Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPAβNdihydrochlorideCat.No.:HY-101444ACASNo.:100929-99-5Synonyms:MC-207,110dihydrochloride;Phe-Arg-β-naphthylamidedihydrochloride分?式:C??H??Cl?N?O?分?量:519.47作?靶點(diǎn):Bacterial作?通路:Anti-infection儲(chǔ)存?式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:83.33mg/mL(160.41mM;Needultrasonic)H2O:14.29mg/mL(27.51mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.9250mL9.6252mL19.2504mL5mM0.3850mL1.9250mL3.8501mL10mM0.1925mL0.9625mL1.9250mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(4.00mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(4.00mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(4.00mM);ClearsolutionBIOLOGICALACTIVITY?物活性PAβNdihydrochloride(MC-207110dihydrochloride)外排泵的抑制劑。體外研究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].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?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?邊的抑制劑?師www.MedChemECaution:Producthasno