GW 4064

  ( 15 citations )    
Product Datasheet
Catalog Number:2473
Chemical Name:3-[2-[2-Chloro-4-[[3-(2,6-dichlorophenyl)-5-(1-methylethyl)-4-isoxazolyl]methoxy]phenyl]ethenyl]benzoic acid
Product Details
Citations (15)
Reviews
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.
Technical Data
  • M.Wt:
    542.84
  • Formula:
    C28H22Cl3NO4
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
    >97
  • Storage:
    Desiccate at +4°C
  • CAS No:
    278779-30-9
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline
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Citations:

The citations listed below are publications that use Tocris products. Selected citations for GW 4064 include:

15 Citations: Showing 1 - 10
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  1. Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis.
    Authors: Kasmi
    Nat Commun  2018;9(1):1393
  2. Activation of FXR pathway does not alter glial cell function.
    Authors: Albrecht Et al.
    J Neuroinflammation  2017;14:66
  3. Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis.
    Authors: Gomez-Ospina Et al.
    J Hematol Oncol  2016;7:10713
  4. The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation
    Authors: Kim Et al.
    Scientific Reports  2016;6:37280
  5. Hormesis in Cholestatic Liver Disease; Preconditioning with Low Bile Acid Concentrations Protects against Bile Acid-Induced Toxicity.
    Authors: Verhaag Et al.
    PLoS One  2016;11:e0149782
  6. Human FXR regulates SHP expression through direct binding to an LRH-1 binding site, independent of an IR-1 and LRH-1.
    Authors: Hoeke Et al.
    PLoS One  2014;9:e88011
  7. Nutrient-sensing nuclear receptors coordinate autophagy.
    Authors: Lee Et al.
    Nature  2014;516:112
  8. Cysteine sulfinic acid decarboxylase regulation: A role for farnesoid X receptor and small heterodimer partner in murine hepatic taurine metabolism.
    Authors: Kerr Et al.
    Hepatol Res  2014;44:E218
  9. Regulation of human cytosolic sulfotransferases 1C2 and 1C3 by nuclear signaling pathways in LS180 colorectal adenocarcinoma cells.
    Authors: Rondini Et al.
    J Clin Invest  2014;42:361
  10. GW4064, a farnesoid X receptor agonist, upregulates adipokine expression in preadipocytes and HepG2 cells.
    Authors: Xin Et al.
    World J Gastroenterol  2014;20:15727
  11. 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.
    Authors: Yang Et al.
    Biochim Biophys Acta  2014;1844:1684
  12. Development of time resolved fluorescence resonance energy transfer-based assay for FXR antagonist discovery.
    Authors: Yu Et al.
    Bioorg Med Chem  2013;21:4266
  13. Impact of bile acids on the growth of human cholangiocarcinoma via FXR.
    Authors: Dai Et al.
    Drug Metab Dispos  2011;4:41
  14. Bile acid stimulates hepatocyte polarization through a cAMP-Epac-MEK-LKB1-AMPK pathway.
    Authors: Fu Et al.
    Proc Natl Acad Sci U S A  2011;108:1403
  15. 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.
    Authors: Fickert Et al.
    Am J Pathol  2009;175:2392
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