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GW 4064

Catalog #: 2473
18 Citations Datasheet
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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 (18)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

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.

Technical Data

M.Wt:
542.84
Formula:
C28H22Cl3NO4
Solubility:
Soluble to 100 mM in DMSO
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. Bile acids PKA-dependently induce a switch of the IL-10/IL-12 ratio and reduce proinflammatory capability of human macrophages.
    Haselow K, Bode J, Wammers M, Ehlting C, Keitel V, Kleinebrecht L, Schupp A, Haussinger D, Graf D
    J Leukoc Biol, 2013;94(6):1253-64.
  3. Hepatocarcinogenesis in FXR-/- mice mimics human HCC progression that operates through HNF1alpha regulation of FXR expression.
    Liu N, Meng Z, Lou G, Zhou W, Wang X, Zhang Y, Zhang L, Liu X, Yen Y, Lai L, Forman BM, Xu Z, Xu R, Huang W
    Mol. Endocrinol., 2012;26(5):775-85.
  4. Positive regulation of osteogenesis by bile acid through FXR.
    Cho S, An J, Park H, Yang J, Choi H, Kim S, Park Y, Kim S, Yim M, Baek W, Kim J, Shin C
    J Bone Miner Res, 2013;28(10):2109-21.
  5. The transcription cofactor CRTC1 protects from aberrant hepatic lipid accumulation

    Sci Rep, 2016;6(0):37280.
  6. Identification of a chemical tool for the orphan nuclear receptor FXR.
    Maloney et al.
    J.Med.Chem., 2000;43:2971
  7. The farnesoid X receptor modulates adiposity and peripheral Ins sensitivity in mice.
    Cariou et al.
    J.Biol.Chem., 2006;281:11039
  8. Activation of the nuclear receptor FXR improves hyperglycemia and hyperlipidemia in diabetic mice.
    Zhang et al.
    Proc.Natl.Acad.Sci.USA, 2006;103:1006

Product Datasheets

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Citations for GW 4064

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

18 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. Activated FXR inhibits leptin signaling and counteracts tumor-promoting activities of cancer-associated fibroblasts in breast malignancy.
    Authors: Giordano Et al.
    Sci.Rep.  2016;6:21782
  8. 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
  9. 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
  10. Nutrient-sensing nuclear receptors coordinate autophagy.
    Authors: Lee Et al.
    Nature  2014;516:112

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