Catalog Number: 4618
Chemical Name: N-((2S)-2-(((1Z)-1-Methyl-3-oxo-3-(4-(trifluoromethyl)phenyl)prop-1-enyl)amino)-3-(4-(2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethoxy)phenyl)propyl)propanamide
Biological Activity
PPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.
Technical Data
  • M.Wt:
    619.67
  • Formula:
    C35H36F3N3O4
  • Solubility:
    Soluble to 75 mM in DMSO and to 20 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    880635-03-0
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 with the permission of GlaxoSmithKline.
Background References
  1. Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα.
    Xu et al.
    Nature, 2002;415:813
  2. An innovative method to study target protein-drug interactions by mass spectrometry.
    Muller et al.
    J.Med.Chem., 2009;52:2875
Citations:

The citations listed below are publications that use Tocris products. Selected citations for GW 6471 include:

13 Citations: Showing 1 - 10
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  1. In vitro evaluation of the effects of perfluorooctanesulfonic acid (PFOS) and perfluorooctanoic acid (PFOA) on IL-2 production in human T-cells.
    Authors: Midgett Et al.
    J Pharmacol Exp Ther 2015;35:459
  2. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    Lipids Health Dis 2015;172:142
  3. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Appl Toxicol 2015;16:5555
  4. Compromised peroxisomes in idiopathic pulmonary fibrosis, a vicious cycle inducing a higher fibrotic response via TGF-β signaling.
    Authors: Oruqaj Et al.
    Proc Natl Acad Sci U S A 2015;112:E2048
  5. Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors.
    Authors: Qian Et al.
    PLoS One 2015;10:e0143439
  6. Palmitoylethanolamide stimulates phagocytosis of Escherichia coli K1 by macrophages and increases the resistance of mice against infections.
    Authors: Redlich Et al.
    Int J Mol Sci 2014;11:108
  7. Differential regulation of the expressions of the PGC-1α splice variants, lipins, and PPARα in heart compared to liver.
    Authors: Kok Et al.
    J Lipid Res 2013;54:1662
  8. Lipids derived from virulent Francisella tularensis broadly inhibit pulmonary inflammation via toll-like receptor 2 and peroxisome proliferator-activated receptor α.
    Authors: Crane Et al.
    Clin Vaccine Immunol 2013;20:1531
  9. Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats.
    Authors: El-Sisi Et al.
    J Neuroinflammation 2013;2013:781348
  10. Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply.
    Authors: Mottillo Et al.
    J Neuroinflammation 2012;287:25038
  11. A metabolic prosurvival role for PML in breast cancer.
    Authors: Carracedo Et al.
    J Clin Invest 2012;122:3088
  12. Activation of peroxisome proliferator activated receptor α ameliorates ethanol induced steatohepatitis in mice.
    Authors: Kong Et al.
    PPAR Res 2012;10:246
  13. 5-Aminoimidazole-4-carboxyamide-ribonucleoside (AICAR)-stimulated hepatic expression of Cyp4a10, Cyp4a14, Cyp4a31, and other peroxisome proliferator-activated receptor α-responsive mouse genes is AICAR 5'-monophosphate-dependent and AMP-activated
    Authors: Bumpus and Johnson
    Br J Pharmacol 2011;339:886
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