A potent CB1 receptor antagonist (IC50 = 118.9 pM; Ki = 27.2 pM for rat CB1); selective for CB1 over CB2

MJ15 – 10 mg

Brand:
Cayman
CAS:
944154-76-1
Storage:
-20
UN-No:
Non-Hazardous - /

MJ15 is a potent antagonist of the cannabinoid (CB) receptor CB1 (IC50 = 118.9 pM; Ki = 27.2 pM for rat CB1).{32932} It is selective for CB1 over CB2, exhibiting only 46% inhibition of CB2 at a concentration of 10 μM. MJ15 reverses (+)-WIN 55,212-2 (Item No. 10009023) inhibition of forskolin-induced cAMP accumulation in a dose-dependent manner in CHO cells expressing human CB1. MJ15 (40 mg/kg) reduces food intake and body weight gain in a rat model of diet-induced obesity. It also reduces body weight gain and white adipose accumulation in a mouse model of early onset diet-induced obesity.  

 

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SKU: 11956 - 10 mg Category:

Description

A potent CB1 receptor antagonist (IC50 = 118.9 pM; Ki = 27.2 pM for rat CB1); selective for CB1 over CB2, exhibiting only 46% inhibition of CB2 at a concentration of 10 μM; reverses (+)-WIN 55,212-2 inhibition of forskolin-induced cAMP accumulation in a dose-dependent manner in CHO cells expressing human CB1; reduces food intake and body weight gain in a rat model of diet-induced obesity at a dose of 40 mg/kg; reduces body weight gain and white adipose accumulation in a mouse model of early onset diet-induced obesity

Formal name: 5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(3-pyridinylmethyl)-1H-pyrazole-3-carboxamide

Synonyms: 

Molecular weight: 471.8

CAS: 944154-76-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Obesity

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