Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEFtsZ-IN-4Cat.No.:HY-150754分?式:C??H??ClF?NO?分?量:387.81作?靶點:Bacterial作?通路:Anti-infection儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性FtsZ-IN-4?種?服有效的細胞分裂蛋?絲狀溫度敏感突變體Z(FtsZ)抑制劑，具有良好的抑活性。FtsZ-IN-4具有良好的藥物性能，對健康細胞低毒(CC50>20μg/mL)。IC50&TargetTarget:Filamentingtemperature-sensitivemutantZ(FtsZ)[1]體外研究MIC:Minimuminhibitionconcentration;MBC:Minimumbactericidalconcentration.FtsZ-IN-4(compound30)showspotentantibacterialactivitytoB.subtilisandS.aureuswithMICsof0.008-0.25μg/mL,respectively[1].FtsZ-IN-4(0.064μg/mLor0.5μg/mL;0-24h)showsrapidbactericidalpropertieswithin3h,andtheMBC/MICratiosare≤4,satisfyingCLSIstandards[1].FtsZ-IN-4(>20μg/mL;72h)exertslowcytotoxicitytowardsVerocells[1].FtsZ-IN-4(0.016μg/mL;3h)increasesthelengthoftheB.subtilisATCC9372,causesabnormalbacterialcelldivisionandleadtobacterialcelldeath[1].FtsZ-IN-4(10μg/mL;0-15min)inducesSaFtsZpolymerizationand(0-35μg/mL;30min)inhibitstheGTPaseactivityofSaFtsZinadose-dependentmanner[1].CellCytotoxicityAssay[1]CellLine:Verocells(Africangreenmonkeykidneycells)Concentration:>20μg/mLIncubationTime:72hoursResult:Exhibitedthe50%cytotoxicconcentration(CC50)>20μg/mL,muchmorethanthe1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEinhibitionofB.subtilisATCC9372(MIC=0.016μg/mL).CellProliferationAssay[1]CellLine:S.aureusATCC25923andBacillusATCC9372Concentration:1×,2×,4×,8×MIC;MIC=0.125μg/mL(S.aureus);0.016μg/mL(Bacillus)IncubationTime:3,6,12,24hoursResult:ReducedB.subtilisATCC9372andS.aureusATCC25923cellsbelowthelowestdetectablelimit(103CFU/mL)in3h.體內(nèi)研究FtsZ-IN-4(compound30)(5mg/kg;p.o.)exhibitsmoderateexposure(AUC(0-t)=544.2h*ng/mL)andanoralbioavailability(F)of61.2%inmice[1].FtsZ-IN-4(25mg/kg;i.v.)exertsgoodinvivoefficacyinmice.MurinepharmacokineticprofilesofFtsZ-IN-4[1]RouteDose(mg/kg)T1/2(h)Tmax(h)Cmax(ng/mL)AUC(0-t)(h?ng/mL)AUC(0-∞)(h?ng/mL)Vss(ng/mL)CL(mL/h/kg)F(%)i.v.10.280.083480.5177.8178.71545.55682.8/52.260.5429.3544.2559.3//61.2AnimalModel:MaleICRmice(infectedwithS.aureusATCC25923)[1]Dosage:25mg/kgAdministration:Intraperitonealinjection;0.5mLResult:Significantlyreducedthebacteriaburdenandshowedcomparableinvivoefficacywithvancomycin.REFERENCES[1].DengJ,etal.Design,synthesisandbiologicalevaluationofbiphenyl-benzamidesaspotentFtsZinhibitors.EurJMedChem.2022Sep5.239:114553.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappli