Anti-MRSA-agent-20-生命科學試劑-MCE

Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEAnti-MRSAagent20Cat.No.:HY-168705分子式: C??H??NO?S?分子量: 661.87作用靶點: Bacterial作用通路: Anti-infection儲存方式: PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Anti-MRSAagent20(Compounda4)是一種針對MRSA的抗菌劑(MIC:<0.03125μg/mL)。Anti-MRSAagent20與核糖體肽基轉(zhuǎn)移酶中心結(jié)合，通過抑制MRSA毒素合成和細菌分裂來抑制細菌生存。Anti-MRSAagent20顯著減少MRSA感染小鼠的肺部MRSA負荷并減輕肺損傷(ED50=6.48mg/kg)[1]。體外研究Anti-MRSAagent20inhibitsthegrowthofStaphylococcusaureusATCC29213,MRSAATCC43300andMRSEATCC51625,withaminimuminhibitoryconcentration(MIC)oflessthan0.03125μg/mL[1].Anti-MRSAagent20(1×MIC-6×MIC,0-24h)exhibitsinhibitoryactivityagainstMRSAintime-killkineticexperiments[1].Anti-MRSA20(21days)slowsthedevelopmentofbacterialresistancetoit,reachingaMICof8μg/mLondays17-18[1].Anti-MRSAagent20(LC50of165.0μg/mL)istoxictoHEK293andHEPG2cellsonlyinthehighconcentrationrange(>120μg/mL),andinhibitsMRSAtoxinsynthesisinthelowconcentrationrange(0.5-1μg/mL),andhasnosignificantteratogeniceffectsonzebrafishembryos[1].CellViabilityAssay[1]CellLine:MRSAConcentration:1×MIC,3×MIC,6×MICIncubationTime:24hResult:Killed99.9%ofMRSAat3×MICafter4h.Killed99.99%ofMRSAat6×MICafter12h.CellViabilityAssay[1]1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemECellLine:HEK293andHEPG2cellsConcentration:7.5,15,30,60,120,250μg/mLIncubationTime:6hResult:ShowedminortoxicitytoHEK293cellsatconcentrationsupto120μg/mL.DisplayedtoxicitytoHEPG2cellsataconcentrationof250μg/mL.體內(nèi)研究Anti-MRSAagent20(2.5-40mg/kg,i.p.,1hafterbacterialinfection)reducesthebacterialloadoflungs,attenuateslunglesions,andincreasessurvivalinMRSA-infectedmice[1].AnimalModel:MRSA-infectedmice[1]Dosage:2.5,5,10,20,40mg/kgAdministration:Intraperitonealinjection(i.p.)Result:Increasedsurvivalofmice.Reducedbacterialloadinlungsofmice.AlleviatedMRSA-inducedlunglesionssuchascongestion,hemorrhageandinflammatorycellinfiltration.REFERENCESYi,etal.Design,synthesis,andbiologicalevaluationofnovelpleuromutilinderivativeswithmethicillin-resistantStaphylococcusaureus-targetingphenollinkergroups.Europeanjournalofmedicinalchemistry,2025,282,117061.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forre