BTZ043-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBTZ043Cat.No.:HY-13579CASNo.:1161233-85-7分?式:C??H??F?N?O?S分?量:431.39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(shù)據(jù)體外實驗DMSO:13.3mg/mL(30.83mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3181mL11.5904mL23.1809mL5mM0.4636mL2.3181mL4.6362mL10mM0.2318mL1.1590mL2.3181mL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。-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%salineSolubility:2.5mg/mL(5.80mM);Suspendedsolution;Needultrasonic1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.5mg/mL(5.80mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.5mg/mL(5.80mM);ClearsolutionBIOLOGICALACTIVITY?物活性BTZ043DprE1的抑制劑，它對結(jié)核分枝桿H37Rv(M.tuberculosisH37Rv)和恥垢分枝桿(Mycobacteriumsmegmatis)的MIC值分別為2.3nM和9.2nM。IC50&TargetDprE1[1].體外研究TheMICofBTZ043againstM.tuberculosisH37RvandMycobacteriumsmegmatisare1ng/mL(2.3nM)and4ng/mL(9.2nM),respectively[2].TheinvitroactivityofBTZ043against30Nocardiabrasiliensisisolatesisalsotested.TheMIC50andMIC90valuesforBTZ043are0.125and0.25μg/mL.TheMICforN.carneaATCC6847is0.003μg/mL,forN.transvalensisATCC6865is0.003μg/mL,forN.brasiliensisNCTC10300is0.03μg/mL,andforN.brasiliensisHUJEG-1is0.125μg/mL.TheMICvalueforM.tuberculosisH37Rvis0.000976μg/mL.TheMICvalueofBTZ-043is>64μg/mLforEscherichiacoliATCC25922andS.aureusATCC29213[3].體內(nèi)研究FourweeksoftreatmentwithBTZ043reducesthebacterialburdeninthelungsandspleensby1and2logs,respectively,attheconcentrationsused.AdditionalresultssuggestthatBTZ043efficacyistime-ratherthandose-dependent.Acute(5g/kg)andchronic(25and250mg/kg)toxicologystudiesinuninfectedmiceshowthat,evenatthehighestdosetested,therearenoadverseanatomical,behavioral,orphysiologicaleffectsafteronemonth[2].PROTOCOLAnimalMice[2]Administration[2]Animalefficacyisdeterminedinastandardmouseinfectionmodel.BALB/cmiceareinfectedwithalowbacillaryload(~200CFU)ofM.tuberculosisH37Rvviaaerosol.Treatmentstartedfour-weekspostinfection.Micearedosedbygavagewith37.5,or300mgofBTZ043,perkgbodyweight,incarboxymethylcelluloseformulation(0.25%),oncedaily,sixtimes/week,forfourweeks.Controlandtreatedmicearesacrificed,lungsandspleenshomogenizedanddilutionsplatedforenumerationofviablebacilli[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻?JMedChem.2020May28;63(10):5367-5386.?ChemNanoMat.2020Oct28.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].VadimMakarovetal.The8-Pyrrole-BenzothiazinonesAreNoncovalentInhibitorsofDprE1fromMycobacteriumtuberculosis.AntimicrobAgentsChemother,2015Aug,59(8):4446-4452.[2].MakarovV,etal.BenzothiazinoneskillMycobacteriumtuberculosisbyblockingarabinansynthesis.Science.2009May8;324(5928):801-4.[3].NormaAlejandraGonzález-Martínezetal.InVivoActivityoftheBenzothiazinonesPBTZ169andBTZ043againstNocardiabrasiliensis.PLoSNeglTropDis,2015Oct,9(10):e0004022.McePdfHeightCaution