752222-83-6
Chemical Structure
GS-6201
Synonym(s): CVT-6883
- CAS No.: 752222-83-6
- Formula:C21H21F3N6O2
- Molecular Weight:446.43
IUPAC Name: 3-ethyl-1-propyl-8-(1-(3-(trifluoromethyl)benzyl)-1H-pyrazol-4-yl)-3,9-dihydro-1H-purine-2,6-dione
InChIKey: KOYXXLLNCXWUNF-UHFFFAOYSA-N
SMILES: O=C(N1CCC)N(CC)C2=C(N=C(C3=CN(CC4=CC=CC(C(F)(F)F)=C4)N=C3)N2)C1=O
Biological Activity: GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM)[1]. GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse[2]. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice[3].
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GS-6201 | 98.47% | GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice. | ||||||||||||||||||||
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GS-6201 (Standard) | ≥98% | GS-6201 (Standard) is the analytical standard of GS-6201 (HY-10081). This product is intended for research and analytical applications. GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM). GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse. GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice. | ||||||||||||||||||||
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References
- [1]. Elzein E, et al. Discovery of a novel A2B adenosine receptor antagonist as a clinical candidate for chronic inflammatory airway diseases. J Med Chem. 2008 Apr 10;51(7):2267-78. [Content Brief]
- [2]. Toldo S, et al. GS-6201, a selective blocker of the A2B adenosine receptor, attenuates cardiac remodeling after acute myocardial infarction in the mouse. J Pharmacol Exp Ther. 2012 Dec;343(3):587-95. [Content Brief]
- [3]. Mustafa SJ, et al. Effect of a specific and selective A(2B) adenosine receptor antagonist on adenosine agonist AMP and allergen-induced airway responsiveness and cellular influx in a mouse model of asthma. J Pharmacol Exp Ther. 2007 Mar;320(3):1246-51. [Content Brief]
