GW 4064

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GW 4064 | CAS No. 278779-30-9 | LXR-like Receptor Agonists
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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%

Product Details
Citations (17)
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:
Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold for research purposes under agreement from GlaxoSmithKline

Background References

  1. Nutrient-sensing nuclear receptors coordinate autophagy.
    Lee Jm, Wagner M, Xiao R et al.
    Nature.
  2. Identification of a chemical tool for the orphan nuclear receptor FXR.
    Maloney et al.
    J.Med.Chem., 2000;43:2971
  3. The farnesoid X receptor modulates adiposity and peripheral Ins sensitivity in mice.
    Cariou et al.
    J.Biol.Chem., 2006;281:11039
  4. Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice.
    Zhang et al.
    Proc.Natl.Acad.Sci.USA, 2006;103:1006

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Citations for GW 4064

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

17 Citations: Showing 1 - 10

  1. 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.
    Authors: Dong Et al.
    Int J Mol Med  2019;43:1927
  2. Macrophage-derived IL-1β/NF-κB signaling mediates parenteral nutrition-associated cholestasis.
    Authors: Kasmi
    Nat Commun  2018;9(1):1393
  3. Activation of FXR promotes intestinal metaplasia of gastric cells via SHP-dependent upregulation of the expression of CDX2.
    Authors: Zhou Et al.
    Oncol Lett  2018;15:7617
  4. Activation of FXR pathway does not alter glial cell function.
    Authors: Albrecht Et al.
    J Neuroinflammation  2017;14:66
  5. Mutations in the nuclear bile acid receptor FXR cause progressive familial intrahepatic cholestasis.
    Authors: Gomez-Ospina Et al.
    J Hematol Oncol  2016;7:10713
  6. The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation
    Authors: Kim Et al.
    Scientific Reports  2016;6:37280
  7. 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
  8. 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
  9. Nutrient-sensing nuclear receptors coordinate autophagy.
    Authors: Lee Et al.
    Nature  2014;516:112
  10. 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

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