GS-6201, also known as CVT-6883, acts as a selective antagonist for the adenosine A2B receptor. It exhibits a strong affinity and specificity towards human adenosine A2B receptors, with an inhibition constant Ki value of 22 nM[1].
GS-6201 动物研究
Animal study
GS-6201 diminishes the activity of caspase-1 in the heart and mitigates the cardiac changes following an acute myocardial infarction (AMI) in mice. When administered at a dosage of 4 mg/kg intraperitoneally every 12 hours for two weeks, GS-6201 notably lowers the plasma levels of IL-6, TNF-α, E-selectin, ICAM-1, and VCAM. Additionally, this treatment significantly reduces the enlargement and dysfunction of both the left and right ventricles after 7 days, with these effects persisting at both 14 and 28 days[2]. Treatment with GS-6201, administered orally at a dose of 2 mg/kg, results in a Cmax of 1110 ng/mL, a dAUC of 6500 ng·h/mL, and a half-life (t1/2) of 4.25 hours[1].
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