GS-6201 (CVT-6883) 是一种选择性的腺苷A2B受体拮抗剂。GS-6201 对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。GS-6201 降低了小鼠急性心肌梗死 (AMI) 后心脏中 caspase-1 的活性，并减弱了心脏重塑。GS-6201 减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。
货号:ajcx15362
CAS:752222-83-6
分子式:C21H21F3N6O2
分子量：446.43
溶解度:Soluble in DMSO
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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 were 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively[1]. Animal Model: Adult out-bred male CD1 mice (8-12 weeks of age, AMI model)[1]

[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.