DMSO in 18 mg/mL Water in <1 mg/mL Ethanol in <1 mg/mL
Reversible inhibitor of Factor Xa
venous thromboembolism, stroke
REVIEW Apixaban is a highly selective, reversible, and direct inhibitor of Human Factor X and Rabbit Factor X with Ki of 0.08 nM and 0.17 nM, respectively. Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor X with Ki of 0.08 nM and 0.17 nM for Human Factor X and Rabbit Factor X, respectively. In vitro, Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 µM, 0.37 µM, 7.4 µM, and 0.4 µM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays.