JC-171-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEJC-171Cat.No.:HY-117432CASNo.:2112809-98-8分⼦式:C₁₆H₁₇ClN₂O₅S分⼦量:384.83作⽤靶点:NOD-likeReceptor(NLR)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:250mg/mL(649.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.5986mL12.9928mL25.9855mL5mM0.5197mL2.5986mL5.1971mL10mM0.2599mL1.2993mL2.5986mL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:≥2.08mg/mL(5.40mM);Clearsolution1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE2.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.40mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性JC-171选择性的NLRP3炎症⼩体抑制剂，抑制LPS/ATP诱导的巨噬细胞释放IL-1β的IC50值为8.45μM。体外研究JC-171(0-100μM)blocksNLRP3inflammasomeactivationandIL-1βproductioninprimarymacrophagesdosedependently[1].CellViabilityAssay[1]CellLine:J774A.1murinemacrophagecellsConcentration:0-100μM.IncubationTime:0.5h(beforeLPS(1μg/mL)treatmentfor4.5h).Result:InhibitedthereleaseofIL-1βinJ774A.1cellsuponstimulationwithLPS/ATP.体内研究JC-171treatmentdelaystheprogressionandreducestheseverityofexperimentalautoimmuneencephalomyelitis(EAE)inmouse[1].AnimalModel:Miceimmunizedsubcutaneouslywith200μgMyelinoligodendrocyteglycoprotein(MOG)35–55peptideemulsifiedinCompleteFreund’sAdjuvant(CFA)onday0followedbyinjectionof200ngofpertussistoxin.Dosage:100mg/kg,10mg/kg.Administration:IPdays0,1and2;andeveryotherdaysthereafter(100mg/kg).Initiatedwhentheclinicalscoresofindividualmicehavereached1(flaccidtail),andgiveneveryotherday(10mg/kg).Result:EfficientlysuppressedEAEprogressioncomparedwithvehicletreatment.ResultedinasubstantialdecreaseinthefrequencyofMOG35–55-specificTh17cellsinthespleensandspinalcordsofEAEmice.REFERENCES[1].ChunqingGuo,etal.DevelopmentandCharacterizationofaHydroxyl-SulfonamideAnalogue,5-Chloro-N-[2-(4-hydroxysulfamoyl-phenyl)-ethyl]-2-methoxy-benzamide,asaNovelNLRP3InflammasomeInhibitorforPotentialTreatmentofMultipleSclerosis.ACSChemMcePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicat