GS 6201

• Supplier: Tocris Bioscience
• Catalog: 2001
• Prices: $189.00, $765.00
• Sizes: 10 mg, 50 mg
• Function Type: Antagonist
• Cas Number: 752222-83-6
• Chemical Name: 3-Ethyl-3,9-dihydro-1-propyl-8-[1-[[3-(trifluoromethyl)phenyl]methyl]-1H-pyrazol-4-yl]-1H-purine-2,6-dione
• Formula: C21H21F3N6O2
• Molecular Weight: 446.43
• Purity: >99 %
• Description: Selective antagonist of adenosine A 2B receptors (K i values are 22, 1070, 1940 and 3280 nM for human A 2B , A 3 , A 1 and A 2A receptors respectively). Attenuates allergen-, NECA- and AMP-induced airway reactivity in an allergic mouse model of asthma. Also shown to attenuate the inflammatory response during acute myocardial infarction in mice; reduces caspase-1 activity in the heart.

Product References

Effect of a specific and selective A(2B) adenosine receptor antagonist on - Effect of a specific and selective A(2B) adenosine receptor antagonist on

Mustafa SJ, Nadeem A, Fan M, Zhong H, Belardinelli L, Zeng D. J Pharmacol Exp Ther. 2007 Mar;320(3):1246-51. Epub 2006 Dec 11.

Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate - Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate

Elzein E, Kalla RV, Li X, Perry T, Gimbel A, Zeng D, Lustig D, Leung K, Zablocki J. J Med Chem. 2008 Apr 10;51(7):2267-78.

GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac - GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac

Toldo S, Zhong H, Mezzaroma E, Van Tassell BW, Kannan H, Zeng D, Belardinelli L, Voelkel NF, Abbate A. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95.