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Merck
CN

G5172

Sigma-Aldrich

GW4064

≥97% (HPLC)

别名:

3-(2,6-二氯苯基)-4-(3'-羧基-2-氯代二苯乙烯-4-基)氧甲基-5-异丙基异恶唑

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About This Item

经验公式(希尔记法):
C28H22Cl3NO4
分子量:
542.84
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.32

质量水平

检测方案

≥97% (HPLC)

形式

powder

储存条件

desiccated

颜色

white

溶解性

DMSO: 10 mg/mL, clear

储存温度

2-8°C

SMILES字符串

CC(C)c1onc(c1COc2ccc(\C=C\c3cccc(c3)C(O)=O)c(Cl)c2)-c4c(Cl)cccc4Cl

InChI

1S/C28H22Cl3NO4/c1-16(2)27-21(26(32-36-27)25-22(29)7-4-8-23(25)30)15-35-20-12-11-18(24(31)14-20)10-9-17-5-3-6-19(13-17)28(33)34/h3-14,16H,15H2,1-2H3,(H,33,34)/b10-9+

InChI key

BYTNEISLBIENSA-MDZDMXLPSA-N

一般描述

GW4064是合成异恶唑,用于揭示类法尼醇X受体(FXR)的细胞结构和生理功能。是雌激素受体相关受体(ERR)激动剂。

应用

GW4064用于:
  • 研究其保护小鼠肝脏免受脂多糖(LPS)诱导炎症和细胞凋亡影响的能力
  • 研究其抑制脂多糖(LPS)引起回肠粘膜损伤的能力
  • 处理回肠外植体

生化/生理作用

GW4064 是一种 FXR 激动剂。GW4064 是孤儿核受体 FXR 的强效 (EC50 = 15 nM) 非甾体激动剂。它对其他核受体(包括高达1 mM 的 RAR)没有活性,是研究 FXR 参与多种生物活动的重要工具。

特点和优势

该化合物由GlaxoSmithKline开发。要浏览其他药物开发化合物和批准的药物/候选药物列表,单击此处

象形图

Exclamation mark

警示用语:

Warning

危险声明

危险分类

Acute Tox. 4 Oral - Aquatic Chronic 4 - Eye Irrit. 2

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable

个人防护装备

dust mask type N95 (US), Eyeshields, Gloves


分析证书(COA)

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Synthetic FXR Agonist GW4064 Is a Modulator of Multiple G Protein-Coupled Receptors
Singh N, et al.
Molecular Endocrinology, 28(5), 659-673 (2014)
Xiang Jiang et al.
Journal of autoimmunity, 90, 64-75 (2018-02-13)
Mucosal-associated invariant T (MAIT) cells are novel innate-like T cells constituting a significant proportion of circulating and hepatic T cells. Herein, we extensively examine the phenotypical and functional alterations of MAIT cells and their regulation in a cohort of 56
Sarah Farr et al.
American journal of physiology. Gastrointestinal and liver physiology, 318(4), G682-G693 (2020-02-01)
Postprandial dyslipidemia is a common feature of insulin-resistant states and contributes to increased cardiovascular disease risk. Recently, bile acids have been recognized beyond their emulsification properties as important signaling molecules that promote energy expenditure, improve insulin sensitivity, and lower fasting
Esther M Verhaag et al.
PloS one, 11(3), e0149782-e0149782 (2016-03-08)
Cholestasis is characterized by accumulation of bile acids and inflammation, causing hepatocellular damage. Still, liver damage markers are highest in acute cholestasis and drop when this condition becomes chronic, indicating that hepatocytes adapt towards the hostile environment. This may be
GW4064 attenuates lipopolysaccharide-induced hepatic inflammation and apoptosis through inhibition of the Toll-like receptor 4-mediated p38 mitogen-activated protein kinase signaling pathway in mice
Liu HM, et al.
International Journal of Molecular Medicine, 41(3), 1455-1462 (2018)

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