product summary
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company name :
Tocris Bioscience
product type :
chemical
product name :
GW 6471
catalog :
4618
quantity :
10 mg (also 50 mg)
price :
231 USD
more info or order :
citations: 27
Reference
Smith D, Martinelli R, Besra G, Illarionov P, Szatmari I, Brazda P, et al. Identification and characterization of a novel anti-inflammatory lipid isolated from Mycobacterium vaccae, a soil-derived bacterium with immunoregulatory and stress resilience properties. Psychopharmacology (Berl). 2019;: pubmed publisher
Guo B, Huang X, Lee M, Lee S, Broxmeyer H. Antagonism of PPAR-γ signaling expands human hematopoietic stem and progenitor cells by enhancing glycolysis. Nat Med. 2018;24:360-367 pubmed publisher
Yamaguchi S, Moseley A, Almeda Valdes P, Stromsdorfer K, Franczyk M, Okunade A, et al. Diurnal Variation in PDK4 Expression Is Associated With Plasma Free Fatty Acid Availability in People. J Clin Endocrinol Metab. 2018;103:1068-1076 pubmed publisher
Neuhaus W, Kramer T, Neuhoff A, Gölz C, Thal S, Förster C. Multifaceted Mechanisms of WY-14643 to Stabilize the Blood-Brain Barrier in a Model of Traumatic Brain Injury. Front Mol Neurosci. 2017;10:149 pubmed publisher
Qian G, Fan W, Ahlemeyer B, Karnati S, Baumgart Vogt E. 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. 2015;10:e0143439 pubmed publisher
Helmy M, Helmy M, El Mas M. Additive Renoprotection by Pioglitazone and Fenofibrate against Inflammatory, Oxidative and Apoptotic Manifestations of Cisplatin Nephrotoxicity: Modulation by PPARs. PLoS ONE. 2015;10:e0142303 pubmed publisher
Oruqaj G, Karnati S, Vijayan V, Kotarkonda L, Boateng E, Zhang W, et al. 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. 2015;112:E2048-57 pubmed publisher
Lin T, Lu C, Wu C, Huang S, Wang S. Palmitoylethanolamide inhibits glutamate release in rat cerebrocortical nerve terminals. Int J Mol Sci. 2015;16:5555-71 pubmed publisher
Kim Y, Park K, Kim J, Seo H, Shin K, Lee Y, et al. An endoplasmic reticulum stress-initiated sphingolipid metabolite, ceramide-1-phosphate, regulates epithelial innate immunity by stimulating β-defensin production. Mol Cell Biol. 2014;34:4368-78 pubmed publisher
Borrelli F, Romano B, Petrosino S, Pagano E, Capasso R, Coppola D, et al. Palmitoylethanolamide, a naturally occurring lipid, is an orally effective intestinal anti-inflammatory agent. Br J Pharmacol. 2015;172:142-58 pubmed publisher
Midgett K, Peden Adams M, Gilkeson G, Kamen D. In vitro evaluation of the effects of perfluorooctanesulfonic acid (PFOS) and perfluorooctanoic acid (PFOA) on IL-2 production in human T-cells. J Appl Toxicol. 2015;35:459-65 pubmed publisher
Redlich S, Ribes S, Schütze S, Nau R. Palmitoylethanolamide stimulates phagocytosis of Escherichia coli K1 by macrophages and increases the resistance of mice against infections. J Neuroinflammation. 2014;11:108 pubmed publisher
Capasso R, Orlando P, Pagano E, Aveta T, Buono L, Borrelli F, et al. Palmitoylethanolamide normalizes intestinal motility in a model of post-inflammatory accelerated transit: involvement of CB₁ receptors and TRPV1 channels. Br J Pharmacol. 2014;171:4026-37 pubmed publisher
Shih C, Lin I, Ding J, Chen F, Chou T. Antiplatelet activity of nifedipine is mediated by inhibition of NF-κB activation caused by enhancement of PPAR-β/-γ activity. Br J Pharmacol. 2014;171:1490-1500 pubmed publisher
Li T, Zhang Q, Zhang J, Yang G, Shao Z, Luo J, et al. Fenofibrate induces apoptosis of triple-negative breast cancer cells via activation of NF-?B pathway. BMC Cancer. 2014;14:96 pubmed publisher
Okine B, Rea K, Olango W, Price J, Herdman S, Madasu M, et al. A role for PPARα in the medial prefrontal cortex in formalin-evoked nociceptive responding in rats. Br J Pharmacol. 2014;171:1462-71 pubmed publisher
El Sisi A, Hegazy S, El Khateeb E. Effects of three different fibrates on intrahepatic cholestasis experimentally induced in rats. PPAR Res. 2013;2013:781348 pubmed publisher
Crane D, Ireland R, Alinger J, Small P, Bosio C. Lipids derived from virulent Francisella tularensis broadly inhibit pulmonary inflammation via toll-like receptor 2 and peroxisome proliferator-activated receptor ?. Clin Vaccine Immunol. 2013;20:1531-40 pubmed publisher
Kok B, Dyck J, Harris T, Brindley D. Differential regulation of the expressions of the PGC-1? splice variants, lipins, and PPAR? in heart compared to liver. J Lipid Res. 2013;54:1662-77 pubmed publisher
Ambrosino P, Soldovieri M, Russo C, Taglialatela M. Activation and desensitization of TRPV1 channels in sensory neurons by the PPAR? agonist palmitoylethanolamide. Br J Pharmacol. 2013;168:1430-44 pubmed publisher
Carracedo A, Weiss D, Leliaert A, Bhasin M, de Boer V, Laurent G, et al. A metabolic prosurvival role for PML in breast cancer. J Clin Invest. 2012;122:3088-100 pubmed publisher
Mottillo E, Bloch A, Leff T, Granneman J. Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. J Biol Chem. 2012;287:25038-48 pubmed publisher
Hamtiaux L, Masquelier J, Muccioli G, Bouzin C, Feron O, Gallez B, et al. The association of N-palmitoylethanolamine with the FAAH inhibitor URB597 impairs melanoma growth through a supra-additive action. BMC Cancer. 2012;12:92 pubmed publisher
Kong L, Ren W, Li W, Zhao S, Mi H, Wang R, et al. Activation of peroxisome proliferator activated receptor alpha ameliorates ethanol induced steatohepatitis in mice. Lipids Health Dis. 2011;10:246 pubmed publisher
Hamtiaux L, Hansoulle L, Dauguet N, Muccioli G, Gallez B, Lambert D. Increasing antiproliferative properties of endocannabinoids in N1E-115 neuroblastoma cells through inhibition of their metabolism. PLoS ONE. 2011;6:e26823 pubmed publisher
Bumpus N, Johnson E. 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 pro. J Pharmacol Exp Ther. 2011;339:886-95 pubmed publisher
Poleni P, Etienne S, Velot E, Netter P, Bianchi A. 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;2010:635912 pubmed publisher
product information
brand :
Tocris
master code :
4618
SKU :
4618/10
product name :
GW 6471
description :
PPAR antagonist
target :
PPAR alpha Receptor Antagonists
category :
Small Molecules
unit size :
10 mg (also 50 mg)
purity :
98%
observed molecular weight :
619.67
url print :
?utm_source=distributor&utm_medium=referral&utm_campaign=product&utm_term=smallmolecules
details of functionality :
PPAR antagonist (IC50 = 0.24 M). Enhances the binding affinity of the PPAR ligand-binding domain to the co-repressor proteins SMRT and NCoR.
catalog number base :
4618
product keywords :
GW6471 PPAR PPARa PPARalpha PPAR peroxisome proliferator-activated receptor alpha antagonists GlaxoSmithKline gsk PPARalpha Receptors 4618,
extended description :
PPAR antagonist
chemical name text :
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
formula :
C 35 H 36 F 3 N 3 O 4
formula text :
C35H36F3N3O4
cas num :
880635-03-0
2020 USD :
220
2021 USD :
231 USD
storage :
Store at +4°C
more info or order :
company information
Tocris Bioscience
The Watkins Building
Atlantic Road
Avonmouth, Bristol
BS11 9QD
info@bio-techne.com
https://www.tocris.com
800-343-7475
headquarters: UK