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首页 / 抑制剂/激动剂 / G蛋白偶联受体/G蛋白 / 内皮素受体 / Zibotentan

Zibotentan {[allProObj[0].p_purity_real_show]}

货号：A445755 同义名： ZD4054

Zibotentan is an orally administered, potent and specific ETA-receptor (endothelin A receptor) antagonist (IC50 = 21 nM).

Zibotentan 化学结构 CAS号：186497-07-4
Zibotentan 化学结构
CAS号：186497-07-4
Zibotentan 3D分子结构
CAS号：186497-07-4
Zibotentan 化学结构 CAS号：186497-07-4
Zibotentan 3D分子结构 CAS号：186497-07-4
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Zibotentan 纯度/质量文件 产品仅供科研

货号：A445755 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 ET-A ↓ ET-B ↓ 其他靶点 纯度
BQ-123 +++

Endothelin A receptor, IC50: 7.3 nM

 		98%
Macitentan ++++

ET-A, IC50: 0.5 nM

 		+

ET-B, IC50: 391 nM

 		98%
Zibotentan ++

ET-A, IC50: 21 nM

 		99%+
Bosentan hydrate +++

ET-A, Ki: 4.7 nM

 		++

ET-B, Ki: 95 nM

 		98%
Ambrisentan ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Zibotentan 生物活性

靶点

  • ET-A

    ET-A, IC50:21 nM
描述 Endothelin receptors are G protein-coupled receptors (GPCRs) of the β-group of rhodopsin receptors. It can bind to at least four endothelin ligands, ETA, ETB (ETB1, ETB2) and ETC [3]. Zibotentan (ZD4054) potently inhibited the binding of 125iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with the pIC50 of 8.27 nM, but had no measurable affinity (pIC50>10 μM) for ETB [4]. Treatment with 1 μM Zibotentan for 24 hours inhibited proliferation of serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells. And Zibotentan at 1 μM decreased the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells [5]. After oral administration of Zibotentan at a dose of ~3 mg/kg/d for 31days, MBP, SBP and DBP of the rats with hypertension decreased by 5.90 (4.75–7.05) mmHg, 5.91 (4.70–7.11) mmHg and 5.69 (4.26–7.12) mmHg, respectively, and the HR and RR rose by 9.23 (6.21–12.3) bpm and 4.62 (1.89–7.35) br/min, respectively [6].

Zibotentan 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00055471 - Completed - -
NCT00055471 Prostatic Neoplasms ... 展开 >> Metastases, Neoplasm 收起 << Phase 2 Completed - United States, Ohio ... 展开 >> Research Site Cleveland, Ohio, United States, 44195 United States, Wisconsin Research Site Madison, Wisconsin, United States 收起 <<
NCT00929162 Patients With Advanced Ovarian... 展开 >> Cancer Sensitive to Platinum-based Chemotherapy 收起 << Phase 2 Terminated(Primary objective o... 展开 >>f the trial was not met and so there was no benefit in collecting further information) 收起 << - Germany ... 展开 >> Research Site Berlin, Germany Research Site Dresden, Germany Research Site Dusseldorf, Germany Research Site Essen, Germany Research Site Karlsruhe, Germany Research Site Kassel, Germany Research Site Kiel, Germany Research Site Lich, Germany Research Site Magdeburg, Germany Research Site Marburg, Germany Research Site Munchen, Germany Research Site Rostock, Germany Research Site Wiesbaden, Germany Italy Research Site Milano, MI, Italy Research Site Perugia, PG, Italy Research Site Aviano, PN, Italy Research Site Campobasso, Italy Research Site Modena, Italy Research Site Napoli, Italy Research Site Roma, Italy 收起 <<

Zibotentan 参考文献

[1]Rosanò L, Di Castro V, et al. ZD4054, a potent endothelin receptor A antagonist, inhibits ovarian carcinoma cell proliferation. Exp Biol Med (Maywood). 2006 Jun;231(6):1132-5.

[2]Morris CD, Rose A, et al. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer. 2005 Jun 20;92(12):2148-52.

[3] Shepard DR, Dreicer R. Zibotentan for the treatment of castrate-resistant prostate cancer. Expert Opin Investig Drugs. 2010 Jul;19(7):899-908

[4] Morris CD, Rose A, et al. Specific inhibition of the endothelin A receptor with ZD4054: clinical and pre-clinical evidence. Br J Cancer. 2005 Jun 20;92(12):2148-52

[5] Rosanò L, Di Castro V, et al. ZD4054, a specific antagonist of the endothelin A receptor, inhibits tumor growth and enhances paclitaxel activity in human ovarian carcinoma in vitro and in vivo. Mol Cancer Ther. 2007 Jul;6(7):2003-11

[6] Palmer JC, Tayler HM, et al. Zibotentan, an Endothelin A Receptor Antagonist, Prevents Amyloid-β-Induced Hypertension and Maintains Cerebral Perfusion. J Alzheimers Dis. 2020;73(3):1185-1199

Zibotentan 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.36mL

0.47mL

0.24mL

11.78mL

2.36mL

1.18mL

23.56mL

4.71mL

2.36mL

Zibotentan 技术信息

CAS号186497-07-4
分子式C19H16N6O4S
分子量 424.433
别名 ZD4054
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature
溶解度

DMSO: 25 mg/mL(58.9 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方

Tags: Zibotentan | 186497-07-4 | ZD4054 | ZD 4054 | ZD-4054 | ETA Receptor Antagonist | GPCR/G Protein | Apoptosis | Endothelin Receptor | Apoptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Zibotentan 纯度/质量文件 | Zibotentan 亚型比较 | Zibotentan 生物活性 | Zibotentan 临床数据 | Zibotentan 参考文献 | Zibotentan 实验方案 | Zibotentan 技术信息

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