A metabolite of bosentan; produced by CYP3A4 and CYP2C9

Hydroxy Bosentan – 5 mg

Brand:
Cayman
CAS:
253688-60-7
Storage:
-20
UN-No:
Non-Hazardous - /

Hydroxy bosentan is an active phase I metabolite of bosentan (Item No. 11731) produced by the cytochrome P450 isoforms CYP3A4 and CYP2C9.{39033,39032} Bosentan is an antagonist of the endothelin receptors type A (Ki = 6.5 nM) and type B (Ki = 340 nM).{22374,22376} Up to 20% of the activity of bosentan may be due to the action of hydroxy bosentan because even though it has a lower affinity for endothelin receptors, its concentration is 3-fold higher in plasma.{39034}  

 

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Description

A metabolite of bosentan; produced by CYP3A4 and CYP2C9,

Formal name: 4-(2-hydroxy-1,1-dimethylethyl)-N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)[2,2′-bipyrimidin]-4-yl]-benzenesulfonamide

Synonyms:  ,Ro 48-5033|Ro 48-8634

Molecular weight: 567.6

CAS: 253688-60-7

Purity: ≥98%

Formulation: A crystalline solid

Application|Mass Spectrometry||Product Type|Biochemicals|Analytical Standards||Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Xenobiotic Metabolites||Research Area|Toxicology|Drug Metabolism|Cytochrome P450||Research Area|Toxicology|Drug Metabolism|Drug Metabolites

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