Trovafloxacin-mesylate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETrovafloxacinmesylateCat.No.:HY-103399CASNo.:147059-75-4分⼦式:C₂₁H₁₉F₃N₄O₆S分⼦量:512.46作⽤靶点:Bacterial;Topoisomerase;Antibiotic作⽤通路:Anti-infection;CellCycle/DNADamage储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验DMSO:125mg/mL(243.92mM;ultrasonicandwarmingandheatto60°C)H2O:20mg/mL(39.03mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9514mL9.7569mL19.5137mL5mM0.3903mL1.9514mL3.9027mL10mM0.1951mL0.9757mL1.9514mL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(storedundernitrogen)。-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。BIOLOGICALACTIVITY⽣物活性Trovafloxacinmesylate⼀种⼴谱喹诺酮类抗⽣素，对⾰兰⽒阳性，⾰兰⽒性和厌氧具有有效的活性。Trovafloxacinmesylate可阻断DNA促旋酶(DNAgyrase)和拓扑异构酶IV(topoisomeraseIV)的活性。Trovafloxacinmesylate也⼀种有效的，选择性的，⼝服活性的Pannexin1通道(PANX1)抑制剂，对PANX1内向电流的IC50为4μM。Trovafloxacinmesylate不抑制连接蛋⽩43间隙连接或PANX2。Trovafloxacinmesylate通过抑制PANX1导致凋亡细胞碎⽚失调。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetQuinolone体外研究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.体内研究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—您⾝边的抑制剂⼤师www.MedChemEResult:Showedagreaternumberofcellswithincreasednuclear/cytoplasmicp65ratioinliver.户使⽤本产品发表的科研⽂献•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