Darexaban maleate is a direct factor Xa inhibitor, primarily utilized in the research of venous thromboembolism prevention. Its major metabolite, Darexaban glucitol, exhibits pharmacological activity and is formed in the human liver and intestine via UGT1A9 and UGT1A10-mediated glucitolation. The glucitolation exhibits a K(m) value greater than 250 μM in the liver, while in the intestine, it displays substrate inhibition kinetics with a K(m) of 27.3 μM. The presence of fatty acid-free bovine serum albumin significantly lowers the unbound K(m) values in human liver microsomes and UGT1A9.
Darexaban maleate is a direct factor Xa inhibitor, primarily utilized in the research of venous thromboembolism prevention. Its major metabolite, Darexaban glucitol, exhibits pharmacological activity and is formed in the human liver and intestine via UGT1A9 and UGT1A10-mediated glucitolation. The glucitolation exhibits a K(m) value greater than 250 μM in the liver, while in the intestine, it displays substrate inhibition kinetics with a K(m) of 27.3 μM. The presence of fatty acid-free bovine serum albumin significantly lowers the unbound K(m) values in human liver microsomes and UGT1A9.
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