Darexaban (maleate)
Product Specifications
UNSPSC Description
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].
Target Antigen
Endogenous Metabolite
Type
Reference compound
Related Pathways
Metabolic Enzyme/Protease
Applications
Neuroscience-Neuromodulation
Field of Research
Cardiovascular Disease
Assay Protocol
https://www.medchemexpress.com/darexaban-maleate.html
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
Molecular Weight
590.62
References & Citations
[1]Identification of UDP-glucuronosyltransferases responsible for the glucuronidation of darexaban, an oral factor Xa inhibitor, in human liver and intestine
Shipping Conditions
Room temperature
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-135541/Darexaban-maleate-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-135541/
Clinical Information
No Development Reported
CAS Number
365462-24-4
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