Eupatilin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEupatilinCat.No.:HY-N0783CASNo.:22368-21-4分?式:C??H??O?分?量:344.32作?靶點(diǎn):PPAR;Autophagy作?通路:CellCycle/DNADamage;Autophagy儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:33.33mg/mL(96.80mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.9043mL14.5214mL29.0428mL5mM0.5809mL2.9043mL5.8085mL10mM0.2904mL1.4521mL2.9043mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.5mg/mL(7.26mM);Clearsolution1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(7.26mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.26mM);ClearsolutionBIOLOGICALACTIVITY?物活性Eupatilin從艾葉中分到的親脂性酮類化合物，PPARα的激動(dòng)劑，具有抗凋亡，抗氧化及抗炎等功效。IC50&TargetPPARα體外研究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].體內(nèi)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(23?±?2?°C),Administration[1]humidity(55?±?5%),and12?hlight/darkcycles(06:00-18:00?hlight,18:00-06:00dark).Briefly,Balb/cmicearesensitizedonday?7byasingleapplicationof20?μLof1.0%oxazoloneinamixtureofacetoneandoliveoil(4:1)totheinnerandoutersurfaceofbothears.Onday0,themouseearsarechallengedwith20?μLof0.1%oxazoloneat2-dayintervalsfor4weekspost-sensitization.ThemicearetreatedwiththeindicatedconcentrationsofEupatilin(1.5%or3.0%)twiceadayfor4weeks.Thecontrolgroupistreatedwithvehiclealone(acetoneandoliveoil[4:1]).After3weeks,themicearesacrificedandsamplesarecollected.Earsarestoredat?80?°CforRNAisolationandanalysisorimmediatelyfixedin4%formalinforhistologicalanalysis2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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