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 ActivityGW 6471 is a PPARα antagonist (IC50 = 0.24 μM). GW 6471 enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR. GW 6471 blocks SARS-CoV-2 infection in airway organoids (EC50 = 2.1 μM) by blocking and downregulating the hypoxia inducible factor 1 subunit alpha (HIF1α) and HIF1 pathway; also reduces viral RNA. GW 6471 induces apoptosis and cell cycle arrest in kidney cancer cells.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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An innovative method to study target protein-drug interactions by mass spectrometry.
Muller et al.
Structural basis for antagonist-mediated recruitment of nuclear co-repressors by PPARα.
Xu 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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