PAβN-dihydrochloride-MC-207-110-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPAβNdihydrochlorideCat.No.:HY-101444ACASNo.:100929-99-5Synonyms:MC-207,110dihydrochloride;Phe-Arg-β-naphthylamidedihydrochloride分⼦式:C₂₅H₃₂Cl₂N₆O₂分⼦量:519.47作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:83.33mg/mL(160.41mM;Needultrasonic)H2O:14.29mg/mL(27.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9250mL9.6252mL19.2504mL5mM0.3850mL1.9250mL3.8501mL10mM0.1925mL0.9625mL1.9250mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.00mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.00mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.00mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性PAβNdihydrochloride(MC-207110dihydrochloride)外排泵的抑制剂。体外研究PAβNincreasesthesusceptibilitiesofthethreepump-overexpressingmutantsofP.aeruginosatolevofloxacin64-fold.PAβNalsopotentiatestheactivityoflevofloxacinagainststrainPAM2391containingplasmidpAGH97withthemexXYgenesandagainstwild-typestrainPAM1020.PAβNhasaneffectonsusceptibilitiestootherantibioticsthataresubstratesofeffluxpumps.PAβNincreaseslevelsofaccumulationofeffluxpumpsubstratesinsidethecell.ItenhancestheactivityoflevofloxacinagainstclinicalisolatesofP.aeruginosa[1].PAβNreducestheMICsinnineciprofloxacin-resistantisolates,andinfourofthese,PAβNincreasesthesusceptibilitybytwofold.Moreover,PAβNrestoresciprofloxacinsusceptibilityinfiveoftheciprofloxacin-resistantisolates.Inaddition,cleareffectsofNMPontheciprofloxacinMICsareseenfor20oftheseciprofloxacin-resistantisolates[2].PAβNpermeabilizesbacterialmembranesinaconcentration-dependentmanneratlevelsbelowthosetypicallyusedincombinationstudies,andthisadditionalmodeofactionshouldbeconsideredwhenusingPAβNasacontrolforeffluxstudies[3].户使⽤本产品发表的科研⽂献•FrontCellInfectMicrobiol.2021Mar25;11:660431.•JAntimicrobChemother.2021Oct11;dkab375.•MicrobDrugResist.2020Jun;26(6):550-560.•bioRxiv.2020Apr.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].LomovskayaO,etal.IdentificationandcharacterizationofinhibitorsofmultidrugresistanceeffluxpumpsinPseudomonasaeruginosa:novelagentsforcombinationtherapy.AntimicrobAgentsChemother.2001Jan;45(1):105-16.[2].Kurin?i?M,etal.Effectsofeffluxpumpinhibitorsonerythromycin,ciprofloxacin,andtetracyclineresistanceinCampylobacterspp.isolates.MicrobDrugResist.2012Oct;18(5):492-501.[3].LamersRP,etal.Theeffluxinhibitorphenylalanine-argininebeta-naphthylamide(PAβN)permeabilizestheoutermembraneofgram-negativebacteria.PLoSOne.2013;8(3):e60666.McePdfHeight2/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasno