AM 6545
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Description: High affinity and selective CB1 antagonist
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
Purity: ≥98%
Biological Activity
High affinity and selective CB 1 antagonist (K i = 3.3 nM). Exhibits >100-fold selectivity for CB 1 over CB 2 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
-
Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity.
Tam et al.
J.Clin.Invest., 2010;120:2953 -
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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