GW 4064

Name: GW 4064
Brand: Tocris Bioscience
SKU: 2473

Tocris Bioscience, part of Bio-Techne | Catalog # 2473

Citations (74)

COA / SDS

Selective farnesoid X receptor (FXR) agonist

Key Product Details

Description:	Selective farnesoid X receptor (FXR) agonist
Chemical Name:	3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid
Purity:	≥97% (HPLC)
Molecular Weight:	542.84

View Full Technical Details for GW 4064

Technical Data
Citations

Biological Activity 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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data for GW 4064

M. Wt	542.84
Formula	C₂₈H₂₂Cl₃NO₄
Storage	Store at +4°C
Purity	≥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

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

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

Solubility for GW 4064

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	54.3	100

Preparing Stock Solutions for GW 4064

The following data is based on the product molecular weight 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.

Select a batch to recalculate based on the batch molecular weight:

Concentration / Solvent Volume / Mass	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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References for GW 4064

References are publications that support the biological activity of the product.

Giordano Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy. Sci.Rep. 2016 PMID: 26899873
Liu 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. 2018 PMID: 29328388
Lee Nutrient-sensing nuclear receptors coordinate autophagy. Nature 2014 PMID: 25383539
Zhang Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice. Proc.Natl.Acad.Sci.USA
Cariou The farnesoid X receptor modulates adiposity and peripheral Ins sensitivity in mice. J.Biol.Chem. 2006 PMID: 16446356
Maloney Identification of a chemical tool for the orphan nuclear receptor FXR. J.Med.Chem. 2000 PMID: 10956205