Chemical Name: 5-[4-(4-Cyano-1-butyn-1-yl)phenyl]-1-(2,4-dichlorophenyl)-N-(1,1-dioxido-4-thiomorpholinyl)-4-methyl-1H-pyrazole-3-carboxamide
Biological ActivityHigh affinity and selective CB1 antagonist (Ki = 3.3 nM). Exhibits >100-fold selectivity for CB1 over CB2 receptors. Improves glucose homeostasis, reverses hepatic steatosis and reduces body weight in diet-induced obese mice. Orally available and non-brain penetrant.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity.
Tam et al.
A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome.
Bowles et al.
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