Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemERanbezolidCat.No.:HY-19428CASNo.:392659-38-0Synonyms:RBx7644freebase分子式:C??H??FN?O?分子量:461.44作用靶點:Antibiotic;Bacterial作用通路:Anti-infection儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Ranbezolid(RBx7644freebase)是一種口服有效的，針對革蘭式陽性和革蘭式陰性厭氧菌(如金黃色葡萄球菌、表皮葡萄球菌、脆弱擬桿菌)的惡唑烷酮類抗生素(antibiotic)。Ranbezolid可抑制50s核糖體亞基，其對于細(xì)菌核糖體的IC50值為17μM。Ranbezolid還可干擾其細(xì)胞壁和脂質(zhì)合成。Ranbezolid可快速殺菌，顯著降低細(xì)菌負(fù)荷，且具備更好的心血管安全性。Ranbezolid可用于厭氧菌抗生素的研究[1][2][3]。體外研究Ranbezolid(1μg/mL)caneffectivelyinhibitproteinsynthesisinS.aureusaswellasinS.epidermidis,andadditionallysuppressthecellwallandlipidsynthesisofStaphylococcusepidermidis[1].Ranbezoild(1-8μg/mL)cancauseconcentration-dependentdamagetothecellmembraneofS.epidermidis[1].RanbezoildexhibitsaIC50valueof17μMforbacterialribosomesandsafetyindexof865[1].RanbezolidexhibitstheMICsagainsttheanaerobicstrainsofB.fragilis,B.vulgatus,B.thetaiotaomicron,C.perfringens,C.difficileandP.magnuswere0.06,0.015,0.06,0.06,0.03and0.015μg/mL,respectively[2].體內(nèi)研究Ranbezoild(100mg/kg,p.o.,twicedailyfor5days)showsexcellentantibacterialactivityagainstB.fragilisinmurineforeign-bodyinfectionmodel[2].Ranbezoild(≤50mg/kg,p.o.,singledose)doesnotsignificantlyenhancethebloodpressure-raisingeffectofTyramine(HY-W007606)withinthetherapeuticdoserangeinthespontaneoushypertensionmodelofrats[3].AnimalModel:Murineforeign-bodyinfectionwithBacteroidesfragilisestablishedinswissalbinomiceofeithersexweighing20±2g[2]1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEDosage:100mg/kgAdministration:Oraladministration(p.o.),twicedaily,for5daysResult:Displayed5.39log10reductions.AnimalModel:PressorresponsemodelestablishedinmaleWistarrats(250-350g)[3]Dosage:15,50and100mg/kgAdministration:Oraladministration(p.o.),singledoseResult:Increasedmeanarterialpressureby10,11,14mmHg(15,50and100mg/kg)with5mg/kgtyramine.REFERENCESKaliaV,etal.ModeofactionofRanbezolidagainststaphylococciandstructuralmodelingstudiesofitsinteractionwithribosomes.AntimicrobAgentsChemother.2009Apr;53(4):1427-33.MathurT,etal.Anti-anaerobicpotentialofranbezolid:insightintoitsmechanismofactionagainstBacteroidesfragilis.IntJAntimicrobAgents.2013Jan;41(1):36-40.NaruganahalliKS,etal.Ranbezolid,anoveloxazolidinoneantibacterial:invivocharacterisationofmonoamineoxidaseinhibitorypotentialinconsciousrats.EurJPharmacol.2006Sep18;545(2-3):167-72.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappl