Delpazolid-LCB01-0371-DataSheet-生命科學(xué)試劑-MedChemExpress

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(diǎn):Bacterial;Antibiotic作?通路:Anti-infection儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:30mg/mL(97.30mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.2435mL16.2174mL32.4349mL5mM0.6487mL3.2435mL6.4870mL10mM0.3243mL1.6217mL3.2435mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)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(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(8.11mM);Clearsolution3.請(qǐng)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(lèi)抗?素，能抑制MSSA和MRSA的?長(zhǎng)，對(duì)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(nèi)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