Bosentan hydrate

Bosentan is a mixed Endothelin Receptor Antagonist which is used as a vasodilator. Bosentan is an inhibitor of ETAR and ETBR. It is used for the treatment of pulmonary artery hypertension (PAH). Bosentan blocks the action of endothelin molecules that would otherwise promote narrowing of the blood vessels and lead to high blood pressure.

Bosentan hydrate 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.

Properties:

Appearance & Physical State: white powder

Boiling Point: 742.3ºC at 760 mmHg

Flash Point: 402.8ºC

Vapor Pressure: 3.84E-23mmHg at 25°C

Endothelin Receptor Inhibitors Related Prodcuts:

[1]. 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.

[2]. Akamata K, et al. Bosentan reverses the pro-fibrotic phenotype of systemic sclerosis dermal fibroblasts via increasing DNA binding ability of transcription factor Fli1. Arthritis Res Ther. 2014 Apr 3;16(2):R86.

[3]. Iglarz M, et al. Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension. Life Sci. 2014 Nov 24;118(2):333-9.