GW 6471

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Cat.No. 4618 - GW 6471 | C35H36F3N3O4 | CAS No. 880635-03-0
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% (HPLC)
Datasheet
Citations (24)
Reviews
Literature

Biological Activity

PPARα antagonist (IC50 = 0.24 μM). Enhances the binding affinity of the PPARα ligand-binding domain to the co-repressor proteins SMRT and NCoR.

Licensing Information

Sold with the permission of GlaxoSmithKline.

Compound Libraries

GW 6471 is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 619.67
Formula C35H36F3N3O4
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 880635-03-0
PubChem ID 446738
InChI Key TYEFSRMOUXWTDN-DYQICHDWSA-N
Smiles CC2=C(N=C(C4=CC=CC=C4)O2)CCOC(C=C1)=CC=C1C[C@@H](CNC(CC)=O)N/C(C)=C\C(C3=CC=C(C(F)(F)F)C=C3)=O

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 46.48 75
ethanol 12.39 20

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
0.75 mM 2.15 mL 10.76 mL 21.52 mL
3.75 mM 0.43 mL 2.15 mL 4.3 mL
7.5 mM 0.22 mL 1.08 mL 2.15 mL
37.5 mM 0.04 mL 0.22 mL 0.43 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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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

24 Citations for GW 6471

Citations are publications that use Tocris products. Selected citations for GW 6471 include:

Helmy et al (2015) Additive Renoprotection by Pioglitazone and Fenofibrate against Inflammatory, Oxidative and Apoptotic Manifestations of Cisplatin Nephrotoxicity: Modulation by PPARs. PLoS One 10 e0142303 PMID: 26536032

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

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

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

Carracedo et al (2012) A metabolic prosurvival role for PML in breast cancer. J Clin Invest 122 3088 PMID: 22886304

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

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

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

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

El-Sisi et al (2013) Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats. J Neuroinflammation 2013 781348 PMID: 23997763

Hamtiaux et al (2012) The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action. BMC Cancer 12 92 PMID: 22429826

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

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

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

Hamtiaux et al (2011) Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism. PLoS One 6 e26823 PMID: 22046372


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