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Zibotentan

Zibotentan

产品编号 T6258   CAS 186497-07-4
别名: ZD4054

Zibotentan (ZD4054) 是一种选择性的,具有口服活性的内皮素 A (ETA) 受体拮抗剂,Ki 为 13 nM。它具有抗癌作用,可研究去势抵抗性前列腺癌。

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Zibotentan Chemical Structure
Zibotentan, CAS 186497-07-4
规格 价格/CNY 货期 数量
1 mg ¥ 385 现货
2 mg ¥ 549 现货
5 mg ¥ 872 现货
10 mg ¥ 1,490 现货
25 mg ¥ 2,530 现货
50 mg 特惠询价 现货
1 mL * 10 mM (in DMSO) ¥ 959 现货
产品目录号及名称: Zibotentan (T6258)
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特惠询价: Zibotentan (T6258)
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选择批次  
纯度: 99.34%
纯度: 97.00%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Zibotentan (ZD4054) (ZD4054) is a specific Endothelin (ET)A antagonist with IC50 of 21 nM, exhibiting no activity at ETB. Phase 3.
靶点活性 ET-A:21 nM
体外活性 As Zibotentan specifically inhibits ETA-mediated antiapoptotic effects, but not ETB-mediated proapoptotic effects in human and rat smooth muscle cells, Zibotentan binds to endothelin A receptor (ETA) with high affinity with Ki of 13 nM, and has no affinity for endothelin B receptor (ETB) with IC50 of >10 μM. [1] Zibotentan treatment at 1 μM inhibits ET-1 induced mitogenic activity in ovarian carcinoma cell lines HEY and OVCA 433 secreting ET-1 and expressing ETA and ETB mRNA. [2] ZD4054 (1 μM) inhibits ET-1 induced EGFR transactivation in HEY and OVCA 433 cells. Zibotentan (1 μM) reverts ET-1 mediated epithelial-mesenchymal transition (EMT), by enhancing E-cadherin expression and promoter activity, and inhibiting vascular endothelial growth factor (VEGF) secretion and invasiveness in HEY and OVCA 433 cells. [3] Zibotentan also potently inhibits the basal and ET-1 induced cell proliferation in SKOV-3 and A-2780 cells, associated with the inhibition of AKT and p42/44MAPK phosphorylation, and with increased apoptosis through the inhibition of bcl-2 and activation of caspase-3 and poly(ADP-ribose) polymerase proteins. [4]
体内活性 Administration of Zibotentan at 10 mg/kg/day for 21 days potently inhibits the growth of HEY ovarian carcinoma xenografts in mice by 69% with no associated toxicity, which is in association with the blocking of cell proliferation evaluated by 37% inhibition of the Ki-67 expression, and the 62% inhibition of tumor-induced vascularization. Consistently, Zibotentan treatment significantly inhibits the expression of matrix metalloproteinase-2 (MMP-2) and VEGF, as well as the activation of p42/44 MAPK and EGFR, and potently enhances the expression of E-cadherin. [3]
激酶实验 Receptor-binding assays: The inhibition by Zibotentan (varying concentrations) of 125iodine-ET-1 binding to cloned human ETA is assessed using standard radioligand-binding techniques. Human recombinant ETA is expressed in mouse erythroleukaemic cells, and cell membranes prepared for competitive binding studies using 125iodine-ET-1 as the radioligand. Incubations are carried out in triplicate in the presence of Zibotentan, 100 pM to 100 μM in half-log increments, and inhibition of ET-1 binding is expressed as the geometric mean pIC50 value (concentration to inhibit 50% of binding) with a 95% confidence interval (CI). The affinity of Zibotentan for cloned human ETA is also assessed using the equation of Cheng and Prusoff to determine the equilibrium dissociation constant (Ki) in a further receptor-binding screen utilizing a greater number of concentration-response curves determined in three separate studies.
细胞实验 Cells are serum starved by incubation for 24 hours in serum-free DMEM before exposed to Zibotentan for 48 hours. After the treatment, cells are lysed and the supernatant is recovered and assayed for histone-associated DNA fragments, at 405 nm by the use of a microplate reader. For detection of early apoptotic events, floating and adherent cells are collected. Cells are double stained with FITC-conjugated Annexin V and propidium iodide using the Vybrant Apoptosis Kit and are immediately analyzed by cytofluorometric analysis.(Only for Reference)
别名 ZD4054
分子量 424.43
分子式 C19H16N6O4S
CAS No. 186497-07-4

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 23 mg/mL (54.2 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3561 mL 11.7805 mL 23.561 mL 58.9025 mL
5 mM 0.4712 mL 2.3561 mL 4.7122 mL 11.7805 mL
10 mM 0.2356 mL 1.1781 mL 2.3561 mL 5.8903 mL
20 mM 0.1178 mL 0.589 mL 1.1781 mL 2.9451 mL
50 mM 0.0471 mL 0.2356 mL 0.4712 mL 1.1781 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Morris CD, et al. Br J Cancer, 2005, 92(12), 2148-2152. 2. Rosanò L, et al. Exp Biol Med (Maywood), 2006, 231(6), 1132-113 3. Rosanò L, et al. Cancer Res, 2007, 67(13), 6351-635 4. Rosanò L, et al. Mol Cancer Ther, 2007, 6(7), 22003-201
Endothelin 1 (swine, human) acetate Avosentan Myriceric acid C Aprocitentan Ro 46-2005 Darusentan Sparsentan Atrasentan hydrochloride

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 抗癌临床化合物库 高选择性抑制剂库 抗癌药物库 经典已知活性库 GPCR靶点分子库 药物功能重定位化合物库 抗癌化合物库 已知活性化合物库 人代谢物化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Zibotentan 186497-07-4 Apoptosis GPCR/G Protein Endothelin Receptor 44MAPK ETA Inhibitor bcl-2 ZD-4054 ZD 4054 CRPC ZD4054 inhibit p42 anticancer caspase-3 inhibitor

 

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