂₅H₂₁ClN₂O

1132922-57-6

Solid

Light yellow to yellow

O=C(C1=C(C)N(CC2=CC=C(C=C2)Cl)C(C3=CC=CC=C3)=C1N)C4=CC=CC=C4

Room temperature in continental US; may vary elsewhere.

• [1]. LoVerme J, et al. Synthesis and characterization of a peripherally restricted CB1 cannabinoid antagonist, URB447, that reduces feeding and body-weight gain in mice. Bioorg Med Chem Lett. 2009 Feb 1;19(3):639-43.  [Content Brief]