Ertapenem-sodium-L-749345-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEErtapenemsodiumCat.No.:HY-13625CASNo.:153773-82-1Synonyms:L-749345;MK-826分⼦式:C₂₂H₂₄N₃NaO₇S分⼦量:497.5作⽤靶点:Bacterial;Antibiotic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H2O:50mg/mL(100.50mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.0101mL10.0503mL20.1005mL5mM0.4020mL2.0101mL4.0201mL10mM0.2010mL1.0050mL2.0101mL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.请依序添加每种溶剂：PBSSolubility:100mg/mL(201.01mM);Clearsolution;Needultrasonic1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Ertapenemsodium(L-749345)⼀种⼴谱的长效β-内酰胺。Ertapenemsodium对多种厌氧具有⼴谱抗活性，其MIC值为0.12μg/mL。Ertapenemsodium可⽤于⽪肤、肺、胃、⾻盆和泌尿道的细感染相关的研究[1][2]。IC50&Targetβ-lactam体外研究Ertapenemsodium(0-100μg/mLapproximately,48h)isactiveagainst99.1%ofallanaerobeswithamodeMICof0.12μg/mLandMIC90of1μg/mL,andMIC’s≥8μg/mLforB.fragilisandB.vulgatusspecies,respectively[1].CellViabilityAssay[1]CellLine:B.fragilis(ATCC25285),B.thetaiotaomicron(ATCC29741),andEubacteriumlentum(ATCC43055)Concentration:0-100μg/mLapproximatelyIncubationTime:48hResult:Inhibited99.1%ofallisolatewithamodeMICof0.12μg/mLandMIC90of1μg/mL,and98.8%oftheisolatesweresusceptibleamongtheB.fragilisgroup.体内研究Ertapenemsodium(Subcutaneousinjection,0-10mg/kg,0-120hafterinfection,S.aureusthightissueinfectionmodel)shows>3log10CFUreductionoforganismat10mg/kg,andmaintainstheactivitywith3.3and4.4log10CFUeliminatedat2mg/kg[2].Ertapenemsodium(Subcutaneousinjection,4hafterinfection,systemicinfectionmodel)isactiveagainstallgram-positiveorganisms,andisalsoactiveagainstgram-negativeorganismstestedwithED50sof[2].AnimalModel:S.aureusthightissueinfectionmodel(DBA/2mice)[2]Dosage:0.5,1,2,5,10mg/kg(givenat2,6,10,24,48,72,96,120h)Administration:Subcutaneousinjection(0.5mLafterinfection)Result:Displayed>3log10CFUreductionoforganismcomparedtonon-antibiotic-treatedcontrolsat10mg/kg.Maintainedtheactivitywith3.3and4.4log10CFUeliminatedat2mg/kg.AnimalModel:Systemicinfectionmodel(DBA/2femalemice,viralantibody-freeCD-1femalemice)[2]Dosage:0-3mg/kgapproximatelyAdministration:Subcutaneousinjection(0.5mL,beginimmediatelyand4hafterinfection)2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Showedactivityagainstallgram-positiveorganisms,andalsoram-negativeorganismstestedwithED50sof<0.25mg/kg/dose.AnimalModel:CD-1mice,rats[2]Dosage:10mg/kgapproximatelyAdministration:Intraperitonealinjection(pharmacokineticassay)Result:ExhibitedanAUC0-∞rangingfrom1.8-21.82μg•hr/mLintissueinmicefollowinga10-mg/kgi.p.dose.Exhibitedslowclearanceratewithat1/2βof3.2h,Clpof0.47mL/min/kg,AUC0-8of284.15μg•hr/mL.户使⽤本产品发表的科研⽂献•NatCommun.2022Mar2;13(1):1116.•NatCommun.2021Jul22;12(1):4461.•JAntimicrobChemother.2020Jul1;75(7):1850-1858.•BiomedResInt.2018Jul2;2018:3579832.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].KennethEAldridge.Ertapenem(MK-0826),anewcarbapenem:comparativeinvitroactivityagainstclinicallysignificantanaerobes.DiagnMicrobiolInfectDis.2002Oct;44(2):181-6.[2].CJGill,etal.Invivoactivityandpharmacokineticevaluationofanovellong-actingcarbapenemantibiotic,MK-826(L-749,345).AntimicrobAgentsChemother.1998Aug;42(8):1996-2001.McePdfHe