Enmetazobactam-AAI101-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEnmetazobactamCat.No.:HY-103095CASNo.:1001404-83-6Synonyms:AAI101分⼦式:C₁₁H₁₄N₄O₅S分⼦量:314.32作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:≥113.3mg/mL(360.46mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM3.1815mL15.9074mL31.8147mL5mM0.6363mL3.1815mL6.3629mL10mM0.3181mL1.5907mL3.1815mL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(protectfromlight,storedundernitrogen)。-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：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥2.08mg/mL(6.62mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.62mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.62mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Enmetazobactam(AAI101)⼀种⼴谱的β-lactamase抑制剂，能够抵抗很多耐药⾰兰⽒性细。体外研究EnmetazobactamshowspotentactivityagainstspecificresistancephenotypeswithMIC50andMIC90of0.125mg/Land64mg/L[1].Cefepime-EnmetazobactamMICsdecreaseswithincreasingconcentrationsofEnmetazobactam(overtherangefrom1to16mg/L)formoststrains,demonstratingaconcentrationdependenceofEnmetazobactamonrestorationoftheantibacterialactivityofthecephalosporin[1].体内研究Inneutropenicanimals,cefepime-Enmetazobactamtreatmentresultsinreductionsinbacterialdensityof≥0.5log10CFUfor12ofthe20strainstestedandreductionsof≥1log10CFUfor6ofthese.Increasesinbacterialdensityareforonlyfourstrains,threeofwhichhavecefepime-EnmetazobactamMICsof≥64mg/L,irrespectiveoftheEnmetazobactamconcentration[2].PROTOCOLAnimalThe20Enterobacteriaceaestrainsareusedtoinfectgroupsofthreemiceeach.At2hafterinoculation,miceAdministration[2]aretreatedwithhumanizedregimensofcefepimeorcefepime-AAI101.Alldosesareadministeredas0.2-mLsubcutaneousinjections.Toserveascontrolanimals,anadditionalgroupofmiceisadministerednormalsalineatthesamevolumeandfrequencyandbythesameroute.Thighsfromallanimalsareharvestedat24hafterinitiationoftherapy.TheharvestingprocedureforallstudymicebeganwitheuthanasiabyCO2exposure,followedbycervicaldislocation.Aftersacrifice,thighsareremovedandhomogenizedindividuallyinnormalsaline.FordeterminationsofthenumbersofCFU,serialdilutionsofthighhomogenatesarespreadontoTrypticasesoyagarwith5%sheepbloodusingaspiralplater.Inadditiontotheaforementionedtreatmentandcontrolgroups,anothergroupofthreeinfectedbutuntreatedmiceisharvestedattheinitiationofdosingandservedasa0-hcontrol.Efficacy,expressedasthechangeinbacterialdensity,isdeterminedbycalculationofthechangeinthelog10numberofCFUobtainedinmiceafter24hoftreatmentfromthedensitiesobservedinthe0-hcontrolanimals.MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•AntimicrobAgentsChemother.2021Nov22;AAC0167621.•ACSInfectDis.2021Mar16.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].CrandonJL,etal.InVitroActivityofCefepime/AAI101andComparatorsagainstCefepimeNon-susceptibleEnterobacteriaceae.Pathogens.2015Aug18;4(3):620-5.[2].CrandonJL,etal.Invivoactivitiesofsimulatedhumandosesofcefepimeandcefepime-AAI101againstmultidrug-resistantGram-negativeEnterobacteriaceae.AntimicrobAgentsChemother.2015May;59(5):2688-94.MceP