GW 4064

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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)
Citations (18)

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
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 Data for GW 4064

Solvent Max Conc. mg/mL Max Conc. mM
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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Product Datasheets for GW 4064

Certificate of Analysis / Product Datasheet
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References for GW 4064

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

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

18 Citations for GW 4064

Citations are publications that use Tocris products. Selected citations for GW 4064 include:

Zhou et al (2018) Activation of FXR promotes intestinal metaplasia of gastric cells via SHP-dependent upregulation of the expression of CDX2. Oncol Lett 15 7617 PMID: 29849798

Hoeke et al (2014) Human FXR regulates SHP expression through direct binding to an LRH-1 binding site, independent of an IR-1 and LRH-1. PLoS One 9 e88011 PMID: 24498423

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

Dai et al (2011) Impact of bile acids on the growth of human cholangiocarcinoma via FXR. Drug Metab Dispos 4 41 PMID: 21988803

Rondini et al (2014) Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells. J Clin Invest 42 361 PMID: 24335393

Fu et al (2011) Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway. Proc Natl Acad Sci U S A 108 1403 PMID: 21220320

Fickert et al (2009) Farnesoid X receptor critically determines the fibrotic response in mice but is expressed to a low extent in human hepatic stellate cells and periductal myofibroblasts. Am J Pathol 175 2392 PMID: 19910507

Dong et al (2019) Activation of FXR by obeticholic acid induces hepatic gene expression of SR-BI through a novel mechanism of transcriptional synergy with the nuclear receptor LXR. Int J Mol Med 43 1927 PMID: 30896855

Albrecht et al (2017) Activation of FXR pathway does not alter glial cell function. J Neuroinflammation 14 66 PMID: 28351411

Verhaag et al (2016) Hormesis in Cholestatic Liver Disease; Preconditioning with Low Bile Acid Concentrations Protects against Bile Acid-Induced Toxicity. PLoS One 11 e0149782 PMID: 26950211

Yu et al (2013) Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery. Bioorg Med Chem 21 4266 PMID: 23688559

Kasmi (2018) Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis. Nat Commun 9 1393 PMID: 29643332

Kim et al (2016) The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation Scientific Reports 6 37280 PMID: 27869139

Giordano et al (2016) Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy. Sci.Rep. 6 21782 PMID: 26899873

Xin et al (2014) GW4064, a farnesoid X receptor agonist, upregulates adipokine expression in preadipocytes and HepG2 cells. World J Gastroenterol 20 15727 PMID: 25400456

Yang et al (2014) Conformational dynamics of human FXR-LBD ligand interactions studied by hydrogen/deuterium exchange mass spectrometry: insights into the antagonism of the hypolipidemic agent Z-guggulsterone. Biochim Biophys Acta 1844 1684 PMID: 24953769

Kerr et al (2014) Cysteine sulfinic acid decarboxylase regulation: A role for farnesoid X receptor and small heterodimer partner in murine hepatic taurine metabolism. Hepatol Res 44 E218 PMID: 24033844

Gomez-Ospina et al (2016) Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis. J Hematol Oncol 7 10713 PMID: 26888176

Do you know of a great paper that uses GW 4064 from Tocris? Please let us know.

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