GS-6201 是选择性腺苷A2B受体拮抗剂。它对人腺苷 A2B 受体具有高亲和力和选择性 (Ki=22 nM)。它降低了小鼠急性心肌梗死后心脏中 Caspase-1 的活性，并减弱了心脏重塑。它减弱了致敏小鼠 NECA，AMP 或变应原诱导的气道反应性。

GS-6201 is a selective antagonist of adenosine A2B receptor. GS-6201 shows high affinity and selectivity for the human adenosine A2B receptors with a Ki of 22 nM.

GS-6201 (2 mg/kg; p.o.) treatment displays the Cmax, dAUC and t1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively [1]. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) obviously decreases IL-6, TNF-α, E-selectin, ICAM-1, and VCAM plasma levels. GS-6201 (4 mg/kg; i.p.; every 12 h for 14 days) causes an obvious attenuation of left and right ventricular enlargement and dysfunction at 7 days, which was maintained at 14 days and also at 28 days [2].

752222-83-6

C21H21F3N6O2

446.43

CVT-6883

DMSO:30 mg/ml (67.2 mM),Need ultrasonic and warming and heat to 60°C
Powder: -20°C for 3 years
In solvent: -80°C for 2 years