253688-62-9
Chemical Structure
Hydroxy desmethyl Bosentan
Synonym(s): Ro 64-1056
- CAS No.: 253688-62-9
- Formula:C26H27N5O7S
- Molecular Weight:553.59
IUPAC Name: 4-(1-hydroxy-2-methylpropan-2-yl)-N-(6-(2-hydroxyethoxy)-5-(2-hydroxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide
InChIKey: JXXCMZWROOURSZ-UHFFFAOYSA-N
SMILES: O=S(C1=CC=C(C(C)(C)CO)C=C1)(NC2=NC(C3=NC=CC=N3)=NC(OCCO)=C2OC4=CC=CC=C4O)=O
Biological Activity: Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver[1]. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension[2].
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Hydroxy desmethyl Bosentan | Hydroxy desmethyl Bosentan (Ro 64-105) is a Bosentan metabolism produced by the cytochrome P450 enzymes CYP2C9 and CYP3A4 in the liver. Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively. Bosentan can be used in treatment of pulmonary arterial hypertension. | |||||||||||||||||||||
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- [1]. Lepri S, et al. Metabolism study and biological evaluation of bosentan derivatives. Eur J Med Chem. 2016 Oct 4;121:658-670. [Content Brief]
- [2]. Dhillon S, et al. Bosentan: a review of its use in the management of mildly symptomatic pulmonary arterial hypertension. Am J Cardiovasc Drugs. 2009;9(5):331-50. [Content Brief]
Keywords
