Hydroxy Desmethyl Bosentan

Names

[ Name ]:
Hydroxy Desmethyl Bosentan

[Synonym ]:
Hydroxy Desmethyl Bosentan
Bosentan Impurity 3

Biological Activity

[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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.426g/cm3

[ Boiling Point ]:
782ºC at 760 mmHg

[ Molecular Formula ]:
C₂₆H₂₇N₅O₇S

[ Molecular Weight ]:
553.58700

[ Flash Point ]:
426.7ºC

[ Exact Mass ]:
553.16300

[ PSA ]:
185.26000

[ LogP ]:
4.02710

[ Vapour Pressure ]:
9.41E-26mmHg at 25°C

[ Index of Refraction ]:
1.643

Related Compounds

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