GW 501516_317318-70-0_DataSheet_MedChemExpress

Product Data SheetPdtDtShtProduct Name:CAS No.: Cat. No.:MWt:Formula:Purity :GW 501516317318-70-0HY-10838453.50C21H18F3NO3S2>98%Solubility:DMSOMechanisms: Pathways:Cell Cycle/DNA Damage; Target:PPAR Pathways:NF-KB; Target:PPAR Biological Activity:GW501516(GSK-516; GW1516) is a potent and highly selective PPARβ/δ agonist, with EC50 of 1nM, with 1000-fold selectivity over hPPARα and hPPARγ. IC50 Value: 1 nM(EC50) Target: PPARβ/δ in vitro: GW501516 is demonstrated to be 1000-fold more selective in comparison to existingsubtypes. GW501516 increases expression of the reverse cholesterol transporter ATP-bindingcassette A1 and induces apolipoprotein A1-specific cholesterol efflux In macrophages, fibroblasts,and intestinal cells. GW501516 can regulate expression of genes involved in lipid catabolism andenergy uncoupling in skeletal muscle cells. Additionally, GW501516 is shown to block insulinresistanceandfattyacid-inducednuclearfactor-κB activation. GW 501516 reduces the IFNresistance and fatty acid-induced nuclear factor-BactivationGW501516reducestheIFNγ-induced up-regulation of TNFα and inducible NO synthase, and showed anti-inflammatory activity. in vivo: GW501516 dramatically incr...References:[1]. Barroso, Emma et al. The peroxisome proliferator-activated receptor .beta./.delta.(PPAR.beta./.delta.) agonist GW501516 prevents TNF-.alpha.-induced NF-.kappa.B activation inhumanHaCaTcellsbyreducingp65acetylationthroughAMPKandSIRT1Biochemicalhuman HaCaT cells by reducing p65 acetylation through AMPK and SIRT1. BiochemicalPharmacology (2011) Volume: 81, Issue: 4, Pages: 534-543 [2]. Ciocoiu CC, Ravna AW, Sylte I, Rustan AC, Hansen TV.Synthesis, molecular modeling studiesand biological evaluation of fluorine substituted analogs of GW 501516.Bioorg Med Chem. 2011Dec 1;19(23):6982-8. Epub 2011 Oct 17. [3]. Ciocoiu CC, Nikoli? N, Nguyen HH, Thoresen GH, Aasen AJ, Hansen TV.Synthesis and dualPPARalpha/delta agonist effects of 1,4-disubstituted 1,2,3-triazole analogues of GW 501516.Eur JMed Chem. 2010 Jul;45(7):3047-55. Epub 2010 Mar 27. [4]. Lu T, Chai Q, Yu L, d'Uscio LV, Katusic ZS, He T, Lee HC.Reactive oxygen sp...[]ygpCaution: Not fully tested. For research purposes onlyMedchemexpress LLCwww.medchemexpress.com18Wilkinson Way, Princeton, NJ 08540,USAess.com Web: www.medchemexpress.comEmail: info@medchemexpr