Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEJH-X-119-01hydrochlorideCat.No.:HY-103017分?式:C??H??ClN?O?分?量:488.93作?靶點:IRAK儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:50mg/mL(102.26mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.0453mL10.2264mL20.4528mL5mM0.4091mL2.0453mL4.0906mL10mM0.2045mL1.0226mL2.0453mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的?作液，建議您現?現配，當天使?；澄的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分?指該溶劑在您配制終溶液中的體積占?)：1.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.11mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.11mM);ClearsolutionBIOLOGICALACTIVITY?物活性JH-X-119-01hydrochloride?種有效的選擇性?介素1受體相關激酶1(IRAK1)抑制劑。JH-X-119-011/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEhydrochloride可改LPS誘導的??敗?癥[1]。IC50&TargetIRAK1體外研究Jh-X-119-01(10μM)decreasesphosphorylationofNF-κBandmRNAlevelsofIL-6andTNFαinLPS-treatedmacrophagesinvitro.Jh-X-119-01selectivelyinhibitsIRAK1phosphorylation[1].WesternBlotAnalysis[1]CellLine:RAW264.7cellsandTHP-1cellsConcentration:10μMIncubationTime:15minutesResult:DecreasedLPS(100ng/mL)-inducedphosphorylationofIκBαandNF-κB-P65.體內研究Jh-X-119-01improvessurvivalanddecreasesimmunopathiesofLPS-challengedmice.Jh-X-119-01increasessurvivalofmiceatthedoseof5mg/kgbodyweight.Survivalisfurtherimprovedwhenthedoseisincreasedto10mg/kg[1].AnimalModel:C57BL/6(20-22g,male)mice[1]Dosage:5mg/kgand10mg/kgAdministration:Intraperitoneallyinjected;5daysResult:ProtectedmicefromLPS(20mg/kg)-inducedsepsis.Survivalatday5was13.3%incontrolgroupwheresepticmiceweretreatedbyvehicle,whilethevalueswere37.5%and56.3%for5mg/kgand10mg/kg.REFERENCES[1].BinPan,etal.Selectiveinhibitionofinterleukin-1receptor-associatedkinase1ameliorateslipopolysaccharide-inducedsepsisinmice.IntImmunopharmacol.2020Aug;85:106597.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchu