Contezolid-acefosamil-sodium-MRX-4-sodium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEContezolidacefosamilsodiumCat.No.:HY-19915BCASNo.:1807365-35-0Synonyms:MRX-4sodium分⼦式:C₂₀H₁₇F₃N₄NaO₈P分⼦量:552.33作⽤靶点:Bacterial;Antibiotic;MonoamineOxidase作⽤通路:Anti-infection;NeuronalSignaling储存⽅式:-80°C,storedundernitrogen溶解性数据体外实验DMSO:180mg/mL(325.89mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.8105mL9.0526mL18.1051mL5mM0.3621mL1.8105mL3.6210mL10mM0.1811mL0.9053mL1.8105mL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(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4.5mg/mL(8.15mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥4.5mg/mL(8.15mM);Clearsolution1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE3.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥4.5mg/mL(8.15mM);ClearsolutionBIOLOGICALACTIVITY⽣物活性Contezolidacefosamilsodium(MRX-4)⼀种新型的恶唑烷酮，⽤于耐药⾰兰⽒阳性引起的⽪肤组织感染并发症(cSSTI)的抗⽣素。Contezolidacefosamilsodium(MRX-4)可显著降低⾻髓移植和单胺氧化酶抑制。体外研究Contezolid(MRX-I)ishighlypotentagainstallGrampositiveclinicalisolatesofstaphylococci,streptococci,andenterococci,includingMDRorganismssuchasMRSA,methicilline-resistantStreptococcusepidermidis(MRSE),penicillin-resistantStreptococci(PRSP),andVRE[2].体内研究OralabsorptionofContezolid(MRX-I)occurrsrapidlyinmouse,rat,anddog,withpeakplasmaconcentrationsobservedat0.5−2.6hpostdose.Inmouse,rat,anddog,respectively,PKparametersaredeterminedasfollows:dose-normalizedCmax/dosewas524,1065,and259ng/mL/(mg/kg);dose-normalizedAUC0−t/dosewas1654,3703,and1664ng•h/mL/(mg/kg);T1/2is1,1.5,and3h;andtheoralbioavailabilityis69%,109%,and37%[2].Contezolid(MRX-I)exhibitsnoobvioustoxicity[2].Contezolid(MRX-I,100mg/kg,oncedaily)significantlyreducedthebacterialloadinlungscomparedtotheuntreatedearlyandlatecontrols[3].AnimalModel:BALB/cmiceinfectedintranasallywithM.tuberculosisErdman[3].Dosage:100,50(twice),25(twice)mg/kg.Administration:Gavage,onceortwicedaily,fivedaysperweekforfourweeks.Result:SignificantlyreducedtheCFUrecoveredfromthelungscomparedtotheearlyandlatecontrolmice(P<0.05).TwicedailyMRX-Iat50mg/kgand25mg/kgweresignificantlybetterthanthelatecontrolmice(P<0.05).OncedailyMRX-Iat100mg/kgwassignificantlybetterthantwicedaily50mg/kgand25mg/kg(P<0.05).Therewasnostatisticaldifferencebetweentwicedaily50mg/kgofMRX-Iand25mg/kg(P>0.05).AnimalModel:Rats[2].Dosage:20,100,and200/300mg/kg/day.Administration:Orallytwicedaily.Result:Nomortalitywasobserved.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].JunzhenWu,etal.EvaluationoftheEffectofContezolid(MRX-I)ontheCorrectedQTIntervalinaRandomized,Double-Blind,Placebo-andPositive-ControlledCrossoverStudyinHealthyChineseVolunteers.AntimicrobAgentsChemother.2020May21;64(6):e02158-19.[2].MikhailFGordeev,etal.Newpotentantibacterialoxazolidinone(MRX-I)withanimprovedclasssafetyprofile.JMedChem.2014Jun12;57(11):4487-97.[3].CarolynShoen,etal.InVitroandInVivoActivitiesofContezolid(MRX-I)againstMycobacteriumtuberculosis.AntimicrobAgentsChemother.2018Jul27;62(8):e00493-18.McePdfHeightCaution:Produ