Delpazolid-LCB01-0371-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEDelpazolidCat.No.:HY-100180CASNo.:1219707-39-7Synonyms:LCB01-0371分⼦式:C₁₄H₁₇FN₄O₃分⼦量:308.31作⽤靶点:Bacterial;Antibiotic作⽤通路:Anti-infection储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验DMSO:30mg/mL(97.30mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM3.2435mL16.2174mL32.4349mL5mM0.6487mL3.2435mL6.4870mL10mM0.3243mL1.6217mL3.2435mL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。-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:≥2.5mg/mL(8.11mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.11mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(8.11mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Delpazolid⼀种新型的恶唑烷酮类抗⽣素，能抑制MSSA和MRSA的⽣长，对它们的MIC90值都为2μg/mL。IC50&TargetOxazolidinone体外研究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].体内研究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—您⾝边的抑制剂⼤师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