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Active ingredient: Bosentan - Chemisty and Biological Activity

Chemisty and Biological Activity

Chemical Formula


Chemical Name

N-[6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-2-pyrimidin-2-yl-pyrimidin-4- yl]-4-tert-butyl-benzenesulfonamide

Chemical Structure

Molecular Weight

551.615 g/mol

Physical State


Melting Point

Not Available

Water Solubility

Poorly soluble in water (1.0 mg/100 ml) and in aqueous solutions at low pH (0.1 mg/100 ml at pH 1.1 and 4.0; 0.2 mg/100 ml at pH 5.0). Solubility increases at higher pH values (43 mg/100 ml at pH 7.5).

Isoelectric Point

Not Available

Organisms Affected

Humans and other mammals

Phase 1 Metabolising Enzyme (1-st Step of Metabolism)


Primary Drug Target
NameEndothelin B receptor precursor
Gene NameEDNRB
SynonymsET-B; Endothelin receptor Non- selective type
Specific FunctionNon-specific receptor for endothelin 1, 2, and 3. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system

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