GW 4064

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Cat.No. 2473 - GW 4064 | C28H22Cl3NO4 | CAS No. 278779-30-9
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)
Datasheet
Citations (15)
Reviews
Literature

Biological Activity

Selective, non-steroidal farnesoid X receptor (FXR) agonist (EC50 = 15 nM). 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.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Technical Data

M. Wt 542.84
Formula C28H22Cl3NO4
Storage Desiccate 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 Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
ethanol 5.43 10
DMSO 54.3 100

Preparing Stock Solutions

The following data is based on the product molecular weight 542.84. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

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

Certificate of Analysis / Product Datasheet
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References

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 insulin 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


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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

15 Citations for GW 4064

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

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

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

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

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

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

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

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

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

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

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


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