JC-171-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEJC-171Cat.No.:HY-117432CASNo.:2112809-98-8分?式:C??H??ClN?O?S分?量:384.83作?靶點:NOD-likeReceptor(NLR)作?通路:Immunology/Inflammation儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:250mg/mL(649.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.5986mL12.9928mL25.9855mL5mM0.5197mL2.5986mL5.1971mL10mM0.2599mL1.2993mL2.5986mL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，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?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：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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:≥2.08mg/mL(5.40mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(5.40mM);ClearsolutionBIOLOGICALACTIVITY?物活性JC-171選擇性的NLRP3炎癥?體抑制劑，抑制LPS/ATP誘導(dǎo)的巨噬細胞釋放IL-1β的IC50值為8.45μM。體外研究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.體內(nèi)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?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedformedicalapplicat