NHC-diphosphate-triammonium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENHC-diphosphatetriammoniumCat.No.:HY-135867F分⼦式:C₉H₂₄N₆O₁₂P₂分⼦量:470.27作⽤靶点:EndogenousMetabolite;Enterovirus;HCV;Topoisomerase;SARS-CoV作⽤通路:MetabolicEnzyme/Protease;Anti-infection;CellCycle/DNADamage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H2O:160mg/mL(340.23mM;Needultrasonicandwarming)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.1264mL10.6322mL21.2644mL5mM0.4253mL2.1264mL4.2529mL10mM0.2126mL1.0632mL2.1264mL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。BIOLOGICALACTIVITY⽣物活性NHC-triphosphatetriammoniumNHC(HY-125033)的活性胞内磷酸盐代谢物(intracellularmetabolite)，以三磷酸盐的形式存在。NHC-triphosphatetriammonium病毒聚合酶(viralpolymerase)的弱底物替代物，会被并⼊HCV复制⼦RNA中。体外研究Inanintracellularmetabolismassay,HCVrepliconcellsaretreatedwith10μM3H-labeledNHC,andintracellularnucleotidelevelsaredeterminedafter1,2and8hoursincubations.NHCisrapidlyconveredinto1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEthemono-,di-,andtriphosphateforms,andNHC-TPreachesupto71.12pMafter8hours[1].NHC-triphosphatetriammonium(NHC-TP)(5-40μM)absenceleadstofull-lengthpolymerizationproducts,itcanbeaweakalternativesubstrate.Inaddition,incorporationofNHC-TPinsteadofCTPincreasesthemolecularweightofthepolymerizationproductby16(oneextraoxygen)foreacheventandanobviouselectrophoreticshiftisobservedincell-freeHCVNS5Bpolymerizationreactions[1].Huh-7cellsareincubatedwith(10-50μM;4h)NHCoraMcGuiganphosphoramidateprodrugofNHC.IntracellularlevelsoftheparentalcompoundsandphosphorylatedmetabolitesaremeasuredusingLC-MS/MS.SmallamountsofNHC-monophosphate(MP)andNHC-diphosphate(DP)canbeobserved,whileNHC-triphosphatetriammonium(HY-135867)remainsthemostabundantmetabolite[2].NHC-triphosphatetriammonium(NHC-TP)metabolitemaydirectlytargettheviralpolymeraseandbehaveasanonobligatechainterminator.Itplaysaprominentroleininhibitingearlynegative-strandRNAsynthesis,eitherthroughchainterminationormutagenesis,whichmayinturninterferewithcorrectreplicasecomplexformation.REFERENCES[1].StuyverLJ,etal.RibonucleosideanaloguethatblocksreplicationofbovineviraldiarrheaandhepatitisCvirusesinculture.AntimicrobAgentsChemother.2003Jan;47(1):244-54.[2].MaryamEhteshami,etal.Characterizationofβ-d-N4-HydroxycytidineasaNovelInhibitorofChikungunyaVirus.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala