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Chemical Structure : Bosentan
CAS No.: 147536-97-8
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.
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|---|---|---|---|
| 100 mg | $158 | In stock | |
| 500 mg | $298 | In stock | |
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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.
| M.Wt | 551.62 | |
| Formula | C27H29N5O6S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
4-(tert-butyl)-N-(6-(2-hydroxyethoxy)-5-(2-methoxyphenoxy)-[2,2'-bipyrimidin]-4-yl)benzenesulfonamide |
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1. Dhillon S, et al. J Cardiovasc Drugs. 2009;9(5):331-50.
2. Gardiner SM, et al. Br J Pharmacol. 1994 Jul;112(3):823-30.
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