Taniborbactam-hydrochloride-VNRX-5133-hydrochloride-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETaniborbactamhydrochlorideCat.No.:HY-109124ACASNo.:2244235-49-0Synonyms:VNRX-5133hydrochloride分?式:C??H??BCl?N?O?分?量:462.18作?靶點:Bacterial作?通路:Anti-infection儲存?式:-20°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數據體外實驗DMSO:200mg/mL(432.73mM;Needultrasonic)H2O:33.33mg/mL(72.11mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1637mL10.8183mL21.6366mL5mM0.4327mL2.1637mL4.3273mL10mM0.2164mL1.0818mL2.1637mL請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month(protectfromlight,storedundernitrogen)。-80°C儲存時，請在6個?內使?，-20°C儲存時，請在1個?內使?。體內實驗請根據您的實驗動物和給藥?式選擇適當的溶解?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結果的可靠性，澄的儲備液可以根據儲存條件，適當保存；體內實驗的?作液，建議您現?現配，當天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：1%DMSO>>99%saline1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥0.5mg/mL(1.08mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥5mg/mL(10.82mM);Clearsolution3.請依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥5mg/mL(10.82mM);Clearsolution4.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥5mg/mL(10.82mM);Clearsolution5.請依序添加每種溶劑：5%DMSO>>40%PEG300>>5%Tween-80>>50%salineSolubility:≥2.5mg/mL(5.41mM);Clearsolution6.請依序添加每種溶劑：5%DMSO>>95%(20%SBE-β-CDinsaline)Solubility:≥2.5mg/mL(5.41mM);Clearsolution7.請依序添加每種溶劑：PBSSolubility:50mg/mL(108.18mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性Taniborbactamhydrochloride(VNRX-5133hydrochloride)?種可逆的，選擇性的含硼酸全光譜β-內酰胺酶(β-lactamase)抑制劑，IC50為8-530nM。Taniborbactamhydrochloride對KPC-2，AmpC，OXA-48和VIM-2的IC50分別為30nM，32nM，42nM，20nM。Taniborbactamhydrochloride具有抗?蘭?性(bacteria)活性。IC50&Targetβ-lactamase[1]體外研究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].體內研究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].戶使?本產品發(fā)表的科研?獻?AntimicrobAgentsChemother.2021Nov22;AAC0167621.Seemorecustomervalidationsonwww.MedChemE2/3MasterofBioactiveMolecules—您?邊的抑制劑?師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