Pretomanid-PA-824-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPretomanidCat.No.:HY-10844CASNo.:187235-37-6Synonyms:PA-824;(S)-PA824分?式:C??H??F?N?O?分?量:359.26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:125mg/mL(347.94mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.7835mL13.9175mL27.8350mL5mM0.5567mL2.7835mL5.5670mL10mM0.2783mL1.3917mL2.7835mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(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(5.79mM);Clearsolution;Needultrasonic2.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:2.08mg/mL(5.79mM);Suspendedsolution;Needultrasonic3.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:2.08mg/mL(5.79mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Pretomanid(PA-824)?種抗?素，可?于肺部多重耐藥性結(jié)核病的研究。Pretomanid對結(jié)核病(MTB)具有亞微爾作?活性。Pretomanid對MTB泛敏感和抗Rifampin的臨床分離株的MIC值為0.015?0.25μg/mL[1]。IC50&TargetTuberculosis.體外研究Pretomanid(PA-824)exhibitedasub-micromolarminimalinhibitoryconcentration(MIC)againstMTB,AlthoughPretomanid(PA-824)wasnotthemostpotentNAPagainstculturedMTBclinicalisolates,itwasthemostactiveininfectedmicewhenorallyadministeredat25mg/kg.ThisindicatedthatPretomanid(PA-824)mightpossessmoredesirablepharmacokineticpropertiesthantheothermorepotentNAPcompoundsthatwetested.Furtherstudiesinmiceat25,50and100mgkg-1Pretomanid(PA-824)dailyfor10daysresultedinreductionsofmycobacterialburdeninbothspleenandlungtissuesthatwerecomparabletothatofINHat25mgkg-1[1].Pretomanid(PA-824)showedsignificantactivityat2,10,and50microg/ml,similartothatofmetronidazole,inadose-dependentmanner.Pretomanid(PA-824)at100mg/kgincyclodextrin/lecithinwasasactiveasmoxifloxacinat100mg/kgandisoniazidat25mg/kgandwasslightlymoreactivethanrifampinat20mg/kg.Long-termtreatmentwithPretomanid(PA-824)at100mg/kgincyclodextrin/lecithinreducedthebacterialloadbelow500CFUinthelungsandspleen[2].Pretomanid(PA-824)hasnoeffectontheviabilityofM.lepraeinallthreemodels,consistentwiththelackofthenitroimidazo-oxazine-specificnitroreductase,encodedbyRv3547intheM.lepraegenome,whichisessentialforactivationofthismolecule[3].戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?DisModelMech.2021Oct13;dmm.049145.?ACSInfectDis.2020Dec15.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].StoverCK,etal.Asmall-moleculenitroimidazopyrandrugcandidateforthetreatmentoftuberculosis.Nature.2000Jun22;405(6789):962-6.[2].LenaertsAJ,etal.PreclinicaltestingofthenitroimidazopyranPA-824foractivityagainstMycobacteriumtuberculosisinaseriesofinvitroandinvivomodels.AntimicrobAgentsChemother.2005Jun;49(6):2294-301.[3].ManjunathaUH,etal.MycobacteriumlepraeisnaturallyresistanttoPA-824.AntimicrobAgentsChemother.2006Oct;50(10):3350-4.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEMcePdfHeightCaution:Producthasn