KRN5-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEKRN5Cat.No.:HY-112126CASNo.:1800465-47-7分⼦式:C₂₇H₂₂FNO₅分⼦量:459.47作⽤靶点:NuclearFactorofactivatedTCells(NFAT)作⽤通路:Immunology/Inflammation储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:5mg/mL(10.88mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1764mL10.8821mL21.7642mL5mM0.4353mL2.1764mL4.3528mL10mM0.2176mL1.0882mL2.1764mL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%salineSolubility:0.5mg/mL(1.09mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:0.5mg/mL(1.09mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性KRN5KRN2的衍⽣物，具有⼝服活性的T细胞激活核因⼦(NFAT5)的抑制剂，IC50值为750nM。KRN5有潜⼒⽤于NFAT5-介导的慢性关节炎的研究。IC50&TargetIC50:750nM(NFAT5)[1].体外研究KRN5islesstoxicthanBBRasdeterminedbyacytotoxicityassay,hERGK+channelassay,cytochromeinhibitionassay,andlivermicrosomalmetabolicstabilitytest,whichmakesitapotentialdrugcandidate[1].KRN5ataconcentrationof1μMinhibitstheexpressionsofNFAT5,IL-6,MCP-1,andGM-CSF,whichareNFAT5targetmolecules,inRAW264.7macrophagesstimulatedwithLPS[1].体内研究OralfeedingofKRN5(15mg/kgand60mg/kg)everyotherdayfor3weeksfromday21dose-dependentlymitigatesarthritisseverity[1].Theconcentrationofserumanti-typeIIcollagenIgGalsosignificantlydecreasesintheseraofKRN5-treatedmice.TNF-αandIL-6productionbyLPS-stimulatedsplenocytesaresignificantlylowerinKRN5-treatedCIAmicethaninvehicle-treatedmice[1].AnimalModel:8-week-oldDBA/1JmiceimmunizedwithbovinetypeIIcollagen[1].Dosage:15mg/kgand60mg/kg.Administration:Orallyonalternatedays(everyotherday)for3weeks.Result:Dose-dependentlymitigatedarthritisseverity.REFERENCES[1].HanEJ,etal.SuppressionofNFAT5-mediatedInflammationandChronicArthritisbyNovelκB-bindingInhibitors.EBioMedicine.2017Apr;18:261-273.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For