GS-6201

GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (K_i=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]. IC50 & Target: Ki: 22 nM (human A2B receptors), 1070 nM (human A3 receptors), 1940 nM (human A1 receptors), 3280 nM (human A2A receptors)^[1] 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 C_max, dAUC and t_1/2 are 1110 ng/mL, 6500 ng h/mL, and 4.25 hours, respectively^[1].