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Submit ReviewBosentan is a high affinity dual ETA and ETB receptor antagonist (Ki values are 4.7 and 95 nM for ETA and ETB, respectively). Inhibits ET-1 induced contraction of isolated rat aorta and sarafotoxin S6C-induced contraction of rat trachea in vitro. Orally bioavailable.
Bosentan is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 551.61 |
公式 | C27H29N5O6S |
储存 | Store at +4°C |
纯度 | ≥98% (HPLC) |
CAS Number | 147536-97-8 |
PubChem ID | 104865 |
InChI Key | GJPICJJJRGTNOD-UHFFFAOYSA-N |
Smiles | COC1=C(C=CC=C1)OC2=C(N=C(C3=NC=CC=N3)N=C2NS(=O)(C4=CC=C(C(C)(C)C)C=C4)=O)OCCO |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 55.16 | 100 | |
ethanol | 27.58 | 50 |
以下数据基于产品分子量 551.61。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.81 mL | 9.06 mL | 18.13 mL |
5 mM | 0.36 mL | 1.81 mL | 3.63 mL |
10 mM | 0.18 mL | 0.91 mL | 1.81 mL |
50 mM | 0.04 mL | 0.18 mL | 0.36 mL |
参考文献是支持产品生物活性的出版物。
Clozel et al (1994) Pharmacological characterization of bosentan, a new potent orally active nonpeptide endothelin receptor antagonist. J.Pharmacol.Exp.Ther. 270 228 PMID: 8035319
Gardiner et al (1994) Effects of bos. (Ro 47-0203), an ETA-, ETB-receptor antagonist, on regional haemodynamic responses to endothelins in conscious rats. Br.J.Pharmacol. 112 823 PMID: 7921608
If you know of a relevant reference for Bosentan, please let us know.
关键词: Bosentan, Bosentan supplier, High, affinity, endothelin, antagonists, antagonism, ETA, ETB, orally, bioavailable, Ro470203, Ro, 47-0203, Non-selective, Endothelin, 6232, Tocris Bioscience
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