| Bioactivity | 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]. | |||||||||
| Target | Ki: 22 nM (human A2B receptors), 1070 nM (human A3 receptors), 1940 nM (human A1 receptors), 3280 nM (human A2A receptors) | |||||||||
| In Vivo | GS-6201 (CVT-6883) (4 mg/kg; i.p.; every 12 h for 14 days) significantly reduces IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels[2].GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) leads to a significant attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days[2].GS-6201 (2 mg/kg; p.o.) treatment shows the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively[1]. Animal Model: | |||||||||
| Name | GS-6201 | |||||||||
| CAS | 752222-83-6 | |||||||||
| Formula | C21H21F3N6O2 | |||||||||
| Molar Mass | 446.43 | |||||||||
| Appearance | Solid | |||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | |||||||||
| Storage |
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| Reference | [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. [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. [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. |