Cyclosporin-A-Cyclosporine-A-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemECyclosporinACat.No.:HY-B0579CASNo.:59865-13-3Synonyms:CyclosporineA;CiclosporinA;CsA分⼦式:C₆₂H₁₁₁N₁₁O₁₂分⼦量:1202.61作⽤靶点:MolecularGlues;Phosphatase;ComplementSystem;Antibiotic作⽤通路:PROTAC;MetabolicEnzyme/Protease;Immunology/Inflammation;Anti-infection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:62.5mg/mL(51.97mM;Needultrasonic)Ethanol:50mg/mL(41.58mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM0.8315mL4.1576mL8.3152mL5mM0.1663mL0.8315mL1.6630mL10mM0.0832mL0.4158mL0.8315mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.08mg/mL(1.73mM);Suspendedsolution;Needultrasonic2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(1.73mM);Suspendedsolution;Needultrasonic3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(1.73mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:2.62mg/mL(2.18mM);Suspendedsolution;Needultrasonic5.请依序添加每种溶剂：cornoilSolubility:50mg/mL(41.58mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性CyclosporinA(CyclosporineA)⼀种免疫抑制剂，能与亲环素结合，抑制calcineurin活性的IC50值为7nM[3]。CyclosporinA也抑制CD11a/CD18粘附分⼦[8]。IC50&TargetIC50:7nM(calcineurin)体外研究CyclosporinAisabletobindwiththecyclophilininTcells[1].CyclosporinAworksbyformingaCyclophilin-CyclosporinAcomplextoinhibitcalcineurin[2].CyclosporinAinhibitscalcineurininstimulatedcellswithanIC50valueof7nM[3].CyclosporinAsuppressesthenucleartranslocationofNF-AT[4].CyclosporinAshowsaneffectonmitochondriaviapreventingtheMTPfromopeningwithanIC50of39nM[5].体内研究CyclosporinAhasimmunosuppressiveactivity,andisactiveviaparenteralandp.o.administrationinmice,ratandguineapigs[6].CyclosporinAcanbeusedinorgantransplantationtopreventrejection[7].PROTOCOLCellAssay[3]Immunosuppressiveagentsaredissolvedinethanolatconcentrations1000-foldmorethantheconcentrationdesiredforcelltreatments.Cells(106)aresuspendedin1mLofcompletemediuminmicrocentrifugetubes;1μLofethanoloroftheethanolicsolutionofCyclosporinAisadded,andthecellsareincubatedat37°Cfor1hr.Cellsarewashedtwicewith1mLofPBSoniceandlysedin50μLofhypotonicbuffercontaining50mMTris(pH7.5);0.1mMEGTA;1mMEDTA;0.5mMdithiothreitol;and50μgofphenylmethylsulfonylfluoride,50μgofsoybeantrypsininhibitor,5μgofleupeptin,and5μgofKiker52GpermL.Lysatesaresubjectedtothreecyclesoffreezinginliquidnitrogenfollowedbythawingat30°Candthenarecentrifugedat4°Cfor10minat12,000×g.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalRatsareimmunizedonday0i.p.with05mLandmicei.v.with02mLofa10%suspensionofwashedAdministration[6]sheeperythrocytes(SE).Toelicitasecondaryresponse,miceareboosted8-11weeksaftertheprimaryimmunizationwithani.v.injectionof0-2mLof025%washedSE(107cells).Forprolongedtreatmenttheanimalsreceiveontheaverage45mg/kgcyclosporinAdailyinthefoodduring13weeks.Theseratsare2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEimmunized5daysbeforekilling.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•NatCommun.2021May18;12(1):2915.•AdvSci(Weinh).2021Jan6;8(5):2002738.•BioactMater.2023,23：300-313•ArthritisRheumatol.2022Sep3.•ProcNatlAcadSciUSA.2021Jan12;118(2):e2009539118.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].HandschumacherRE,etal.Cyclophilin:aspecificcytosolicbindingproteinforcyclosporinA.Science.1984Nov2;226(4674):544-7.[2].LiuJ,etal.Calcineurinisacommontargetofcyclophilin-cyclosporinAandFKBP-FK506complexes.Cell.1991Aug23;66(4):807-15.[3].FrumanDA,etal.CalcineurinphosphataseactivityinTlymphocytesisinhibitedbyFK506andcyclosporinA.ProcNatlAcadSciUSA.1992May1;89(9):3686-90.[4].FlanaganWM,etal.NuclearassociationofaT-celltranscriptionfactorblockedbyFK-506andcyclosporinA.Nature.1991Aug29;352(6338):803-7.[5].NicolliA,etal.Interactionsofcyclophilinwiththemitochondrialinnermembraneandregulationofthepermeabilitytransitionpore,andcyclosporinA-sensitivechannel.JBiolChem.1996Jan26;271(4):2185-92.[6].BorelJF,etal.Effectsofthenewanti-lymphocyticpeptidecyclosporinAinanimals.Immunology.1977Jun;32(6):1017-25.[7].Williams,R,etal.RandomisedtrialcomparingFK506andcyclosporininpreventionofliverallograftrejection.EuropeanFK506MulticentreLiverStudyGroup.Lancet,1994,344(8920),423-428.[8].DalmarcoEM,etal.CyclosporinAinhibitsCD11a/CD18adhesionmoleculesduetoinhibitionofTNFalphaandIL-1betalevelsinthemousemodelofp