MJ-15 is a selective cannabinoid CB(1) receptor antagonist with a potency in obesity and dyslipidemia treatment. In receptor binding assays, MJ-15 displayed a high affinity for rat cannabinoid CB(1) receptor (Ki=27.2 pM, and IC50=118.9 pM), but a much lower affinity for rat cannabinoid CB(2) receptor (only 46% inhibition at 10 uM). In animal experiments, MJ15 promoted the small intestine peristalsis in ICR mice and inhibited food intake and body weight increase in diet-induced obesity (DIO) rat and mouse. 40 mg/kg MJ15 significantly reduced food intake at initial 2 weeks of treatment, prevented the increase of body weight and adipose by 46% and 28% respectively in DIO rats, and reduced body weight and adipose gain by 70% and 23% respectively in early onset obesity DIO mice after 4 weeks treatment. Dyslipidemia were ameliorated in both models.