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 ActivityPPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.
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.
Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα.
Xu et al.
An innovative method to study target protein-drug interactions by mass spectrometry.
Muller et al.
Citations for GW 6471
The citations listed below are publications that use Tocris products. Selected citations for GW 6471 include:
27 Citations: Showing 1 - 10
Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties.
Authors: Smith Et al.
Psychopharmacology (Berl) 2019;
Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis.
Authors: Guo Et al.
Nat Med 2018;24:360
Diurnal Variation in PDK4 Expression Is Associated With Plasma Free Fatty Acid Availability in People.
Authors: Yamaguchi Et al.
J Clin Endocrinol Metab 2018;103:1068
Multifaceted Mechanisms of WY-14643 to Stabilize the Blood-Brain Barrier in a Model of Traumatic Brain Injury.
Authors: Neuhaus Et al.
Front Mol Neurosci 2017;10:149
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
Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
Authors: Borrelli Et al.
Lipids Health Dis 2015;172:142
Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
Authors: Lin Et al.
J Appl Toxicol 2015;16:5555
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
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
Additive Renoprotection by pioglit. and fenofi. against Inflammatory, Oxidative and Apoptotic Manifestations of cisp. Nephrotoxicity: Modulation by PPARs.
Authors: Helmy Et al.
PLoS One 2015;10:e0142303
An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production.
Authors: Kim Et al.
Mol Cell Biol 2014;34:4368
Palmitoylethanolamide normalizes intestinal motility in a model of post-inflammatory accelerated transit: involvement of CB? receptors and TRPV1 channels.
Authors: Capasso Et al.
Br J Pharmacol 2014;171:4026
Antiplatelet activity of nifed. is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity.
Authors: Shih Et al.
Br J Pharmacol 2014;171:1490
A role for PPARα in the medial prefrontal cortex in formalin-evoked nociceptive responding in rats.
Authors: Okine Et al.
Br J Pharmacol 2014;171:1462
Fenofibrate induces apoptosis of triple-negative breast cancer cells via activation of NF-κB pathway.
Authors: Li Et al.
BMC Cancer 2014;14:96
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
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
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
Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats.
Authors: El-Sisi Et al.
J Neuroinflammation 2013;2013:781348
Activation and desensitization of TRPV1 channels in sensory neurons by the PPARα agonist palmitoylethanolamide.
Authors: Ambrosino Et al.
Br J Pharmacol 2013;168:1430
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
The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action.
Authors: Hamtiaux Et al.
BMC Cancer 2012;12:92
A metabolic prosurvival role for PML in breast cancer.
Authors: Carracedo Et al.
J Clin Invest 2012;122:3088
Activation of peroxisome proliferator activated receptor α ameliorates ethanol induced steatohepatitis in mice.
Authors: Kong Et al.
PPAR Res 2012;10:246
Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism.
Authors: Hamtiaux Et al.
PLoS One 2011;6:e26823
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
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.
Authors: Poleni Et al.
PPAR Res 2010;2010:635912
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