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Merck
CN

G5172

GW4064

≥97% (HPLC), farnesoid X receptor agonist, powder

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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关于此项目

经验公式(希尔记法):
C28H22Cl3NO4
化学文摘社编号:
分子量:
542.84
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.32
MDL number:
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产品名称

GW4064, ≥97% (HPLC)

SMILES string

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

assay

≥97% (HPLC)

form

powder

storage condition

desiccated

color

white

solubility

DMSO: 10 mg/mL, clear

storage temp.

2-8°C

Quality Level

General description

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。

Application

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

Biochem/physiol Actions

GW4064 是一种 FXR 激动剂。
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。

Features and Benefits

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

pictograms

Exclamation mark

signalword

Warning

Hazard Classifications

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

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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访问文档库

Farnesoid X receptor agonist GW4064 ameliorates lipopolysaccharide-induced ileocolitis through TLR4/MyD88 pathway related mitochondrial dysfunction in mice
Liu HM, et al.
Biochemical and Biophysical Research Communications, 490(3), 841-848 (2017)
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
Synthetic FXR Agonist GW4064 Is a Modulator of Multiple G Protein-Coupled Receptors
Singh N, et al.
Molecular Endocrinology, 28(5), 659-673 (2014)
Mingyi Liu et al.
Frontiers in pharmacology, 11, 375-375 (2020-04-16)
Berberine, a quinoline alkaloid, can be used in combination with statins to enhance hypolipidemic effects and reduce the dose and side effects of statins. The hypolipidemic effects of statins in the liver are mainly regulated by organic anion transporting polypeptides
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

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