Temafloxacin-hydrochloride-TMFX-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETemafloxacinhydrochlorideCat.No.:HY-113595CASNo.:105784-61-0Synonyms:TMFXhydrochloride;TA-167;A-62254分⼦式:C₂₁H₁₉ClF₃N₃O₃分⼦量:453.84作⽤靶点:Antibiotic;Bacterial作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Temafloxacin(TMFX)hydrochloride⼀种⼝服有效的喹诺酮类⼴谱抗剂。Temafloxacinhydrochloride对下呼吸道和泌尿⽣殖道感染具有较好的耐受性。体外研究Temafloxacinhydrochloride(0-64µg/mL;18-24h)showsgoodantibacterialactivityforgram-positive/negativebacteria,withMICrangesofE.coli,P.aeruginosa,andS.aureus,respectively[1].CellViabilityAssay[1]CellLine:E.coli(16strains),P.aeruginosa(13strains),andS.aureus(17strains)Concentration:0-64µg/mLIncubationTime:18-24hResult:InhibitedE.coli(16strains),P.aeruginosa,andS.aureuswithMICrangesof<0.004-0.5(MIC90%=0.06,=0.06),0.5-2(MIC90%=1,MIC50%=1)and0.06-0.25µg/mL(MIC90%=0.125,MIC50%=0.125).MIC90%and50%meansMICfor90%and50%oftheisolates(unit:µg/mL).体内研究Temafloxacinhydrochloride(6.25,25,100mg/kg;p.o.;single)showsgoodinhibitoryactivitytomurinepyelonephritis[1].Temafloxacinhydrochloride(100mg/kg;p.o.ors.c.;single)showsrapidgastrointestinalabsorption,andhasexcellenttissueandbodyfluidpenetrationandconcentration(exceptforcentralnervoussystem(CNS))[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAnimalModel:FemaleCF-1mice(20-25g)(murinepyelonephritismodel)[1].Dosage:6.25,25,100mg/kgAdministration:Orally;single.Result:Reducedthenumberofviablebacteriainthekidneysofmice.AnimalModel:FemaleCF-1mice(20-25g)[1].Dosage:100mg/kgAdministration:Subcutaneouslyororally;single.Result:1.19PharmacokineticParametersofTemafloxacinhydrochlorideinFemaleCF-1mice[1].Cmax(µg/mL)AUC(µg/mL•h)T1/2(h)%UrinaryrecoverySC(100mg/kg)25.286.63.425.3PO(100mg/kg)13.5REFERENCES[1].HardyDJ,etal.Comparativeantibacterialactivitiesoftemafloxacinhydrochloride(A-62254)andtworeferencefluoroquinolones.AntimicrobAgentsChemother.1987Nov;31(11):1768-74.[2].PankeyGA.Temafloxacin:anoverview.AmJMed.1991Dec30;91(6A):166S-172S.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch