Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDelpazolidCat.No.:HY-100180CASNo.:1219707-39-7Synonyms:LCB01-0371分?式:C??H??FN?O?分?量:308.31作?靶點:Bacterial;Antibiotic作?通路:Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數據體外實驗DMSO:30mg/mL(97.30mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.2435mL16.2174mL32.4349mL5mM0.6487mL3.2435mL6.4870mL10mM0.3243mL1.6217mL3.2435mL請根據產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，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?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：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；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沉淀、析出現象，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:≥2.5mg/mL(8.11mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.11mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.11mM);ClearsolutionBIOLOGICALACTIVITY?物活性Delpazolid?種新型的惡唑烷酮類抗?素，能抑制MSSA和MRSA的?長，對它們的MIC90值都為2μg/mL。IC50&TargetOxazolidinone體外研究Delpazolid(LCB01-0371),atconcentrationsof1×MICand2×MIC,hasbacteriostaticactivityagainstMSSAandMRSAafter24h.Atconcentrationsof4×MICand8×MIC,Delpazolidshowsbacteriostaticactivity,butthereisnoregrowthatconcentrationsof4×MICand8×MICafter24hofincubation[1].ThesurvivalofM.abscessusisgreatlydecreasedinthepresenceofDelpazolid(LCB-0371)(MIC50=1.2μg/mL).Delpazoliddramaticallydecreasesthenumberofintracellularmycobacteriapresentat2daysafterinfectionatconcentrationsof0.1,1,and10μg/mL[2].體內研究Whenadministeredorally,Delpazolid(LCB01-0371)showspotentprotectiveeffectsagainstsystemicinfectionscausedbyGram-positiveandGram-negativebacteria.AgainstinfectioncausedbyS.aureusGiorgio(MSSA),theED50ofDelpazolidis4.53mg/kgofbodyweight.AgainstS.aureusp125(MRSA),theED50ofDelpazolidis2.96mg/kg[1].WhenDelpazolid(LCB-0371)isadministeredat100mg/kgdaily(bygavage),thecolony-formingunit(CFU)countstendtobedecreasedinthelungsofmiceat7daysafterinfection[2].PROTOCOLCellAssay[2]Fortheinvitroinfectionprocedure,bonemarrow-derivedmacrophages(BMDMs)areplatedataconcentrationof2×105cells/wellandinfectedfor4hwithM.abscessus.ThecellsarewashedwithPBStoremoveextracellularbacteriaandtreatedwithDelpazolid(LCB-0371)inmediumfor2days.Thereafter,theintracellularbacteriaareharvestedandthelysatesarediluted10foldinPBS.Eachsampleisplatedon7H10agarplatesandincubatedat37°Cina0.5%CO2incubatorfor7days[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalWTmiceareintranasallyorintravenouslyinjectedwithM.Abscessus(1×107CFU/mouse).After2days,theAdministration[2]miceareorallyadministeredDelpazolid(LCB-0371)for4days,consecutively.At7daysafterM.Abscessusinfection,themicearekilled,andtheirspleens,livers,andlungsarehomogenizedinPBS.Serialdilutionsofthehomogenatesareplatedon7H10mediumsupplementedwith10%OADC(oleicacid,albumin,dextrose,andcatalase)[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].JeongJW,etal.InvitroandinvivoactivitiesofLCB01-0371,anewoxazolidinone.AntimicrobAgentsChemother.2010Dec;54(12):5359-62.[2].KimTS,etal.ActivityofLCB01-0371,aNovelOxazolidinone,againstMycobacteriumabscessus.AntimicrobAgentsChemother.2017Aug24;61(9).McePdfHeightCa