Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAntibacterialagent237Cat.No.:HY-162818分?式:C??H??Cl?N??RuS?分?量:1261.87作?靶點:Bacterial;ReactiveOxygenSpecies作?通路:Anti-infection;Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Antibacterialagent237(compoundRu-8)??葡萄球的抑劑，MIC為0.78-1.56μg/mL。Antibacterialagent237通過破壞細細胞膜，改變其通透性，誘導細產?活性氧，導致細死亡且不引起耐藥性。Antibacterialagent237對兔紅細胞和Raw264.7細胞有較低溶?毒性，在???膚創感染模型和?蠟桿幼?感染模型中，對??葡萄球有顯著抗作?[1]。體外研究Antibacterialagent237hasantibacterialeffectsonS.aureusNewman,S.aureusATCC29213,Methicillin-resistantS.aureusATCC33591,E.coli25922,andPAO1,withMICsof0.78μg/mL,1.56μg/mL,1.56μg/mL,100μg/mL,and50μg/mL[1].Antibacterialagent237stillmaintainstheactivityofinhibitingS.aureusNewmanathighsaltconcentrations,withaMICof0.78μg/mL,andremainsstableinmammalianbodyfluids(serum,plasmaandblood)[1].Antibacterialagent237(0-4.68μg/mL,0-120min)cankillS.aureusNewmanefficientlyandquickly,andisconcentration-dependent,effectivelyavoidingthedevelopmentofdrugresistance[1].Antibacterialagent237(0-49.92μg/mL,24h)canremoveS.aureusNewmanbiofilmsinadose-dependentmanner[1].Antibacterialagent237(0.39μg/mL,5-6h)isnotlikelytoinduceS.aureusNewmanresistance[1].Antibacterialagent237(0.78-4.68μg/mL,0-6h)destroysS.aureusNewmancellmembranes,producesROS,causesbacterialcontentstoleak,andleadstobacterialdeath[1].Antibacterialagent237(0-100μg/mL,24h)hasakillingeffectonS.aureusNewmananddoesnotdamagenormalcells[1].CellViabilityAssay[1]CellLine:S.aureusNewman1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:0,1.56,3.12,4.68μg/mL;0,0.78,1.56,3.12,6.24,12.48,24.96,49.92μg/mL;0.39μg/mL;0.78,1.56,3.12,4.68μg/mL;0-100μg/mLIncubationTime:0,30,60,90,120min;24h;5-6h;0-6hResult:KilledS.aureusNewmanwithin2hoursataconcentrationof6×MIC.Didnotsignificantlyremovethebiofilmat1×MIC(0.78μg/mL),whereaswhentheconcentrationincreasedto16×MIC(12.48μg/mL),thebiofilmremovaleffectdecreasedby60%.DidnotchangethesensitivityofS.aureusNewmanandshowednoobviousresistancetootherantibiotics.Disruptedthecellmembrane,causingROStoaccumulate.CellCytotoxicityAssay[1]CellLine:RAW264.7Concentration:0,6.25,12.5,25,50,100μg/mLIncubationTime:24hResult:Hadakillingeffectonbacteriawithoutdamagingnormalcellsandhadgoodbiocompatibility.Immunofluorescence[1]CellLine:S.aureusNewmanConcentration:4.68μg/mLIncubationTime:2hResult:Showedstrongredfluorescence,indicatingthatithadtheabilitytodestroybacterialcellmembranesandhadaconcentration-dependentdepolarization.體內研究Antibacterialagent237(0-256mg/kg,injectedatthesecondpairofventralpediclesofthetail)showedgooddrugsafetyintheC.aureuslarvaemodelandhadagoodtherapeuticeffectonC.aureuslarvaeinfectioninvivo[1].Antibacterialagent237(50,100μg/mL,appliedwithsterilecream)hasagoodtherapeuticeffectonthemousemodelofS.aureusNewmaninfection[1].AnimalModel:Largewaxborerlarvae;G.mellonellalarvaemodel[1]Dosage:0,32,64,128,256mg/kg;128,256mg/kgAdministration:Injectatthesecondpairofabdominalfeetinthetail2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Showedconcentrationwas32mg/kg,thesurvivalrateofthelarvaeofBacilluswaxiiwas100%,andevenwhenitwasincreasedto256mg/kg,thesurvivalrateofthelarvaeofBacilluswaxiiwasstill75%.Showedconcentrationwas128mg/kg,thesurvivalrateofthelarvaeofBacilluswaxiiwas75%,andwhenthedosewasincreasedto256mg/kg,thesurvivalrateofthelarvaeofBacilluswaxiiincreasedby10%.AnimalModel:Amousebackwoundinfectionmodel[1]Dosage:50and100μg/mLAdministration:ApplyResult:Healedwoundsandreducedbacterialcontentinwounds.REFERENCES[1].WeiDeng,etal.Discoveryofquaternizedpyridine-thiazole-rutheniumcomplexesaspotentanti-Staphylococcusaureusagents.EurJMedChem.2024Nov5:277:1