Hydroxy desmethyl Bosentan

• Description :

  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 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.

• Shipping Conditions :

  Room temperature

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• CAS Number :

  [253688-62-9]