Antibacterial-agent-302-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAntibacterialagent302Cat.No.:HY-179438分⼦式:C₄₄H₇₀N₁₂O₅分⼦量:847.1作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Antibacterialagent302⼀种抗剂。Antibacterialagent302具有强效且⼴谱的抗活性。Antibacterialagent302⽆明显的溶⾎毒性和细胞毒性，且诱导耐药性的倾向较低。Antibacterialagent302通过破坏细菌细胞膜的完整性发挥其抗作⽤。Antibacterialagent302可⽤于细性⾓膜炎的研究[1]。IC50&TargetHIF-1αHIF-1α体外研究Antibacterialagent302(Compound27)showsgoodantibacterialactivityagainstbothGram-positive(S.epidermidisCMCC26069,MIC=0.39μg/mL)andGram-negative(K.pneumoniaeATCC10031,MIC=1.56μg/mL)bacteria[1].Antibacterialagent302exhibitslowhemolytictoxicitytorabbitredbloodcells(RBCs)andhighsafety[1].Antibacterialagent302(24h)showsaCC50of62.44μg/mLagainstHEK293cells,84.46μg/mLagainstNCTCclone929cells,and60.99μg/mLand61.17μg/mLagainstTHLE-2andHSC-T6cells,respectively[1].Antibacterialagent302(21days)maintainsstableMICvaluesagainstStaphylococcusaureusATCC29213andEscherichiacoliATCC25922over20generations,andisnotpronetoinducingdrugresistance[1].Antibacterialagent302(8×MIC,2h)exertsitsbactericidaleffectbydisruptingthecellmembranesofStaphylococcusaureusATCC29213,MRSANCTC10442,andEscherichiacoliATCC25922andcausesbacterialmorphologicaldamage[1].Antibacterialagent302(1-8×MIC,1h)increasesthepermeabilityofthebacterialmembranesofMRSANCTC10442andPseudomonasaeruginosaATCC9027,leadingtoleakageofcontents[1].Antibacterialagent302(1-2×MIC,1h)canincreasetheoutermembranepermeabilityofE.coliinaconcentration-dependentmanner[1].Antibacterialagent302(4×MIC,90min)upregulatesthedltB,mprF,andvraGgenesinStaphylococcus1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEaureusATCC29213by3.9-fold,3.1-fold,and4.9-fold,respectively[1].Antibacterialagent302(0.39-12.5μg/mL,24h)effectivelyinhibitsbiofilmformationinStaphylococcusaureusATCC29213andEscherichiacoliATCC25922[1].CellViabilityAssay[1]CellLine:Caco-2cellsConcentration:2.07μMIncubationTime:72hResult:SuppressedCaco-2cellmigrationwith56.29%woundclosure.CellCycleAnalysis[1]CellLine:Caco-2cellsConcentration:IncubationTime:24hand48hResult:Increasedof%Caco-2cellsinG0/G1phasefrom62.07%inthecontrolto86.36%.Reducednearly3-foldin%Caco-2cellsinbothSphaseandG2/Mphase.ApoptosisAnalysis[1]CellLine:Caco-2cellsConcentration:IncubationTime:24hand48hResult:Increased42foldintotalapoptosisIncreasedtheratioofannexinV-FITCpositiveearlyapoptoticcellsfrom0.54%to20.26%,whilstthepercentageoflateapoptoticcellsrosefrom0.22%to11%.Resultedinacombinedpercentageofearlyandlateapoptoticcellsthatsignificantlyexceededthepercentageofnecroticcells.(Earlyapoptoticcellsis20.26%,lateapoptoticcellsis11.32%,necroticcellsis3.61%).体内研究Antibacterialagent302(Compound27)(5mg/mL,topicalapplication,4-6timesdaily)showssignificantefficacyinvivoagainstkeratitisinducedbyGram-positive(S.aureus)andGram-negative(P.aeruginosa)mice,withnosignificanttoxicsymptomsobservedinthemice[1].AnimalModel:TheleftcorneasoftheC57BL/6miceaged6-8weeks(withaweightof16-18g)werescratchedwithasterileneedle.ThebacterialsuspensionsofS.aureusATCC29213orP.aeruginosaATCC9027wereadjustedtoabacterialcellconcentrationofapproximately5×107CFU/mLandthendroppedontotheinjuredcorneastoestablisha2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEcornealinfectionmodel[1].Dosage:5mg/mLAdministration:ForS.aureusinfection:Topicalapplication,starting24hoursafterinfection,fourtimesdaily(2-hourintervals)forthreeconsecutivedays.ForP.aeruginosainfection:Topicalapplication,onceevery20minutesforthefirsthourafterthefirstdose,thenonceevery2hours(atotalofsixtimesdaily)fortwoconsecutivedays.Result:ForS.aureusinfection,cornealbacterialloaddecreasedby5.56log.ForP.aeruginosainfection,bacterialloaddecreasedby2.20log.REFERENCES[1].ZhongR,etal.Rationaldesignofivacaftor-derivedantimicrobialpeptidomimetics:Membrane-targetingstrategyenhancesbroad-spectrumantimicrobialefficacyagainstMDRpathogens.EurJMedChem.2026Jan1