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NHC-triphosphate
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NHC-triphosphate
CAS No. : 34973-27-8
MCE 站:NHC-triphosphate
产品活性:NHC-triphosphate 是 NHC (HY-125033) 的活性胞内磷酸盐代谢物 (intracellular metabolite ),以三磷酸盐的形式存在。NHC-triphosphate 是病毒聚合酶 (viral polymerase) 的弱底物替代物,会被并入 HCV 复制子 RNA 中。
研究领域:Metabolic Enzyme/Protease | Anti-infection | Cell Cycle/DNA Damage
作用靶点:Endogenous Metabolite | Enterovirus | HCV | Topoisomerase | SARS-CoV
In Vitro: In an intracellular metabolism assay, HCV replicon cells are treated with 10 μM?3H-labeled NHC, and intracellular nucleotide levels are determined after 1, 2 and 8 hours incubations. NHC is rapidly convered into the mono-, di-, and triphosphate forms, and NHC-TP reaches up to 71.12 pM after 8 hours.NHC-triphosphate (NHC-TP) (5-40 μM) absence leads to full-length polymerization products, it can be a weak alternative substrate. In addition, incorporation of NHC-TP instead of CTP increases the molecular weight of the polymerization product by 16 (one extra oxygen) for each event and an obvious electrophoretic shift is observed in cell-free HCV NS5B polymerization reactions.Huh-7 cells are incubated with (10-50 μM; 4 h) NHC or a McGuigan phosphoramidate prodrug of NHC. Intracellular levels of the parental compounds and phosphorylated metabolites are measured using LC-MS/MS. Small amounts of NHC-monophosphate (MP) and NHC-diphosphate (DP) can be observed, while NHC-triphosphate (HY-135867) remains the most abundant metabolite.NHC-triphosphate (NHC-TP) metabolite may directly target the viral polymerase and behave as a nonobligate chain terminator.?It plays a prominent role in inhibiting early negative-strand RNA synthesis, either through chain termination or mutagenesis, which may in turn interfere with correct replicase complex formation.
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热门标签:NHC-TP