Zibotentan (ZD4054)|186497-07-4|(ZD4054)-陌孚医药/Medlife

您当前的位置：

Zibotentan (ZD4054) (Synonyms: ZD4054)

目录号: PC10662 纯度: ≥98%

CAS No. :186497-07-4

商品编号	规格	价格	会员价
PC10662-5mg	5mg	¥1528.00	请登录
PC10662-25mg	25mg	¥4586.00	请登录
PC10662-100mg	100mg	¥12485.00	请登录
PC10662-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥1961.00	请登录

Medlife所售产品仅用于科学研究（非临床研究），非药品不可食用，不可用于人体或动物的临床诊断和治疗，我们不为个人提供产品及服务。产品COA等资料，可至下方“质量控制”中下载。

加入购物车在线咨询收藏产品大包装询价

中文名称

Zibotentan (ZD4054)

中文别名

2-(4-(1,3,4-噁二唑-2-基)苯基)-N-(3-甲氧基-5-甲基吡嗪-2-基)吡啶-3-磺酰胺;N-(3-甲氧基-5-甲基-2-吡嗪基)-2-[4-(1,3,4-恶二唑-2-基)苯基]-;N-(3-甲氧基-5-甲基-2-吡嗪基)-2-[4-(1,3,4-恶二唑-2-基)苯基]-3-吡啶磺酰胺;ZIBOTENTAN (ZD4054) 250MG;ZIBOTENTAN (ZD4054);ZD4054;ZD 4054

英文名称

Zibotentan (ZD4054)

英文别名

2-(4-(1,3,4-Oxadiazol-2-yl)phenyl)-N-(3-methoxy-5-methylpyrazin-2-yl)pyridine-3-sulfonamide;Zibotentan (ZD4054);3-Pyridinesulfonamide,N-(3-methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-;N-(3-methoxy-5-methylpyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide;Zibotentan;Zd 4054;ZD-4054;ZD4054,Zibotentan;N-(3-methoxy-5-methylpyrazin-2-yl)-2-(4-[1,3,4-oxadiazol-2-yl]phenyl)pyridine-3-sulfonamide;N-(3-Methoxy-5-methyl-2-pyrazinyl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]-3-pyridinesulfonamide;ZD454;zibotentan,CID 9910224;3-Pyridinesulfonamide, N-(3-methoxy-5-methylpyrazinyl)-2-(4-(1,3,4-oxadiazol-2-yl)phenyl)-;Zd4054;Zibotentan(ZD4054)

Cas No.

186497-07-4

分子式

C₁₉H₁₆N₆O₄S

分子量

424.43

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ET_A) receptor antagonist with a K_i of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.

性状

Solid

IC50 & Target[1][2]

ET_A

13 nM (Ki)

体外研究(In Vitro)

Zibotentan potently inhibits the binding of iodine-ET-1 to cloned human ETA expressed in mouse erythroleukaemic cells, with a pIC₅₀ (concentration to inhibit 50% of binding) value of 22 nM.
Zibotentan (48 hours) treatment increases the number of early apoptotic cells in serum-starved A2780 WT cells.
Zibotentan (ZD4054; 1 μM; 24 hours) treatment shows significant inhibition of cell proliferation in serum-starved HEY, OVCA 433, SKOV-3, and A-2780 cells.
Zibotentan (ZD4054; 1 μM; 48 hours) treatment induces an increase in apoptotic cells. Zibotentan inhibits bcl-2 and activates caspase-3 and poly(ADP-ribose) polymerase proteins..
Zibotentan (ZD4054; 1 μM) decreases the endogenous ET-1-induced phosphorylation/activation of both kinases (AKT and p42/44MAPK) in HEY cells.
Zibotentan treatment also results in a reduction of ETAR-driven angiogenesis and invasive mediators, such as vascular endothelial growth factor, cyclooxygenase-1/2, and matrix metalloproteinase (MMP).

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

Cell Line:	HEY, OVCA 433, SKOV-3, and A-2780 cells
Concentration:	1 μM
Incubation Time:	24 hours
Result:	Showed significant inhibition of cell proliferation.

Apoptosis Analysis

Cell Line:	HEY and OVCA 433 cells
Concentration:	1 μM
Incubation Time:	48 hours
Result:	Induced an increase in apoptotic cells.

体内研究(In Vivo)

Zibotentan (10 mg/kg; intraperitoneal injection; daily; for 21 days) treatment significantly inhibits tumor growth in mice. And Zibotentan treatment increases E-cadherin expression.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female athymic (nu/nu) mice (4-6 week of age) injected with wild-type A2780 cells
Dosage:	10 mg/kg
Administration:	Intraperitoneal injection; daily ; for 21 days
Result:	Showed significant inhibition in tumor growth in mice.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. C D Morris, 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. [Information]

[2]. Laura Rosanò, et al. Acquisition of chemoresistance and EMT phenotype is linked with activation of the endothelin A receptor pathway in ovarian carcinoma cells. Clin Cancer Res. 2011 Apr 15;17(8):2350-60. [Information]

[3]. Laura Rosanò, et al. ZD4054, a specific antagonist of the endothelin A receptor, inhibits tumor growth and enhances paclitaxel activity in human ovarian carcinoma 体外研究 and in vivo. Mol Cancer Ther. 2007 Jul;6(7):2003-11. [Information]

溶解度数据

体外研究:

DMSO : 25 mg/mL (58.90 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.3561 mL	11.7805 mL	23.5610 mL
5 mM	0.4712 mL	2.3561 mL	4.7122 mL
10 mM	0.2356 mL	1.1781 mL	2.3561 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.89 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.89 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

相关产品

The molarity calculator equation

The dilution calculator equation