Taniborbactam-hydrochloride-VNRX-5133-hydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETaniborbactamhydrochlorideCat.No.:HY-109124ACASNo.:2244235-49-0Synonyms:VNRX-5133hydrochloride分⼦式:C₁₉H₃₀BCl₂N₃O₅分⼦量:462.18作⽤靶点:Bacterial作⽤通路:Anti-infection储存⽅式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性数据体外实验DMSO:200mg/mL(432.73mM;Needultrasonic)H2O:33.33mg/mL(72.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1637mL10.8183mL21.6366mL5mM0.4327mL2.1637mL4.3273mL10mM0.2164mL1.0818mL2.1637mL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(protectfromlight,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。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：1%DMSO>>99%saline1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:≥0.5mg/mL(1.08mM);Clearsolution2.请依序添加每种溶剂：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(10.82mM);Clearsolution3.请依序添加每种溶剂：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(10.82mM);Clearsolution4.请依序添加每种溶剂：10%DMSO>>90%cornoilSolubility:≥5mg/mL(10.82mM);Clearsolution5.请依序添加每种溶剂：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(5.41mM);Clearsolution6.请依序添加每种溶剂：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.41mM);Clearsolution7.请依序添加每种溶剂：PBSSolubility:50mg/mL(108.18mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性Taniborbactamhydrochloride(VNRX-5133hydrochloride)⼀种可逆的，选择性的含硼酸全光谱β-内酰胺酶(β-lactamase)抑制剂，IC50为8-530nM。Taniborbactamhydrochloride对KPC-2，AmpC，OXA-48和VIM-2的IC50分别为30nM，32nM，42nM，20nM。Taniborbactamhydrochloride具有抗⾰兰⽒性(bacteria)活性。IC50&Targetβ-lactamase[1]体外研究Taniborbactamhydrochloride(VNRX-5133hydrochloride)hasIC50sof0.5nM,2nM,0.5nM,0.06nMforKPC-2,OXA-48,VIM-4ofK.pneumoniaestrainandVIM-2ofP.aeruginosastrain[2].Bothcefepime/Taniborbactamhydrochloride(10μg/mL)andmeropenem/TaniborbactamhydrochloridecombinationsarehighlyactiveagainstallsixoftheNDM-1-producingclinicalisolatesfromK.pneumoniaeandE.coli,withMICrangesof16-0.25and1-0.125μg/mL,respectively[1].体内研究Asingledoseofcefepime(32mg/kg)/Taniborbactamhydrochloride(VNRX-5133hydrochloride;16mg/kg;s.c.)achieves>4log10reductioninviablebacterialcountsintheneutropenicmouselunginfectionmodelagainstaCTX-M-14-producingstrainofK.pneumoniae[2].CombinationofCefepime(16mg/kg)andTaniborbactamhydrochloride(16mg/kg;s.c.;twice-a-dayfor7days)demonstrates>2log10reductionsinviablebacterialcountsinthekidneyoftheascendingurinarytractinfectionmodelagainstaCTX-M-15-producingstrainofE.coli[2].TaniborbactamhydrochloridehasaT1/2of0.16hours,aCLof618mL/h/kg,andaVssof143mL/kgformice[2].户使⽤本产品发表的科研⽂献•AntimicrobAgentsChemother.2021Nov22;AAC0167621.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEREFERENCES[1].LiuB,etal.DiscoveryofTaniborbactam(VNRX-5133):ABroad-SpectrumSerine-andMetallo-β-lactamaseInhibitorforCarbapenem-ResistantBacterialInfections.JMedChem.2019Dec16.[2].KrajncA,etal.BicyclicBoronateVNRX-5133InhibitsMetallo-andSerine-β-Lactamases.JMedChem.2019Sep26;62(18):8544-8556.McePdfHeightCaution:Produ