产品描述:
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}