Antifungal-agent-22-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAntifungalagent22Cat.No.:HY-144632CASNo.:2640054-39-1分?式:C??H??Cl?NOS分?量:446.86作?靶點(diǎn):Fungal作?通路:Anti-infection儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Antifungalagent22(compoundD16)?種潛在的?服有效的抗真藥物，其IC50值為0.5μg/mL。Antifungalagent22能穿透?腦屏障，通過(guò)破壞真細(xì)胞膜的完整性殺死C.neoformansH99細(xì)胞。Antifungalagent22具有選擇性抗隱球活性，代謝穩(wěn)定性好，細(xì)胞毒性低[1]。IC50&TargetIC50:0.5μg/mL(Fungal)[1].體外研究Antifungalagent22(compoundD16)(0-1μg/mL,24h)inhibitsergosterolbiosynthesis,whichresultsinstress-inducedupregulationofERGgenesinC.neoformansH99[1].Antifungalagent22(0-8μg/mL)effectivelyinhibitsthegrowthofC.neoformansH99(0-72h),inhibitstheformationofC.neoformansH99biofilmsinaconcentration-dependentmanner(24h)[1].Antifungalagent22(0-8μg/mL,48-72h)showsselectiveanti-Cryptococcusactivity,hasafungistaticeffect[1].Antifungalagent22(0-100μM,48h)showslowcytotoxicityagainstahumanHUVECcelllinewithanIC50of20.18μM[1].CellProliferationAssayCellLine:C.neoformansH99cells[1]Concentration:0,1,2,4,8μg/mLIncubationTime:0,4,8,12,24,48,and72hResult:AlmostcompletelyinhibitedthegrowthofC.neoformansH99at8μg/mL,remainedat1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEnearly100%inhibitionrateafter72h,hadminimumfungicidalconcentrationsof8μg/mL.CellViabilityAssayCellLine:Fungalcells(RPMI1640medium)[1]Concentration:0,0.5,1,2,4,8μg/mLIncubationTime:48,72hResult:Showedselectiveanti-Cryptococcusactivity,withIC50rangeof0.06-2μg/mLandaMIC50value(averageIC50values)of0.62μg/mL.體內(nèi)研究Antifungalagent22(D16)(15mg/kg,Intragastrically,dailyfor5days)showspotentanti-Cryptococcalefficacy[1].AnimalModel:ICRfemalemice(18-22g,4-6weeks,tailveininjectedwithC.neoformansH99cells)[1]Dosage:15mg/kgAdministration:Intragastrically,dailyfor5daysResult:Showedpotentanti-Cryptococcalefficacy,significantlyreducedthenumberofC.neoformansH99cellsinthebrainafter5days,prolongthemediansurvivaltime(14days)oftheinfectedmiceatadoseof15mg/kg.REFERENCES[1].LiW,YunZ,JiC,etal.DiscoveryofNovelSertralineDerivativesasPotentanti-CryptococcusAgents.JMedChem.2022Mar6;10.1021/acs.jmedchem.1c01845.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.For