Hydroxy desmethyl Bosentan is a metabolite of Bosentan, primarily produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. As a dual antagonist of endothelin-1 (ET) at the ETA and ETB receptors, it exhibits inhibitory constants (Ki) of 4.7 nM and 95 nM, respectively, in human smooth muscle cells. This compound is relevant for studies related to pulmonary arterial hypertension and provides insight into drug metabolism and pharmacokinetics of Bosentan.
Hydroxy desmethyl Bosentan is a metabolite of Bosentan, primarily produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. As a dual antagonist of endothelin-1 (ET) at the ETA and ETB receptors, it exhibits inhibitory constants (Ki) of 4.7 nM and 95 nM, respectively, in human smooth muscle cells. This compound is relevant for studies related to pulmonary arterial hypertension and provides insight into drug metabolism and pharmacokinetics of Bosentan.
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