Home / PPAR alpha Receptor Antagonists / GW 6471

GW 6471

Catalog #: 4618
38 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
4618/10
4618/50
GW 6471 | CAS No. 880635-03-0 | PPAR alpha Receptor Antagonists
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Description: PPARα antagonist

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

Purity: ≥98%

Product Details
Citations (38)
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Biological Activity

GW 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.

Technical Data

M.Wt:
619.67
Formula:
C35H36F3N3O4
Solubility:
Soluble to 75 mM in DMSO and to 10 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold with the permission of GlaxoSmithKline.

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Citations for GW 6471

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

38 Citations: Showing 1 - 10

  1. Nuclear receptor modulators inhibit osteosarcoma cell proliferation and tumour growth by regulating the mTOR signaling pathway.
    Authors: Ning Et al.
    Cell Death Dis  2023;14:51
  2. Downregulation of PTEN Promotes Autophagy via Concurrent Reduction in Apoptosis in Cardiac Hypertrophy in PPAR α-/- Mice.
    Authors: Arun Et al.
    Front Cardiovasc Med  2022;9:798639
  3. Regulation of PPARα by APP in Alzheimer disease affects the pharmacological modulation of synaptic activity.
    Authors: Charles Et al.
    JCI Insight  2021;6
  4. High-fat diet-activated fatty acid oxidation mediates intestinal stemness and tumorigenicity.
    Authors: Peter Et al.
    Cell Rep  2021;35:109212
  5. Inhibition of phosphodiesterase type 9 reduces obesity and cardiometabolic syndrome in mice.
    Authors: David A Et al.
    J Clin Invest  2021;131
  6. Exposure of female mice to perfluorooctanoic acid suppresses hypothalamic kisspeptin-reproductive endocrine system through enhanced hepatic fibroblast growth factor 21 synthesis, leading to ovulation failure and prolonged dioestrus.
    Authors: Lin Et al.
    J Neuroendocrinol  2020;32:e12848
  7. TGFβ2-induced formation of lipid droplets supports acidosis-driven EMT and the metastatic spreading of cancer cells.
    Authors: Carine Et al.
    Nat Commun  2020;11:454
  8. Phytanic acid activates PPARα to promote beige adipogenic differentiation of preadipocytes.
    Authors: Min Et al.
    J Nutr Biochem  2019;67:201-211
  9. An ANGPTL4-ceramide-protein kinase Cζ axis mediates chronic glucocorticoid exposure-induced hepatic steatosis and hypertriglyceridemia in mice.
    Authors: Marc K Et al.
    J Biol Chem  2019;294:9213-9224
  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;
  11. Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis.
    Authors: Guo Et al.
    Nat Med  2018;24:360
  12. 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
  13. 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
  14. 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
  15. PPARα inhibition modulates multiple reprogrammed metabolic pathways in kidney cancer and attenuates tumor growth.
    Authors: Mark Et al.
    Am J Physiol Cell Physiol  2015;308:C890-8
  16. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent.
    Authors: Borrelli Et al.
    Lipids Health Dis  2015;172:142
  17. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals.
    Authors: Lin Et al.
    J Appl Toxicol  2015;16:5555
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. 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
  24. 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
  25. Fenofibrate induces apoptosis of triple-negative breast cancer cells via activation of NF-κB pathway.
    Authors: Li Et al.
    BMC Cancer  2014;14:96
  26. 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
  27. 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
  28. 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
  29. Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats.
    Authors: El-Sisi Et al.
    J Neuroinflammation  2013;2013:781348
  30. Activation and desensitization of TRPV1 channels in sensory neurons by the PPARα agonist palmitoylethanolamide.
    Authors: Ambrosino Et al.
    Br J Pharmacol  2013;168:1430
  31. The synthetic cannabinoid R(+)WIN55,212-2 augments interferon-β expression via peroxisome proliferator-activated receptor-α.
    Authors: Paul N Et al.
    J Biol Chem  2012;287:25440-53
  32. 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
  33. 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
  34. A metabolic prosurvival role for PML in breast cancer.
    Authors: Carracedo Et al.
    J Clin Invest  2012;122:3088
  35. Activation of peroxisome proliferator activated receptor α ameliorates ethanol induced steatohepatitis in mice.
    Authors: Kong Et al.
    PPAR Res  2012;10:246
  36. Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism.
    Authors: Hamtiaux Et al.
    PLoS One  2011;6:e26823
  37. 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
  38. 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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