Cat. No. 4618
Chemical Name: N-((2S)-2-(((1Z)-1-Methyl-3-oxo-3-(
Biological ActivityPPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.
Licensing InformationSold with the permission of GlaxoSmithKline.
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.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Muller et al (2009) An innovative method to study target protein-drug interactions by mass spectrometry. J.Med.Chem. 52 2875. PMID: 19379014.
Xu et al (2002) Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα. Nature 415 813. PMID: 11845213.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for GW 6471 include:
Borrelli et al (2015) Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Lipids Health Dis 172 142. PMID: 25205418.
Lin et al (2015) Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. J Appl Toxicol 16 5555. PMID: 25768340.
Midgett et al (2015) In vitro evaluation of the effects of perfluorooctanesulfonic acid (PFOS) and perfluorooctanoic acid (PFOA) on IL-2 production in human T-cells. J Pharmacol Exp Ther 35 459. PMID: 25056757.
Oruqaj et al (2015) Compromised peroxisomes in idiopathic pulmonary fibrosis, a vicious cycle inducing a higher fibrotic response via TGF-β signaling. Proc Natl Acad Sci U S A 112 E2048. PMID: 25848047.
Qian et al (2015) Peroxisomes in Different Skeletal Cell Types during Intramembranous and Endochondral Ossification and Their Regulation during Osteoblast Differentiation by Distinct Peroxisome Proliferator-Activated Receptors. PLoS One 10 e0143439. PMID: 26630504.
Redlich et al (2014) Palmitoylethanolamide stimulates phagocytosis of Escherichia coli K1 by macrophages and increases the resistance of mice against infections. Int J Mol Sci 11 108. PMID: 24927796.
Crane et al (2013) Lipids derived from virulent Francisella tularensis broadly inhibit pulmonary inflammation via toll-like receptor 2 and peroxisome proliferator-activated receptor α. Clin Vaccine Immunol 20 1531. PMID: 23925884.
El-Sisi et al (2013) Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats. J Neuroinflammation 2013 781348. PMID: 23997763.
Kok et al (2013) Differential regulation of the expressions of the PGC-1α splice variants, lipins, and PPARα in heart compared to liver. J Lipid Res 54 1662. PMID: 23505321.
Carracedo et al (2012) A metabolic prosurvival role for PML in breast cancer. J Clin Invest 122 3088. PMID: 22886304.
Kong et al (2012) Activation of peroxisome proliferator activated receptor α ameliorates ethanol induced steatohepatitis in mice. PPAR Res 10 246. PMID: 22208561.
Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. J Neuroinflammation 287 25038. PMID: 22685301.
Bumpus and Johnson (2011) 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 protein kinase-independent. Br J Pharmacol 339 886. PMID: 21896918.
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Keywords: GW 6471, supplier, GW6471, PPAR, PPARa, PPARalpha, PPARα, peroxisome, proliferator-activated, receptor, alpha, antagonists, GlaxoSmithKline, gsk, Tocris Bioscience, PPARα Antagonist products
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