Avibactam-sodium-NXL-104-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAvibactamsodiumCat.No.:HY-14879ACASNo.:1192491-61-4Synonyms:NXL-104分⼦式:C₇H₁₀N₃NaO₆S分⼦量:287.23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(174.08mM;Needultrasonic)DMSO:≥30mg/mL(104.45mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.4815mL17.4077mL34.8153mL5mM0.6963mL3.4815mL6.9631mL10mM0.3482mL1.7408mL3.4815mL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)1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE1.请依序添加每种溶剂：1%DMSO>>99%salineSolubility:≥0.55mg/mL(1.91mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥2.08mg/mL(7.24mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(7.24mM);Clearsolution4.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.75mg/mL(9.57mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.75mg/mL(9.57mM);Clearsolution6.请依序添加每种溶剂：PBSSolubility:140mg/mL(487.41mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Avibactamsodium(NXL-104)⼀种共价的、可逆的⾮β-内酰胺β-内酰胺酶抑制剂(β-lactamase)抑制剂，抑制β-lactamaseTEM-1和CTX-M-15，IC50分别为8nM和5nM。IC50&TargetIC50:5nM(CTX-M-15),8nM(TEM-1)[1]体外研究Avibactamisamoleculewithlittleantibacterialactivity,thatinhibitsclassAandCβ-lactamases,butnotmetallotypesandAcinetobacterOXAcarbapenemases[2].Ceftazidime(HY-B0593)-Avibactam(0-256mg/L)inhibits16blaKPC-2positiveand1ofblaOXA-232positiveKlebsiellapneumoniagrowthwithMIC50andMIC90forboth8ꢀmg/L[4].体内研究Ceftazidime-Avibactam(0.375ꢀmg/g;s.c.;q8hfor10days)hasasignificanteffectonthebacteriaandledtoacertaintherapeuticefficacyinK.pneumoniaestrainY8infectedmousemodel[3].Avibactam(64mg/kg;s.c.;once)showsmeanestimatedhalf-lifeinplasmaintheterminalphaseof0.24hinPseudomonasaeruginosainfectedneutropenicmicewithlunginfection[3].AnimalModel:Six-week-oldBALB/cmice(female),K.pneumoniaestrainY8infectionmodel[4]Dosage:0.375ꢀmg/gincombinationwithCeftazidimeAdministration:Subcutaneousinjection,4ꢀhpostinfectionandgivenevery8ꢀhfor10ꢀdaysResult:70%ofinfectiongroupmicediedwithin4ꢀdays,andallmiceinthePBSgroupdiedwithin13ꢀdays.Alltreatmentgroupmicesurvivedat10dayspostinfectionwiththeantibioticappliedevery8ꢀh,whereas100%ofmiceinthisgroupdiedwithin4ꢀdaysaftertheantibiotictreatmentstopped.ThespleenandliveroftreatmentgroupmiceshowedlowerCFUcounts,ascomparewiththatofinfectedgroup.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•IntJAntimicrobAgents.2018Aug;52(2):269-271.•BiosensBioelectron.2021Jul21;193:113526.•MicrobiolSpectr.2022Aug16;e0139022.•MicrobiolSpectr.2022Aug24;e0203522.•JInfectDis.2019Jul2;220(3):484-493.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].ZhangW,etal.Invitroandinvivobactericidalactivityofceftazidime-avibactamagainstCarbapenemase-producingKlebsiellapneumoniae.AntimicrobResistInfectControl.2018Nov21;7:142.[2].EhmannDE,etal.Avibactamisacovalent,reversible,non-β-lactamβ-lactamaseinhibitor.ProcNatlAcadSciUSA.2012Jul17;109(29):11663-8.[3].LivermoreDM,etal.Characterizationofβ-lactamaseandporinmutantsofEnterobacteriaceaeselectedwithceftaroline+avibactam(NXL104).JAntimicrobChemother.2012Jun;67(6):1354-8.[4].BerkhoutJ,etal.PharmacokineticsandpenetrationofGR20263andavibactamintoepithelialliningfluidinthigh-andlung-infectedmice.AntimicrobAgentsChemother.2015Apr;59(4):2299