Trovafloxacin-mesylate-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETrovafloxacinmesylateCat.No.:HY-103399CASNo.:147059-75-4分?式:C??H??F?N?O?S分?量:512.46作?靶點(diǎn):Bacterial;Topoisomerase;Antibiotic作?通路:Anti-infection;CellCycle/DNADamage儲存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實驗DMSO:125mg/mL(243.92mM;ultrasonicandwarmingandheatto60°C)H2O:20mg/mL(39.03mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9514mL9.7569mL19.5137mL5mM0.3903mL1.9514mL3.9027mL10mM0.1951mL0.9757mL1.9514mL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(storedundernitrogen)。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性Trovafloxacinmesylate?種?譜喹諾酮類抗?素，對?蘭?陽性，?蘭?性和厭氧具有有效的活性。Trovafloxacinmesylate可阻斷DNA促旋酶(DNAgyrase)和拓?fù)洚悩?gòu)酶IV(topoisomeraseIV)的活性。Trovafloxacinmesylate也?種有效的，選擇性的，?服活性的Pannexin1通道(PANX1)抑制劑，對PANX1內(nèi)向電流的IC50為4μM。Trovafloxacinmesylate不抑制連接蛋?43間隙連接或PANX2。Trovafloxacinmesylate通過抑制PANX1導(dǎo)致凋亡細(xì)胞碎?失調(diào)。1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIC50&TargetQuinolone體外研究Trovafloxacin(20μM;24hours;HepG2cells)andtumornecrosisfactor(TNF;4ng/mL)incubationinducesapoptosisandincreasesleakageoflactatedehydrogenase(LDH)inHepG2cells[1].Trovafloxacin(20μM;24hours;HepG2cells)andTNF(4ng/mL)incubationincreasesexpressionofearlyNF-κB-relatedfactorsA20andIκBα[1].TrovafloxacinprolongsTNF-inducedactivationofMAPKsandIKKα/βactivationinHepG2[1].TrovafloxacinisapotentinhibitorofTO-PRO-3uptakebyapoptoticcells.TrovafloxacinalsoinhibitsATPreleasefromapoptoticcells.Trovafloxacindoesnotinhibitcaspase3/7activation,orcaspase-mediatedPANX1cleavageduringapoptosis[2].Trovafloxacinisequallyactiveagainstbothpenicillin-susceptibleand-resistantpneumococci,withMICsof0.06-0.25mg/mLreportedformorethan700isolates.TheMICsofTrovafloxacinatwhich90%ofisolatesareinhibitedfor55isolatesofpneumococciis0.125μg/mL[3].ApoptosisAnalysis[1]CellLine:HepG2cellsConcentration:20μMIncubationTime:24hoursResult:ShowedagradualincreaseofAnnexinV-stainingandanincreasedleakageoflactatedehydrogenase(LDH)at24h.RT-PCR[1]CellLine:HepG2cellsConcentration:20μMIncubationTime:24hoursResult:CausedahigherincreaseinthetranscriptionofA20andIκBαinHepG2cells.體內(nèi)研究Trovafloxacin(150mg/kg;oraladministration;maleC57BL/6Jmice)treatmentdisruptsTNF-inducedp65nucleartranslocation.TrovafloxacintreatmentincreasesexpressionofearlyNF-κB-relatedfactorsA20andIκBα[1].Trovafloxacin,whenadministeredincombinationwithlipopolysaccharide(LPS)orTNFtomiceinducesseverelivertoxicityassociatedwithvastapoptoticareasintheliver,increasedserumlevelsofalanineaminotransferases(ALT)andpro-inflammatorycytokines[1].AnimalModel:MaleC57BL/6Jmice(9-11-week-old)injectedwithrecombinantmurineTNFion[1]Dosage:150mg/kgAdministration:Oraladministration;once2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEResult:Showedagreaternumberofcellswithincreasednuclear/cytoplasmicp65ratioinliver.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?BiotechnolBioeng.2021Sep3.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].GiustariniG,etal.ThehepatotoxicfluoroquinolonetrovafloxacindisturbsTNF-andLPS-inducedp65nucleartranslocationinvivoandinvitro.ToxicolApplPharmacol.2020Mar15;391:114915.[2].PoonIK,etal.Unexpectedlinkbetweenanantibiotic,pannexinchannelsandapoptosis.Nature.2014Mar20;507(7492):329-34.[3].GootzTD,etal.Activityofthenewfluoroquinolonetrovafloxacin(CP-99,219)againstDNAgyraseandtopoisomeraseIVmutantsofStreptococcuspneumoniaeselectedinvitro.AntimicrobAgentsChemother.1996Dec;40(12):2691-7.McePdfHeigh