GW4064|278779-30-9|-陌孚医药/Medlife

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GW4064

目录号: PC14933 纯度: ≥98%

CAS No. :278779-30-9

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PC14933-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥656.60	请登录

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中文名称

GW4064

中文别名

3-(2,6-二氯苯基)-4-(3'-羧基-2-氯二苯乙烯-4-基)氧甲基-5-异丙基异恶唑;3-(2,6-二氯苯基)-4-(3''-羧基-2-氯二苯乙烯-4-基)氧甲基-5-异丙基异恶唑;3-(2,6-二氯苯基)-4-(3-羧基-2-氯二苯乙烯-4-基)氧甲基-5-异丙基异恶唑;3-[2-[2-氯-4-[[3-(2,6-二氯苯基)-5 -(1-甲基乙基)-4-异噁唑基]甲氧基]苯基]乙烯基]-苯甲酸;5,5''-二溴-[2,2‘:5',2“]三噻吩;GW4064 抑制剂

英文名称

GW4064

英文别名

GW 4064;3-(2,6-Dichlorophenyl)-4-(3'-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole;3-[2-[2-Chloro-4-[3-(2,6-dichlorophenyl)-5-isopropyl-isoxazol-4-ylMethoxy]phenyl]vinyl]benzoic acid;Benzoic acid, 3-[2-[2-chloro-4-[[3-(2,6-dichlorophenyl)-5 -(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]-;GW 4064,3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoicacid;GW-4064;3-(2,6-Dichlorophenyl)-4-(3’-carboxy-2-chlorostilben-4-yl)oxymethyl-5-isopropylisoxazole;GW4064;(E)-3-(2-chloro-4-((3-(2,6-dichlorophenyl)-5-isopropylisoxazol-4-yl)methoxy)styryl)benzoic acid;SR225WUZ0H;Benzoic acid, 3-(2-(2-chloro-4-((3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl)methoxy)phenyl)ethenyl)-;3-[2-[2-Chloro-4-[[3-(2,6-Dichlorophenyl)-5-(1-Methylethyl)-4-Isoxazolyl]Methoxy]Phenyl]Ethenyl]Benzoic Acid;3-[(E)-2-(2-Chloro-4-{[3-(2,6-Dichlorophenyl)-5-(1-Methylethyl)isoxazol-4-

Cas No.

278779-30-9

分子式

C₂₈H₂₂Cl₃NO₄

分子量

542.84

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

GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.

性状

Solid

IC50 & Target[1][2]

EC50: 65 nM (FXR)

体外研究(In Vitro)

Treatment with different concentrations of GW4064 (1, 2.5, 5, 10 μM) reduces the lipid accumulation in the cells. Concordantly, GW4064 treatment significantly represses oleic acid-induced CD36 protein levels in a dose-dependent manner. Taken together, these data indicate that prevention of hepatic lipid accumulation is likely due to an inhibition of Cd36 expression by long-term GW4064 treatment.

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

体内研究(In Vivo)

GW4064 suppresses weight gain in C57BL/6 mice fed with either a high-fat diet (HFD) or high-fat, high-cholesterol diet. GW4064 treatment of mice on HFD significantly represses diet-induced hepatic steatosis as evidenced by lower triglyceride and free fatty acid level in the liver. GW4064 markedly reduces lipid transporter CD36 expression without affecting expression of genes that are directly involved in lipogenesis. GW4064 treatment attenuates hepatic inflammation while having no effect on white adipose tissue. GW4064 (30 mg/kg) treatment results in substantial, statistically significant reductions in serum activities of ALT, AST, LDH, and ALP in the ANIT-treated rats. Serum bile acid levels are also significantly reduced by GW4064 treatment. Bilirubin levels are decreased in the GW4064-treated rats, but statistical significance is not achieved. Notably, GW4064 is much more effective in decreasing these markers of liver damage than TUDCA, which reduces only LDH levels.

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

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

参考文献

[1]. Akwabi-Ameyaw A, et al.Conformationally constrained farnesoid X receptor (FXR) agonists: Naphthoic acid-based analogs of GW 4064. Bioorg Med Chem Lett, 2008, 18(15), 4339-4343. [Information]

[2]. Ma Y, et al. Synthetic FXR agonist GW4064 prevents diet-induced hepatic steatosis and resistance. Pharm Res. 2013 May;30(5):1447-57. [Information]

[3]. Liu Y, et al. Hepatoprotection by the farnesoid X receptor agonist GW4064 in rat models of intra- and extrahepatic cholestasis. J Clin Invest. 2003 Dec;112(11):1678-87. [Information]

溶解度数据

体外研究:

DMSO : 100 mg/mL (184.22 mM; Need ultrasonic)

DMF : 100 mg/mL (184.22 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	1.8422 mL	9.2108 mL	18.4216 mL
5 mM	0.3684 mL	1.8422 mL	3.6843 mL
10 mM	0.1842 mL	0.9211 mL	1.8422 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% DMF 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
2.

建议依照次序添加每种溶剂： 10% DMF 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution
3.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
4.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.83 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.83 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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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。

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