Hotline:400-820-3792
Inhibitors?ScreeningLibraries?Proteins
www.MedChemE
PPARαagonist5
Cat.No.:HY-173217
分?式:C??H??O?
分?量:368.42
作?靶点:PPAR;Phosphatase
作?通路:CellCycle/DNADamage;MetabolicEnzyme/Protease;Vitamin
DRelated/NuclearReceptor
储存?式:Pleasestoretheproductundertherecommendedconditionsin
theCertificateofAnalysis.
BIOLOGICALACTIVITY
?物活性PPARαagonist5是?种?服有效选择性PPARα部分激动剂(EC50:3nM)。PPARαagonist5减少脂质积累
并上调PPARα靶基因，发挥抗脂肪肝作?。PPARαagonist5还通过部分PPARγ激动活性和对蛋?酪氨酸
磷酸酶1B(PTP1B)的轻度抑制(IC50:79.1μM)，表现出显著的降?脂和降?糖作?。PPARαagonist5具有
良好的安全性，可?于?脂异常的2型糖尿病的研究[1]。
IC50TargetPPARαPPAR-γPPARδ
3nM(EC50)1.66μM(EC50)25μM(EC50)
体外研究PPARαagonist5(Compound(S)-2)selectivelyagonizesPPARαinHepG2cells(EC50:3nM),is
approximately550-foldmoreactiveagainstPPARαthanagainstPPARγ(EC50:1.66μM),andhasno
significantactivityagainstPPARδ[1].
PPARαagonist5(0.025-25μM,24h/15days)significantlyreduceslipidaccumulationinducedbyoleicacid
inHepaRGcellsandupregulatedPPARαtargetgenesassociatedwithfattyacidoxidation,indicatingth