- $97
- Alomone
- ZK-0039511
- 以色列
- 2025年11月20日
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- Synthetic
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- 详细信息
- 技术资料
- 供应商：
上海再康生物科技有限公司
- 库存：
大量
- 靶点：
见官方网站
- 级别：
高
- 目录编号：
S-185
- 克隆性：
多克隆
- 抗原来源：
Synthetic
- 保质期：
6个月
- 抗体英文名：
Sitaxsentan sodium salt
- 抗体名：
Sitaxsentan sodium salt
- 标记物：
见官方网站
- 宿主：
Synthetic
- 适应物种：
见官方网站
- 免疫原：
见官方网站
- 亚型：
见官方网站
- 形态：
液体或冻干粉
- 应用范围：
见官方网站
- 浓度：
见官方网站
- 保存条件：
-20°C
- 规格：
10 mg, 25 mg, 50 mg, 100 mg
Sitaxsentan sodium salt
TBC-11251 sodium saltA Potent and Selective Antagonist of Endothelin A Receptor
Cat #: S-185
Sizes: 10 mg, 25 mg, 50 mg, 100 mg
Source: Synthetic
MW: 476.88 Da.
Target: ET-A receptors
CLICK HERE TO RECEIVE A 10 mg FREE TRIAL SAMPLE!
Sitaxsentan, is a synthetic compound that acts as a potent and selective antagonist of ET-A endothelin receptors. Sitaxsentan is one of the most selective ET-A antagonists reported1. Sitaxsentan inhibits Endothelin-1 radioligand binding to human ET-A and ET-B receptors with IC50 of 1.4 nM and 9.8 µM, respectively1.
In pulmonary arterial hypertension clinical trials, sitaxsentan was shown to improve exercise capacity, improve functional capacity, and delay clinical worsening. However, the compound shows high liver toxicity and is no longer used to treat hypertension2.
Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also distributed in several regions of the brain.
ET-A has high affinity for endothelin-1 and endothelin -2 and relatively low affinity for endothelin -3, while the ET-B receptor has high affinity equally for all endothelin isopeptides3.
Alomone Labs is pleased to offer Sitaxsentan sodium salt (#S-185).
Sitaxsentan sodium saltReferences
- Wu, C. et al. (1997) J. Med. Chem. 40, 1690.
- Lepist, E.I. et al. (2014) PLoS One 9, e87548.
- Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286.
- Our Bioassay
- Specifications
- Related Products
Alomone Labs Sitaxsentan sodium salt inhibits ETA receptor-mediated Ca2+ mobilization in CHO cells.
Dose response curve of Sitaxsentan sodium salt (#S-185) inhibition of the ET-A receptor-mediated, Endothelin-1-evoked Ca2+ mobilization. IC50 was determined at 9.29 nM. Cells were loaded with Calcium 6 dye, incubated with Sitaxsentan sodium salt, and stimulated with 15 nM Endothelin-1 (EC80). Changes in intracellular Ca2+ levels were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™.
Purity>99%.
Effective concentration1-100 nM.
Chemical name(4-chloro-3-methyl-1,2-oxazol-5-yl)-[2-[2-(6-methyl-1,3-benzodioxol-5-yl)acetyl]thiophen-3-yl]sulfonylazanide sodium.
Molecular formulaC18H14ClN2NaO6S2.
CAS number210421-74-2.
ActivitySitaxsentan is a potent and selective antagonist of ET-A Endothelin receptors, inhibiting Endothelin-1 radioligand binding to human ET-A and ET-B receptors with IC50 of 1.4 nM and 9.8 µM, respectively (a 7000-fold selectivity). in vitro, Sitaxsentan inhibits Endothelin-1 induced phosphoinositide turnover with a pA2 of 8.01. Sitaxsentan is orally bioavailable and active in vivo1,2.
Storage before reconstitutionProduct before reconstitution should be stored at -20oC.
ReconstitutionSoluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Storage after reconstitutionUp to three months at -20°C.
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