Catalog Number: 5443
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 Activity
High 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.
Technical Data
  • M.Wt:
    556.46
  • Formula:
    C26H23Cl2N5O3S
  • Solubility:
    Soluble to 20 mM in DMSO
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    1245626-05-4
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity.
    Tam et al.
    J.Clin.Invest., 2010;120:2953
  2. A peripheral endocannabinoid mechanism contributes to glucocorticoid-mediated metabolic syndrome.
    Bowles et al.
    Proc.Natl.Acad.Sci.U.S.A., 2015;112:285

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