Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemENHC-triphosphatetetraammoniumCat.No.:HY-135867E分?式:C?H??N?O??P?分?量:567.28作?靶點(diǎn):EndogenousMetabolite;Enterovirus;HCV;Topoisomerase;SARS-CoV作?通路:MetabolicEnzyme/Protease;Anti-infection;CellCycle/DNADamage儲(chǔ)存?式:-80°C,protectfromlight,storedundernitrogen溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:200mg/mL(352.56mM;Needultrasonicandwarming)DMSO:170mg/mL(299.68mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.7628mL8.8140mL17.6280mL5mM0.3526mL1.7628mL3.5256mL10mM0.1763mL0.8814mL1.7628mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months(protectfromlight,storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)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(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥4.25mg/mL(7.49mM);Clearsolution2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥4.25mg/mL(7.49mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEBIOLOGICALACTIVITY?物活性NHC-triphosphatetetraammoniumNHC(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-triphosphatetetraammonium病毒聚合酶(viralpolymerase)的弱底物替代物，會(huì)被并?HCV復(fù)制?RNA中。體外研究Inanintracellularmetabolismassay,HCVrepliconcellsaretreatedwith10μM3H-labeledNHC,andintracellularnucleotidelevelsaredeterminedafter1,2and8hoursincubations.NHCisrapidlyconveredintothemono-,di-,andtriphosphateforms,andNHC-TPreachesupto71.12pMafter8hours[1].NHC-triphosphatetetraammonium(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-triphosphatetetraammonium(HY-135867)remainsthemostabundantmetabolite[2].NHC-triphosphatetetraammonium(NHC-TP)metabolitemaydirectlytargettheviralpolymeraseandbehaveasanonobligatechainterminator.Itplaysaprominentroleininhibitingearlynegative-strandRNAsynthesis,eitherthroughchainterminationormutagenesis,whichmayinturninterferewithcorrectreplicasecomplexformation.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?NucleicAcidsRes.2021Jan8;49(D1):D1113-D1121.?JBiolChem.2021May11;100770.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].StuyverLJ,etal.RibonucleosideanaloguethatblocksreplicationofbovineviraldiarrheaandhepatitisCvirusesinculture.AntimicrobAgentsChemother.2003Jan;47(1):244-54.[2].MaryamEhteshami,etal.Characterizationofβ-d-N4-HydroxycytidineasaNovelInhibitorofChikungunyaVirus.McePdfHeightCaution:Producthasnotbeenfully