Application

Bosentan hydrate has been used in cell viability assay. It has also been used as a positive control for calcium transient analysis.

Biochem/physiol Actions

Bosentan is an endothelin receptor antagonist. Endothelin is a potent vasoconstrictor, making antagonists of clinical interest for the treatment of conditions associated with vasospasm, such as subarachnoid hemorrhage (SAH) and hypertension. Bosentan is a dual endothelin receptor antagonist effective in the treatment of pulmonary arterial hypertension (PAH), the first of the class to make it to market. Bosentan is an orally available, competitive antagonist of both the ETA and ETB receptor subtypes with a Ki of 4.7 nM for ETA and a Ki of 95 nM for ETB.

Bosentan is found to decrease deposition of collagen in the lungs, which has been observed in bleomycin-induced pulmonary fibrosis rat model.

Packaging

10, 50 mg in glass bottle