Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEARN14974Cat.No.:HY-103592CASNo.:1644158-57-5分?式:C??H??FN?O?分?量:404.43作?靶點:Ceramidase作?通路:MetabolicEnzyme/Protease儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數據體外實驗DMSO:50mg/mL(123.63mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4726mL12.3631mL24.7262mL5mM0.4945mL2.4726mL4.9452mL10mM0.2473mL1.2363mL2.4726mL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；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。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。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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，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沉淀、析出現象，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:1mg/mL(2.47mM);Suspendedsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1mg/mL(2.47mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性ARN14974?種酸性神經酰胺酶的抑制劑(IC50=79nM)[1]。體外研究ARN14974(20μM;24hours;SW403andRaw264.7cells)inhibitsacidceramidase(AC)inacomplexcellularenvironment,leadingtotheintendedbiochemicalresponse,thatis,increasedceramideanddecreasedsphingosinelevels[1].體內研究ARN14974(10mg/kg;i.p.;mice)causesasubstantialreductioninACactivityinmultipleorgans,includingbrain,liver,heart,lungs,andkidney[1].ARN14974(10mg/kg;i.p.)quicklyentersthebloodstreamafterasingleintraperitonealadministrationinmice,reachingamaximalplasmaconcentration,Cmax,of1767.9ng/mLanddisplayingahalf-lifetimeof458minincirculation.ARN14974(1mg/kg;i.v.)showsaCmaxandahalf-lifetimeof628ng/mLand72min,respectively[1].REFERENCES[1].PizziraniD,etal.Benzoxazolonecarboxamides:potentandsystemicallyactiveinhibitorsofintracellularacidceramidase.AngewChemIntEdEngl.2015;54(2):485-489.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.