Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEKRN5Cat.No.:HY-112126CASNo.:1800465-47-7分?式:C??H??FNO?分?量:459.47作?靶點(diǎn):NuclearFactorofactivatedTCells(NFAT)作?通路:Immunology/Inflammation儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:5mg/mL(10.88mM;ultrasonicandwarmingandheatto80°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1764mL10.8821mL21.7642mL5mM0.4353mL2.1764mL4.3528mL10mM0.2176mL1.0882mL2.1764mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:0.5mg/mL(1.09mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:0.5mg/mL(1.09mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性KRN5KRN2的衍?物，具有?服活性的T細(xì)胞激活核因?(NFAT5)的抑制劑，IC50值為750nM。KRN5有潛??于NFAT5-介導(dǎo)的慢性關(guān)節(jié)炎的研究。IC50&TargetIC50:750nM(NFAT5)[1].體外研究KRN5islesstoxicthanBBRasdeterminedbyacytotoxicityassay,hERGK+channelassay,cytochromeinhibitionassay,andlivermicrosomalmetabolicstabilitytest,whichmakesitapotentialdrugcandidate[1].KRN5ataconcentrationof1μMinhibitstheexpressionsofNFAT5,IL-6,MCP-1,andGM-CSF,whichareNFAT5targetmolecules,inRAW264.7macrophagesstimulatedwithLPS[1].體內(nèi)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