Mupirocin-calcium-BRL-4910A-calcium-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMupirocincalciumCat.No.:HY-B0958ACASNo.:104486-81-9Synonyms:BRL-4910Acalcium;Pseudomonicacidcalcium分?式:C??H??O?.?/?Ca分?量:520.66作?靶點:Antibiotic;Bacterial作?通路:Anti-infection儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Mupirocin(BRL-4910A,Pseudomonicacid)calcium可從Pseudomonasfluorescens中分離得到，?種有?服活性的抗?素。Mupirocincalcium通過可逆地抑制異亮氨酸轉(zhuǎn)移RNA，從?抑制細蛋?和RNA的合成?發(fā)揮抗作?。體外研究Mupirocin(BRL-4910A,Pseudomonicacid)calcium(0-100μM;48h)showsantibacterialeffectagainststaphylococci,streptococciandcertaingram-negativebacteria,withMICvaluesrangefrom0.06-0.25μg/mL(MIC50=0.12μg/mL,MIC90=0.25μg/mL)[1].Mupirocincalciumishighlybound(95%bound)tohumanserumprotein,thusresultsinactivityinhibitioninthepresenceofhumanserum[1].Mupirocincalciumapparentlyexertsitsantimicrobialactivitybyreversiblyinhibitingisoleucyl-transferRNA,therebyinhibitingbacterialproteinandRNAsynthesis[2].Mupirocincalcium(2%ointment)reducespro-inflammatorycytokinesIL-1βandIL-17level,decreasestumornecrosisfactor-alpha(TNF-α)expression,andincreasestheleavelofvascularendothelialgrowthfactor(VEGF)[4].MupirocincalciuminhibitsMS(S.epidermidisATCC12228),MR(S.epidermidis(Se56-99)),andVIR(S.epidermidis(Se43-98))withMICsof0.25,1.26,1.59mg/L[5].Note:MIC,theminimuminhibitionconcentration.CellViabilityAssay[1]CellLine:Staphylococcusaureus1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:0-100μM/mLIncubationTime:24,48hoursResult:Resultedina90to99%reductionat24h,withMICvaluesrangedfrom0.12-1.0μM/mLandMBCvaluesrangedfrom4.0-32μM/mLat48h.體內(nèi)研究MRSA:Meticillin-resistantStaphylococcusaureusMupirocin(BRL-4910A,Pseudomonicacid)calciumiswellabsorbedafteroralandparenteraladministrationbutserumantibioticconcentrationswereshort-livedasaresultofextensivedegradationtotheantibacteriallyinactivemetabolite,monicacidA[1].Mupirocincalcium(2%ointment;externaladministration;twicedaily;3-6d)decreasesthetotalbacterialloadsintheskinlesionswitheithertopicaltreatment[3].Mupirocincalcium(2%ointment;externaladministration;4d)alleviatesMRSA-infectedpressureulcersinmice[4].Mupirocincalcium(100mg/mL;s.c.;7d)exertspreventionefficacyagainstvascularprostheticgraftinfectionduetoStaphylococcusepidermidis[5].AnimalModel:MRSAskininfectionmodelinmice(10-12weeksold)[3]Dosage:2%ointmentAdministration:Externaladministration;twicedaily;3-6daysResult:Reducedthetotalbacterialloadsintheskinlesions,anddecreasedby2.0,5.1log10CFUonday3and6,respectively.AnimalModel:Diabeticpressureulcermousemodel(33.2-39.2g)[4]Dosage:2%ointmentAdministration:Externaladministration;4daysResult:Resultedlesssuperficialmatsofbacterialcolonies,andimprovedhistopathologyevaluation.AnimalModel:AdultmaleWistarrats(weight275-325g)[5]Dosage:Impregnatedwith100μgofmupirocin/mL;segments:1.5cm*1cm2Administration:Subcutaneousimplantation;7daysResult:ResultedinpreventingS.epidermidisinfectionofthegraftinaratmodelwithspontaneouslyboundtocollagen-sealedDacrongrafts.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].SutherlandR,etal.Antibacterialactivityofmupirocin(pseudomonicacid),anewantibioticfortopicaluse.AntimicrobAgentsChemother.1985Apr;27(4):495-8.[2].ParentiMA,etal.Mupirocin:atopicalantibioticwithauniquestructureandmechanismofaction.ClinPharm.1987Oct;6(10):761-70.[3].VingsboLundbergC,etal.Efficacyoftopicalandsystemicantibiotictreatmentofmeticillin-resistantStaphylococcusaureusinamurinesuperficialskinwoundinfectionmodel.IntJAntimicrobAgents.2013Sep.42(3):272-5.[4].MohammadH,AbutalebNS,DieterlyAM,LyleLT,SeleemMN.Investigatingauranofinforthetreatmentofinfecteddiabeticpressureulcersinmiceanddermaltoxicityinpigs.SciRep.2021May25;11(1):10935.[5].GiacomettiA,etal.Mupirocinprophylaxisagainstmethicillin-susceptible,methicillin-resistant,orvancomycin-intermediateStaphylococcusepidermidisvascular-graftinfection.AntimicrobAgentsChemother.2000Oct.44