PPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.
Sold with the permission of GlaxoSmithKline.
|Storage||Store at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 619.67. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.61 mL||8.07 mL||16.14 mL|
|5 mM||0.32 mL||1.61 mL||3.23 mL|
|10 mM||0.16 mL||0.81 mL||1.61 mL|
|50 mM||0.03 mL||0.16 mL||0.32 mL|
References are publications that support the biological activity of the product.
Xu et al (2002) Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα. Nature 415 813 PMID: 11845213
Muller et al (2009) An innovative method to study target protein-drug interactions by mass spectrometry. J.Med.Chem. 52 2875 PMID: 19379014
If you know of a relevant reference for GW 6471, please let us know.
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Keywords: GW 6471, GW 6471 supplier, GW6471, PPAR, PPARa, PPARalpha, PPARα, peroxisome, proliferator-activated, receptor, alpha, antagonists, GlaxoSmithKline, gsk, Receptors, 4618, Tocris Bioscience
21 Citations for GW 6471
Citations are publications that use Tocris products. Selected citations for GW 6471 include:
Neuhaus et al (2017) Multifaceted Mechanisms of WY-14643 to Stabilize the Blood-Brain Barrier in a Model of Traumatic Brain Injury. Front Mol Neurosci 10 149 PMID: 28603485
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
Capasso et al (2014) Palmitoylethanolamide normalizes intestinal motility in a model of post-inflammatory accelerated transit: involvement of CB? receptors and TRPV1 channels. Br J Pharmacol 171 4026 PMID: 24818658
Kim et al (2014) An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production. Mol Cell Biol 34 4368 PMID: 25312644
Okine et al (2014) A role for PPARα in the medial prefrontal cortex in formalin-evoked nociceptive responding in rats. Br J Pharmacol 171 1462 PMID: 24303983
Li et al (2014) Fenofibrate induces apoptosis of triple-negative breast cancer cells via activation of NF-κB pathway. BMC Cancer 14 96 PMID: 24529079
Shih et al (2014) Antiplatelet activity of nifedipine is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity. Br J Pharmacol 171 1490 PMID: 24730061
Ambrosino et al (2013) Activation and desensitization of TRPV1 channels in sensory neurons by the PPARα agonist palmitoylethanolamide. Br J Pharmacol 168 1430 PMID: 23083124
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
Kong et al (2012) Activation of peroxisome proliferator activated receptor α ameliorates ethanol induced steatohepatitis in mice. PPAR Res 10 246 PMID: 22208561
Poleni et al (2010) Activation of PPARs α, β/δ, and γ Impairs TGF-β1-Induced Collagens' Production and Modulates the TIMP-1/MMPs Balance in Three-Dimensional Cultured Chondrocytes. PPAR Res 2010 635912 PMID: 20981144
El-Sisi et al (2013) Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats. J Neuroinflammation 2013 781348 PMID: 23997763
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 Br J Pharmacol 339 886 PMID: 21896918
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
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
Borrelli et al (2015) Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Lipids Health Dis 172 142 PMID: 25205418
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
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
Carracedo et al (2012) A metabolic prosurvival role for PML in breast cancer. J Clin Invest 122 3088 PMID: 22886304
Do you know of a great paper that uses GW 6471 from Tocris? Please let us know.
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