AM 6545
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
AM 6545 is a 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
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
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Cannabinoid CB1 receptor overactivity contributes to the pathogenesis of idiopathic pulmonary fibrosis
R Cinar, BR Gochuico, MR Iyer, T Jourdan, T Yokoyama, JK Park, NJ Coffey, H Pri-Chen, G Szanda, Z Liu, K Mackie, WA Gahl, G Kunos
JCI Insight, 2017;2(8):. -
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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Citation for AM 6545
The citations listed below are publications that use Tocris products. Selected citations for AM 6545 include:
1 Citation: Showing 1 - 1
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Identification of an endocannabinoid gut-brain vagal mechanism controlling food reward and energy homeostasis.
Authors: Giulio G Et al.
Mol Psychiatry 2022;27:2340-2354
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