GW 4064

Cat. No. 2473 18 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Selective farnesoid X receptor (FXR) agonist

化学名： 3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid

纯度： ≥97% (HPLC)

引用文献 (18)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for GW 4064

GW 4064 is a potent and selective, non-steroidal farnesoid X receptor (FXR) agonist (EC₅₀ = 15 nM). GW 4064 displays no activity at other nuclear receptors at concentrations up to 1 μM. Improves hyperglycaemia and hyperlipidemia in diabetic db/db mice. Shown to suppress autophagy in nutrient-deprived mouse hepatocytes. GW 4064 protects against lipopolysaccharide (LPS)-induced liver inflammation and apoptosis in mice. GW 4064 reduces Leptin signaling pathway activation in breast cancer cells and inhibits tumor growth in mouse xenografts.

许可信息

Sold for research purposes under agreement from GlaxoSmithKline

技术数据 for GW 4064

分子量	542.84
公式	C₂₈H₂₂Cl₃NO₄
储存	Store at +4°C
纯度	≥97% (HPLC)
CAS Number	278779-30-9
PubChem ID	9893571
InChI Key	BYTNEISLBIENSA-MDZDMXLPSA-N
Smiles	CC(C)C1=C(COC2=CC(Cl)=C(\C=C\C3=CC=CC(=C3)C(O)=O)C=C2)C(=NO1)C1=C(Cl)C=CC=C1Cl

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for GW 4064

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
溶解性	DMSO	54.3	100

制备储备液 for GW 4064

以下数据基于产品分子量 542.84。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	1.84 mL	9.21 mL	18.42 mL
5 mM	0.37 mL	1.84 mL	3.68 mL
10 mM	0.18 mL	0.92 mL	1.84 mL
50 mM	0.04 mL	0.18 mL	0.37 mL

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产品说明书 for GW 4064

分析证书/产品说明书

化学品安全技术说明书

参考文献 for GW 4064

参考文献是支持产品生物活性的出版物。

Maloney et al (2000) Identification of a chemical tool for the orphan nuclear receptor FXR. J.Med.Chem. 43 2971 PMID: 10956205

Cariou et al (2006) The farnesoid X receptor modulates adiposity and peripheral Ins sensitivity in mice. J.Biol.Chem. 281 11039 PMID: 16446356

Zhang et al (2006) Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc.Natl.Acad.Sci.USA 103 1006

Lee et al (2014) Nutrient-sensing nuclear receptors coordinate autophagy. Nature 516 112 PMID: 25383539

Liu et al (2018) GW4064 attenuates lipopolysaccharide induced hepatic inflammation and apoptosis through inhibition of the Toll like receptor 4 mediated p38 mitogen activated protein kinase signalling pathway in mice. Int.J.Mol.Med. 41 1455 PMID: 29328388

Giordano et al (2016) Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy. Sci.Rep. 2 21782 PMID: 26899873

If you know of a relevant reference for GW 4064, please let us know.

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关键词: GW 4064, GW 4064 supplier, Selective, farnesoid, X, receptor, FXR, agonists, Receptors, Liver, LXR-like, GW4064, GlaxoSmithKline, GSK, Autophagy, 2473, Tocris Bioscience