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首页-小分子抑制剂&激动剂-GPCR-Endothelin Receptor-Bosentan
Bosentan

Chemical Structure : Bosentan

CAS No.: 147536-97-8

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Bosentan (Ro 47-0203)

货号: 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 ￥1580 In stock
500 mg ￥2980 In stock
1 g ￥4980 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 551.62
分子式 C27H29N5O6S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

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

参考文献

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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