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[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].

Product Specifications

CAS Number

[253688-62-9]

Product Name Alternative

Ro 64-1056

UNSPSC

12352005

Hazard Statement

H302

Target

Drug Metabolite

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/hydroxy-desmethyl-bosentan.html

Solubility

10 mM in DMSO

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

Molecular Formula

C26H27N5O7S

Molecular Weight

553.59

Precautions

P264-P270-P330-P501

References & Citations

[1]Lepri S, et al. Metabolism study and biological evaluation of bosentan derivatives. Eur J Med Chem. 2016 Oct 4;121:658-670.|[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.