Mevastatin-Compactin-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEMevastatinCat.No.:HY-17408CASNo.:73573-88-3Synonyms:Compactin;ML236B分⼦式:C₂₃H₃₄O₅分⼦量:390.51作⽤靶点:HMG-CoAReductase(HMGCR);Bacterial;Autophagy;Apoptosis;Antibiotic作⽤通路:MetabolicEnzyme/Protease;Anti-infection;Autophagy;Apoptosis储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:250mg/mL(640.19mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5608mL12.8038mL25.6075mL5mM0.5122mL2.5608mL5.1215mL10mM0.2561mL1.2804mL2.5608mL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(protectfromlight)。-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%saline1/4MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(6.40mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(6.40mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(6.40mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Mevastatin(Compactin)第⼀个属于他汀类的HMG-CoA还原酶抑制剂。Mevastatin⼀种降脂药，可诱导细胞凋亡，将癌细胞阻滞在G0/G1期。Mevastatin还可以增加内⽪型⼀氧化氮合酶(eNOS)的mRNA和蛋⽩质⽔平。Mevastatin具有抗肿瘤活性，并可⽤于⼼⾎管疾病的研究。IC50&TargetHMG-CoAreductase[1][2]Apoptosis[1]体外研究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—您⾝边的抑制剂⼤师www.MedChemEResult:Causedadose-dependentincreaseofcellsinG0/G1andG2/Mphasesofthecellcycle.WesternBlotAnalysis[2]CellLine:Caco-2cellsConcentration:32µM,64µM,128µMIncubationTime:72hoursResult:Resultedinadown-regulationofcyclin-dependentkinases(cdk)4andcdk6aswellascyclinD1.体内研究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.户使⽤本产品发表的科研⽂献•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—您⾝边的抑制剂⼤师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].WächtershäuserA,etal.HMG-CoAreductaseinhibitormevastatinenhancesthegrowthinhibitoryeffectofbutyrateinthecolorectalcarcinomacelllineCaco-2.Carcinogenesis.2001Jul;22(7):1061-7.[4].Amin-HanjaniS,StaglianoNE,YamadaM,etal.Mevastatin,anHMG-CoAreductaseinhibitor,reducesstrokedamageandupregulatesendothelial