Catalog No.: PC-20918Not For Human Use, Lab Use Only.
Bosentan (Ro 47-0203) is a potent, 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 (Ro 47-0203) is a potent, 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 (Ro 47-0203) competitively and specifically antagonizes binding of 125I-labelled ET-1 to ETA receptors on human smooth muscle cells (SMC) and ETB receptors on human placenta cells. Bosentan (Ro 47-0203) shows 67-fold greater selectivity for ETA than ETB receptors (mean IC50=7.1 vs 474.8 nM) in an in vitro 125I-labeling assay. Bosentan (Ro 47-0203) blocks the initial depressor, tachycardic and hindquarters hyperaemic vasodilator effects of ET-1, -2 and -3, and substantially curtailed the primary renal and secondary hindquarters vasoconstrictor responses.
