365462-24-4
Chemical Structure
Darexaban maleate
Synonym(s): YM150 maleate
- CAS No.: 365462-24-4
- Formula:C31H34N4O8
- Molecular Weight:590.62
IUPAC Name: N-(3-hydroxy-2-(4-(4-methyl-1,4-diazepan-1-yl)benzamido)phenyl)-4-methoxybenzamide maleate
InChIKey: WHMPMUVISXATBH-BTJKTKAUSA-N
SMILES: OC(/C=C\C(O)=O)=O.O=C(C1=CC=C(N2CCCN(CC2)C)C=C1)NC3=C(C=CC=C3O)NC(C4=CC=C(C=C4)OC)=O
Biological Activity: Darexaban maleate (YM150 maleate) is a direct factor Xa inhibitor with activity in preventing venous thromboembolism. The major metabolite of Darexaban maleate in humans is Darexaban glucitol, which acts pharmacologically. The glucitolation reaction of Darexaban maleate is mainly catalyzed by UGT1A9 and UGT1A10 in the human liver and intestine. The K(m) value of Darexaban maleate glucitolation in the liver is greater than 250 μM, while in the intestine it exhibits substrate inhibition kinetics with a K(m) value of 27.3 μM. The unbound K(m) value of Darexaban maleate is significantly reduced by the influence of fatty acid-free bovine serum albumin in both HLM and UGT1A9[1].
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Darexaban maleate | Darexaban maleate (YM150 maleate) is a direct factor Xa inhibitor with activity in preventing venous thromboembolism. The major metabolite of Darexaban maleate in humans is Darexaban glucitol, which acts pharmacologically. The glucitolation reaction of Darexaban maleate is mainly catalyzed by UGT1A9 and UGT1A10 in the human liver and intestine. The K(m) value of Darexaban maleate glucitolation in the liver is greater than 250 μM, while in the intestine it exhibits substrate inhibition kinetics with a K(m) value of 27.3 μM. The unbound K(m) value of Darexaban maleate is significantly reduced by the influence of fatty acid-free bovine serum albumin in both HLM and UGT1A9. | |||||||||||||||||||||
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Keywords
