Antimicrobial-agent-34-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEAntimicrobialagent-34Cat.No.:HY-161988分?式:C??H??N?O?分?量:512.77作?靶點(diǎn):Bacterial作?通路:Anti-infection儲(chǔ)存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Antimicrobialagent-34(compound4h)?種抗劑(MIC=1–4μg/mL)，clogP值為9.14。Antimicrobialagent-34?漿穩(wěn)定性好(HC50為131.1μg/mL)，具有良好的膜選擇性(HC50/MIC為65.6)，具備快速殺能?。Antimicrobialagent-34通過(guò)破壞細(xì)細(xì)胞膜完整性，誘導(dǎo)細(xì)胞內(nèi)活性氧增加及蛋?質(zhì)和DNA泄漏，最終導(dǎo)致細(xì)死亡。Antimicrobialagent-34在??葡萄球ATCC43300感染的??敗?癥模型中，展現(xiàn)了顯著的體內(nèi)抗效?[1]。體外研究Antimicrobialagent-34canbestablypresentinhumanserum,plasmaandblood,withMBCsof16,16and32μg/mL,respectively,withoutlosingitsantimicrobialeffect[1].Antimicrobialagent-34hasthestrongestantibacterialactivityagainst6Gram-positivebacteria,withawideantibacterialspectrumandaMICrangeof1-4μg/mL.ItalsohasgoodantibacterialactivityagainstKlebsiellapneumoniaeATCC10031,UnstableBacteriaATCC19606,andEscherichiacoliATCC25922,withMICsof4,2,and4μg/mL,respectively[1].Antimicrobialagent-34(1×-16×MIC)showsrapidantibacterialactivityagainstStaphylococcusaureus,anditisdose-dependent[1].Antimicrobialagent-34(2-16mg/mL;0-24h)isdifficulttoinduceresistance.TheresistancetestofStaphylococcusaureusATCC43300undersub-MIC(1/2MIC)showsaMICchangeofonly2-4times[1].Antimicrobialagent-34(2-64mg/mL,0-20days)hasastrongabilitytoinhibitbiofilmformationanddestroypre-formedbiofilm,anditisdose-dependent[1].Antimicrobialagent-34(2-32mg/mL,0-20min)disruptesthetransmembranepotentialofS.aureus,therebyincreasingpermeabilityandeffectivelyincreasingthelevelsofROS,DNA,andproteininS.aureus[1].CellViabilityAssay[1]CellLine:StaphylococcusaureusATCC433001/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:2,4,8,16mg/mLIncubationTime:0,2,4,6,8,10,12,20,24hResult:Achieveda8.35logreduction(killing≥99.9%ofS.aureus)in4hcomparedwiththecontrol,andthekillingratewas100%after8h,whilereferencedrugvancomycinexhibiteda8.55logreductionofS.aureuswithin8hatthesameconcentration.CellViabilityAssay[1]CellLine:StaphylococcusaureusATCC43300Concentration:2,4,8,16,32,64mg/mLIncubationTime:20daysResult:InhibitedtheformationofbiofilmofStaphylococcusaureus,andtheformationofbiofilmwassignificantlyreducedwiththeincreaseofconcentration.8μg/mLeliminated26.69%oftheestablishedbiofilmofStaphylococcusaureus,andtheeradicationrateofbiofilmat64μg/mLexceeded40%.體內(nèi)研究Antimicrobialagent-34(5and10mg/kg,i.p.,continuouslyat12-hintervalsfor2days)hasastronginhibitoryeffectonGram-positivebacteriainvivo,significantlyreducingthebacterialloadintheblood,liver,kidney,spleenandotherorgansofmiceinthesepsismodelofmiceinfectedwithStaphylococcusaureusATCC43300.TNF-αandIL-6inthebloodofmicearereducedaftertreatment[1].AnimalModel:MousesepsismodelinfectedbyS.aureusATCC43300[1].Dosage:5and10mg/kg;continuouslyat12-hintervalsfor2daysAdministration:Intraperitonealinjection(i.p.)Result:Achieved1.10,1.98,2.00and2.09log(91.8%,98.9%,99.0%and99.2%)reductionsinthenumberofsurvivingbacterialcoloniesinblood,liver,spleenandkidneyby5mg/mL.Achieved,respectively,1.46,2.69,2.24and2.84log(95.9%,99.8%,99.4%and99.9%)by10mg/mL.DecreasedinthelevelofproinflammatorycytokinesincludingTNF-αandIL-6.REFERENCES[1].FangquanLiu,etal.Design,synthesisandbiologicalevaluationofamphiphilicbenzopyranderivativesaspotentantibacterialagentsagainstmultidrug-resistantbacteria.EurJMedChem.2024Nov5:277:116784.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECa