Catalog No.: PC-23821Not For Human Use, Lab Use Only.
BQ-788 sodium salt is a potent, selective endothelin-B receptor (ETB) antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, >1000-fold selective over ETA receptor.
BQ-788 sodium salt is a potent, selective endothelin-B receptor (ETB) antagonist with IC50 of 1.2 nM for inhibition of ET-1 binding to human Girardi heart cells, >1000-fold selective over ETA receptor. BQ-788 poorly inhibits the binding to ETA receptors on human neuroblastoma cell line SK-N-MC cells (IC50, 1300 nM). BQ-788 shows no agonist activity up to 10 microM in isolated rabbit pulmonary arteries. BQ-788 competitively antagonizes the vasoconstriction induced by an ETB-selective agonist, BQ-3020 (pA2, 8.4). BQ-788 (1 mg/kg, i.v.) abolishes the depressor response, resulting in a rapid onset of apparently enhanced pressor response in rats.
