Mevastatin-Compactin-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMevastatinCat.No.:HY-17408CASNo.:73573-88-3Synonyms:Compactin;ML236B分?式:C??H??O?分?量:390.51作?靶點(diǎn):HMG-CoAReductase(HMGCR);Bacterial;Autophagy;Apoptosis;Antibiotic作?通路:MetabolicEnzyme/Protease;Anti-infection;Autophagy;Apoptosis儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:250mg/mL(640.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5608mL12.8038mL25.6075mL5mM0.5122mL2.5608mL5.1215mL10mM0.2561mL1.2804mL2.5608mL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(protectfromlight)。-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%saline1/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.5mg/mL(6.40mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.40mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性Mevastatin(Compactin)第?個(gè)屬于他汀類的HMG-CoA還原酶抑制劑。Mevastatin?種降脂藥，可誘導(dǎo)細(xì)胞凋亡，將癌細(xì)胞阻滯在G0/G1期。Mevastatin還可以增加內(nèi)?型?氧化氮合酶(eNOS)的mRNA和蛋?質(zhì)?平。Mevastatin具有抗腫瘤活性，并可?于??管疾病的研究。IC50&TargetHMG-CoAreductase[1][2]Apoptosis[1]體外研究Mevastatin(0-128μM;5days;Caco-2cells)treatmentcausesadose-dependentdecreaseincellnumber[1].Mevastatin(32-128μM;24-72hours;Caco-2cells)treatmentcausesanearlyG0/G1phaseandalateG2/Mphasecellcyclrarrest[1].Mevastatin(32-128μM;72hours;Caco-2cells)treatmentcausesadown-regulationofcyclin-dependentkinases(cdk)4andcdk6aswellascyclinD1,whilecdk2andcyclinEproteinlevelsremainedunchanged.Cellcycleinhibitorsp21andp27aresignificantlyupregulatedbyMevastatin[1].Mevastatin(16-256μM;Caco-2cells)treatmentinducesapoptosisinadose-dependentmanner[1].TreatmentofNeuro2acellswithmevastatinfor24hoursinducedneuriteoutgrowthassociatedwithup-regulationoftheneuronalmarkerproteinNeuN.Mevastatintriggersphosphorylationofthekeykinasesepidermalgrowthfactorreceptor(EGFR),ERK1/2,andAkt/proteinkinaseB.InhibitionofEGFR,PI3K,andthemitogen-activatedproteinkinasecascadeblocksMevastatin-inducedneuriteoutgrowth[4].CellViabilityAssay[2]CellLine:Caco-2cellsConcentration:0μM,8μM,16μM,32μM,64μM,128μMIncubationTime:5daysResult:Causedadose-dependentdecreaseincellnumber.CellCycleAnalysis[2]CellLine:Caco-2cellsConcentration:32μM,64μM,128μMIncubationTime:24hours,48hours,72hours2/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Causedadose-dependentincreaseofcellsinG0/G1andG2/Mphasesofthecellcycle.WesternBlotAnalysis[2]CellLine:Caco-2cellsConcentration:32μM,64μM,128μMIncubationTime:72hoursResult:Resultedinadown-regulationofcyclin-dependentkinases(cdk)4andcdk6aswellascyclinD1.體內(nèi)研究Mevastatin(2-20mg/kg;deliveredviaALZETminiosmoticpumps;daily;for7,14,or28days;wild-type129-SV/eVTAcBrmalemiceandeNOS-deficientmalemice)treatmentincreaseslevelsofendothelialnitricoxidesynthase(eNOS)mRNAandprotein,reducesinfarctsize,andimprovesneurologicaldeficitsinadose-andtime-dependentmanner[2].ThetopicalinfusionofMevastatin(2.5pmol/hr)increasesbonemass(MRL/MpJmouse)ofisograftedbonebyincreasingboneturnoverand,atleastinpart,bypromotingtheexpressionofbonemorphogeneticprotein-2(BMP-2)mRNAandreceptoractivatorofNF-κBligand(RANKL)mRNA[3].AnimalModel:Wild-type129-SV/eVTAcBrmalemiceandeNOS-deficientmalemice(18-22g)withthefilamentmodel[2]Dosage:2mg/kgor20mg/kgAdministration:Deliveredvia7-or14-dayALZETminiosmoticpumpsimplantedsubcutaneously;daily;for7,14,or28daysResult:Increasedlevelsofendothelialnitricoxidesynthase(eNOS)mRNAandprotein,reducedinfarctsize,andimprovedneurologicaldeficitsinadose-andtime-dependentmanner.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?SciChinaLifeSci.2021May27;1-21.?CellDeathDis.2020Jan13;11(1):25.?FrontCellDevBiol.2020May28;8:404.?PLoSNeglTropDis.2019Aug20;13(8):e0007681.?OncolLett.2020Sep;20(3):2855-2869.Seemorecustomervalidationsonwww.MedChemEREFERENCES3/4MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].SugazakiM,HirotaniH,EchigoS,etal.EffectsofmevastatinongraftedboneinMRL/MpJmice.ConnectTissueRes.2010Apr;51(2):105-12.[2].EvangelopoulosME,WeisJ,KrüttgenA.Mevastatin-inducedneuriteoutgrowthofneuroblastomacellsviaactivationofEGFR.JNeurosciRes.2009Jul;87(9):2138-44.[3].W?chtersh?userA,etal.HMG-CoAreductaseinhibitormevastatinenhancesthegrowthinhibitoryeffectofbutyrateinthecolorectalcarcinomacelllineCaco-2.Carcinogenesis.2001Jul;22(7):1061-7.[4].Amin-HanjaniS,StaglianoNE,YamadaM,etal.Mevastatin,anHMG-CoAreductaseinhibitor,reducesstrokedamageandupregulatesendothelial