Eupatilin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEupatilinCat.No.:HY-N0783CASNo.:22368-21-4分⼦式:C₁₈H₁₆O₇分⼦量:344.32作⽤靶点:PPAR;Autophagy作⽤通路:CellCycle/DNADamage;Autophagy储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:33.33mg/mL(96.80mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.9043mL14.5214mL29.0428mL5mM0.5809mL2.9043mL5.8085mL10mM0.2904mL1.4521mL2.9043mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.26mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.26mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.26mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Eupatilin从艾叶中分到的亲脂性酮类化合物，PPARα的激动剂，具有抗凋亡，抗氧化及抗炎等功效。IC50&TargetPPARα体外研究EupatilinisaPPARαagonist.Eupatilin(10,30,100μM)suppressesIL-4expressionanddegranulationinRBL-2H3cells[1].Eupatilin(50-100μM)slightlyreducescellviabilityofHaCaTcells.Eupatilin(10,30,50,100μM)increasesPPARαtransactivationandexpressioninHaCaTcells.Eupatilin(10,30,50μM)alsosuppressesTNFα-inducedMMP-2/-9expressioninHaCaTcells.Furthermore,EupatilininhibitsTNFα-inducedp65translocation,IκBαPhosphorylation,AP-1andMAPKsignalingviaPPARα[2].Eupatilin(10-50μM)showsnocytotoxiceffectsonARPE19cells.Eupatilin(10,25,50μM)elevatescellviabilityfromoxidativestress,andinhibitsH2O2-inducedROSproductioninARPE19cells.Moreover,Eupatilin(50μM)inbibitsH2O2-inducedcellsapoptosisandpromotestheactivationofPI3K/AktpathwayinRPEcells[3].体内研究Eupatilin(1.5%or3.0%)restoresPPARαmRNAexpression,andimprovesatopicdermatitis(AD)-likesymptomsinoxazolone-inducedBalb/cmice.EupatilincausessignificantdecreaseinserumIgE,IL-4levels,oxazolone-inducedTNFα,IFNγ,IL-1β,TSLP,IL-33andIL-25mRNAexpressioninoxazolone-inducedmice.EupatilinalsoincreasesfilaggrinandloricrinmRNAexpressioninoxazolone-inducedmice[1].PROTOCOLCellAssay[3]CellviabilityisdetectedusingaMTTassay.Inbrief,aftertreatment,themediumisreplacedwithfreshmediumcontaining0.5mg/mLMTTfor4hat37°C.Then,themediumisgentlyaspiratedand150μLofDMSOisaddedtoeachwelltosolubilizetheformazancrystals.Theabsorbanceismeasuredat450nmbyamicroplatereader.Therelativecellviabilityisdefinedastheabsorbanceoftreatedwellsdividedbythatofthecontrol[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalSix-week-oldfemaleBalb/cmicearehousedunderconditionsofcontrolledtemperature(23ꢀ±ꢀ2ꢀ°C),Administration[1]humidity(55ꢀ±ꢀ5%),and12ꢀhlight/darkcycles(06:00-18:00ꢀhlight,18:00-06:00dark).Briefly,Balb/cmicearesensitizedonday−7byasingleapplicationof20ꢀμLof1.0%oxazoloneinamixtureofacetoneandoliveoil(4:1)totheinnerandoutersurfaceofbothears.Onday0,themouseearsarechallengedwith20ꢀμLof0.1%oxazoloneat2-dayintervalsfor4weekspost-sensitization.ThemicearetreatedwiththeindicatedconcentrationsofEupatilin(1.5%or3.0%)twiceadayfor4weeks.Thecontrolgroupistreatedwithvehiclealone(acetoneandoliveoil[4:1]).After3weeks,themicearesacrificedandsamplesarecollected.Earsarestoredat−80ꢀ°CforRNAisolationandanalysisorimmediatelyfixedin4%formalinforhistologicalanalysis2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•ActaPharmSinB.2021Jan;11(1):143-155.•OxidMedCellLongev.17Jan2022.•LifeSci.2020Jul15;253:117745.•IntJMolMed.2021Feb;47(2):511-522.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].JungY,etal.Eupatilin,anactivatorofPPARα,inhibitsthedevelopmentofoxazolone-inducedatopicdermatitissymptomsinBalb/cmice.BiochemBiophysResCommun.2018Feb5;496(2):508-514.[2].JungY,etal.EupatilinwithPPARαagonisticeffectsinhibitsTNFα-inducedMMPsignalinginHaCaTcells.BiochemBiophysResCommun.2017Nov4;493(1):220-226.[3].DuL,etal.EupatilinpreventsH2O2-inducedoxidativestressandapoptosisinhumanretinalpigmentepithelialcells.BiomedP