Antituberculosis-agent-10-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEAntituberculosisagent-10Cat.No.:HY-163486CASNo.:2095636-19-2分⼦式:C₁₇H₁₇FN₂O₄S分⼦量:364.39作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Antituberculosisagent-10(Compound9)具有对Mycobacteriumtuberculosis的抗活性(MIC=0.3μM)。通过靶向细的50S核糖体亚，抑制蛋⽩质合成，从⽽发挥其抗作⽤。Antituberculosisagent-10还具有⼝服活性[1]。体外研究Antituberculosisagent-10(72h)isinactiveininhibitingmitochondrialproteinsynthesis(MPS)inHepG2cells(IC50=150μM),butitsmetabolitesshowsmitochondrialtoxicity[1].体内研究Antituberculosisagent-10((i.g.;5-50mg/kg;onceortwiceaday)exhibitsexcellentpermeabilityandsustainedactivitywithininfectedC3HeB/FeJmice[1].Antituberculosisagent-10((i.g.;4mg/kg;twicedailyforoneweekthenoncedaily)reducesthevolumeoftuberculosisfociinMtb-infectedmarmosetswithpotentantibacterialactivity[1].PharmacokineticAnalysisinAntituberculosisagent-10[1]RouteDose(mpk)Cl/Clu(mL/min/kg)Vd/Vdu(L/kg)MRT/sst1/2(h)F(%)i.v.212/3160.6/160.8/0.6/p.o.10///64AnimalModel:infectedC3HeB/FeJmice[1]Dosage:5,10,15,,50mg/kg,twicedaily;30mg/kg,oncedailyAdministration:i.g.1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEResult:Penetratedeffectivelyintoboththecellularandnecroticcompartmentsofthelesions.MaintainedconcentrationsabovetheMICfortuberculosisbacteriaatvariouslesionsites.AnimalModel:Mtb-infectedmarmosets[1]Dosage:4mg/kg,twicedailyfor1weekthen4mg/kgoncedailyAdministration:i.g.Result:Reducedphysicallesionsizeandbacterialloadwithinthoselesions.Showedsuperiororatleastcomparableresultsinreducinglesionvolumeandbacterialcountthanlinezolid(HY-10394).REFERENCES[1].BoshoffHIM,etal.Mtb-Selective5-AminomethylOxazolidinoneProdrugs:RobustPotencyandPotentialLiabilities.ACSInfectDis.2024Apr6.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel: