Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEEnmetazobactamCat.No.:HY-103095CASNo.:1001404-83-6Synonyms:AAI101分?式:C??H??N?O?S分?量:314.32作?靶點:Bacterial作?通路:Anti-infection儲存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實驗DMSO:≥113.3mg/mL(360.46mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.1815mL15.9074mL31.8147mL5mM0.6363mL3.1815mL6.3629mL10mM0.3181mL1.5907mL3.1815mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的?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.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.08mg/mL(6.62mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.08mg/mL(6.62mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.08mg/mL(6.62mM);ClearsolutionBIOLOGICALACTIVITY?物活性Enmetazobactam(AAI101)?種?譜的β-lactamase抑制劑，能夠抵抗很多耐藥?蘭?性細(xì)。體外研究EnmetazobactamshowspotentactivityagainstspecificresistancephenotypeswithMIC50andMIC90of0.125mg/Land64mg/L[1].Cefepime-EnmetazobactamMICsdecreaseswithincreasingconcentrationsofEnmetazobactam(overtherangefrom1to16mg/L)formoststrains,demonstratingaconcentrationdependenceofEnmetazobactamonrestorationoftheantibacterialactivityofthecephalosporin[1].體內(nèi)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.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?AntimicrobAgentsChemother.2021Nov22;AAC0167621.?ACSInfectDis.2021Mar16.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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