Laquinimod-ABR-215062-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemELaquinimodCat.No.:HY-13010CASNo.:248281-84-7Synonyms:ABR-215062分⼦式:C₁₉H₁₇ClN₂O₃分⼦量:356.8作⽤靶点:NF-κB;Apoptosis作⽤通路:NF-κB;Apoptosis储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:100mg/mL(280.27mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.8027mL14.0135mL28.0269mL5mM0.5605mL2.8027mL5.6054mL10mM0.2803mL1.4013mL2.8027mL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%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.5mg/mL(7.01mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(7.01mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Laquinimod(ABR-215062)⼀种可⼝服的羧酰胺衍⽣物，⼀种有效的免疫调节剂，可防⽌中枢神经系统的神经变性和炎症。Laquinimod减少形胶质细胞NF-κB的活化以防⽌铜酮(Cuprizone)诱导的脱髓鞘。Laquinimod具有⽤于多发性硬化症(MS；RRMS或CPMS)的复发缓解(RR)和慢性进⾏性(CP)形式以及神经退⾏性疾病研究的潜⼒。IC50&TargetNF-κB体外研究LaquinimodreversesEAEandinhibitspathogenicTcellimmuneresponses.LaquinimodreversesRR-EAEandinhibitsinflammatoryTcellresponsesviaadirecteffectonmyeloidAPC.LaquinimodaltersmyeloidAPCsubsetsandinhibitsTh1andTh17polarizationofmyelin-specificTcells.Laquinimod-inducedtypeII(M2)monocytesreverseestablishedEAE[1].LaquinimodmodulatesthephenotypeofBcellsofhealthydonors.LaquinimodmodulatesexpressionofmarkersrelatedtoregulatorycapacityinBcellsofRRMSpatients.LaquinimodreducesIFNγcytokineexpressioninCD4+Tcells[2].体内研究Laquinimodtreatmentinhibitsdonormyelin-specificTcellsfromtransferringEAEtonaiverecipientmice.Invivolaquinimodtreatmentalterssubpopulationsofmyeloidantigenpresentingcells(APC)thatincludeadecreaseinCD11c+CD11b+CD4+dendriticcells(DC)andanelevationofCD11bhiGr1himonocytes[1].PROTOCOLCellAssay[1]PurifiedCD11b+cellsfromlaquinimod-orvehicle-treatedmiceareculturedwithnaiveCD4+cellsisolatedfromlaquinimod-orvehicle-treated2D2miceandantigen(MOGp35-55,20µg/mL).Cellsareculturedin96-wellmicrotitreplatesataconcentrationof0.25×106cells/mL.CulturemediumconsistedofRPMI1640supplementedwithL-glutamine(2mM),sodiumpyruvate(1mM),penicillin(100U/mL),streptomycin(0.1mg/mL),2-mercaptoethanol(5×10-5M)and10%(v/v)fetalbovineserum.Cellsareincubatedfor48handpulsedfor18hwith1µCiperwellof[3H]-thymidinebeforeharvesting.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalSevento10-week-oldfemaleC57BL/6,DBA/1orSJL/Jmiceareinjectedsubcutaneouslywith50µgMOGAdministration[1]p35-55,50µgrMOGor100µgPLPp139-151,respectively,incompleteFreund'sadjuvant.Afterimmunizationand2dayslater,micereceive200ng(C57BL/6)or100ng(SJL/J)pertussistoxinintraperitoneally(i.p.).Foradoptivetransfer,donorSJL/Jmiceareimmunizedasdescribedaboveandtreateddailywithlaquinimodorvehicle.10dayslater,cellsfromdraininglymphnodesandspleenareisolated,re-stimulatedfor48h(20µg/mLPLPp139-151),onaiveSJL/Jrecipients(107cellspermouse).Animalsareobserveddailyandclinicalscoresareassessedasfollows:0,nosigns;1,decreasedtailtone;2,mildmonoparesisorparaparesis;3,severeparaparesis;4,paraplegiaand/or2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEquadraparesis;and5,moribundordeath.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JNeuroimmunol.2020Feb20;342:577195.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].Schulze-Topphoff,Ulf.,etal.Laquinimod,aquinoline-3-carboxamide,inducestypeIImyeloidcellsthatmodulatecentralnervoussystemautoimmunity.PLoSOne(2012),7(3),e33797.[2].ToubiE,etal.LaquinimodmodulatesBcellsandtheirregulatoryeffectsonTcellsinMultipleSclerosis.JNeuroimmunol.2012Oct15;251(1-2):45-54.[3].BrückW,etal.ReducedastrocyticNF-κBactivationbylaquinimodprotectsfromcuprizone-induceddemyelination.ActaNeuropathol.2012Sep;124(3):411-24.[4].JanThöne,etal.Laquinimodinthetreatmentofmultiplesclerosis:areviewofthedatasofar.DrugDesDevelT