Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrariesNHC-triphosphatetetrasodiumCat.No.:HY-135867A分?式:C?H??N?Na?O??P?分?量:587.08作?靶點:EndogenousMetabolite;Enterovirus;HCV;Topoisomerase作?通路:MetabolicEnzyme/Protease;Anti-infection;CellCycle/DNADamage儲存?式:-20°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealedstorage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實驗H2O:100mg/mL(170.33mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.7033mL8.5167mL17.0335mL5mM0.3407mL1.7033mL3.4067mL10mM0.1703mL0.8517mL1.7033mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性NHC-triphosphatetetrasodiumNHC(HY-125033)的活性胞內(nèi)磷酸鹽代謝物(intracellularmetabolite)，以三磷酸鹽的形式存在。NHC-triphosphatetetrasodium病毒聚合酶(viralpolymerase)的弱底物替代物，會被并?HCV復制?RNA中。體外研究Inanintracellularmetabolismassay,HCVrepliconcellsaretreatedwith10μM3H-labeledNHC,andintracellularnucleotidelevelsaredeterminedafter1,2and8hoursincubations.NHCisrapidlyconveredintothemono-,di-,andtriphosphateforms,andNHC-TPreachesupto71.12pMafter8hours[1].NHC-triphosphate(NHC-TP)(5-40μM)absenceleadstofull-lengthpolymerizationproducts,itcanbeaweakalternativesubstrate.Inaddition,incorporationofNHC-TPinsteadofCTPincreasesthemolecularweightofthepolymerizationproductby16(oneextraoxygen)foreacheventandanobviouselectrophoretic1/2shiftisobservedincell-freeHCVNS5Bpolymerizationreactions[1].Huh-7cellsareincubatedwith(10-50μM;4h)NHCoraMcGuiganphosphoramidateprodrugofNHC.IntracellularlevelsoftheparentalcompoundsandphosphorylatedmetabolitesaremeasuredusingLC-MS/MS.SmallamountsofNHC-monophosphate(MP)andNHC-diphosphate(DP)canbeobserved,whileNHC-triphosphate(HY-135867)remainsthemostabundantmetabolite[2].NHC-triphosphate(NHC-TP)metabolitemaydirectlytargettheviralpolymeraseandbehaveasanonobligatechainterminator.Itplaysaprominentroleininhibitingearlynegative-strandRNAsynthesis,eitherthroughchainterminationormutagenesis,whichmayinturninterferewithcorrectreplicasecomplexformation.戶使?本產(chǎn)品發(fā)表的科研?獻?NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.REFERENCES[1].StuyverLJ,etal.RibonucleosideanaloguethatblocksreplicationofbovineviraldiarrheaandhepatitisCvirusesinculture.AntimicrobAgentsChemother.2003Jan;47(1):244-54.[2].MaryamEhteshami,etal.Characterizationofβ-d-N4-HydroxycytidineasaNovelInhibitorofChikungunyaVirus.McePdfHeightMedChemExpress(MC