KRN2-bromide-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKRN2bromideCat.No.:HY-112125ACASNo.:1390654-28-0分⼦式:C₂₇H₂₃BrFNO₄分⼦量:524.38作⽤靶点:NuclearFactorofactivatedTCells(NFAT)作⽤通路:Immunology/Inflammation储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:18.33mg/mL(34.96mM;Needultrasonic)H2O:1.1mg/mL(2.10mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9070mL9.5351mL19.0701mL5mM0.3814mL1.9070mL3.8140mL10mM0.1907mL0.9535mL1.9070mL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(sealedstorage,awayfrommoisture)。-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%salineSolubility:≥1.83mg/mL(3.49mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥1.83mg/mL(3.49mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥1.83mg/mL(3.49mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性KRN2bromide选择性的T细胞激活核因⼦(NFAT5)的抑制剂，IC50值为100nM。KRN2bromide有潜⼒⽤于NFAT5-介导的慢性关节炎的潜能。IC50&TargetIC50:100nM(NFAT5)[1]体外研究KRN2selectivelysuppressestheexpressionofpro-inflammatorygenes,includingNos2andIl6,withouthamperinghigh-salt-inducedNFAT5anditstargetgeneexpressions[1].KRN2dose-dependentlyinhibitstheNF-κBp65bindingtoNfat5promoter1anddirectlyblockstheinteractionbetweenNF-κBp65anditsDNAbindingsequenceintheupstreamsite(basepairs-3000to+1)ofNfat5exon1[1].体内研究KRN2(3mg/kg,i.p.,dailyfor2weeks)effectivelysuppressesAIAinwhichinnateimmunecellsplayapredominantrole[1].KRN2(3mg/kg,i.p.,daily)effectivelysuppressesCIAaswellasAIAinmice,decreasingtheproductionofpro-inflammatorycytokinesandautoantibodiesaswellasmacrophageinfiltration[1].AnimalModel:8-week-oldC57BL/6miceinjectedintradermallywith2mgofcompleteFreund'sadjuvant[1].Dosage:3mg/kg.Administration:Peritoneally(i.p.)dailyfor2weeks.Result:EffectiveinsuppressingAIA.AnimalModel:8-week-oldDBA/1JmiceimmunizedwithbovinetypeIIcollagen[1].Dosage:3mg/kg.Administration:Peritoneally(i.p.)daily.Result:EffectiveinsuppressingCIAaswellasAIAinmice,decreasingtheproductionofpro-inflammatorycytokinesandautoantibodiesaswellasmacrophageinfiltration.户使⽤本产品发表的科研⽂献•JImmunol.2021Jun1;206(11):2652-2667.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].HanEJ,etal.SuppressionofNFAT5-mediatedInflammationandChronicArthritisbyNovelκB-bindingInhibitors.EBioMedicine.2017Apr;18:261-273.McePdfHeightCaution:Producthasnotbeenfullyvalidated