中文名称:

N-羟基胞苷

中文同义词:

N-羟基胞苷;N-羟基胞苷(NHC(EIDD-1931))

英文名称:

N(4)-hydroxycytidine

英文同义词:

N(4)-hydroxycytidine;1-[(2R)-3α,4α-Dihydroxy-5β-(hydroxymethyl)oxolane-2β-yl]-4-(hydroxyamino)pyrimidine-2(1H)-one;3,4-Dihydro-1-β-D-ribofuranosyl-4-(hydroxyimino)pyrimidin-2(1H)-one;N-Hydroxycytidine;β-D-N4-Hydroxycytidine;Beta-d-N4-hydroxycytidine;EIDD-1931;Beta-d-N4-hydroxycytidine (NHC)

CAS号:

3258-02-4

分子式:

C9H13N3O6

分子量:

259.22

EINECS号:

相关类别:

芳香族;抑制剂;医药原料;化合物产品

Mol文件:

3258-02-4.mol

熔点 

169-172 °C(Solv: methanol (67-56-1))

密度 

1.93±0.1 g/cm3(Predicted)

储存条件 

Inert atmosphere,Store in freezer, under -20°C

酸度系数(pKa)

8.19±0.20(Predicted)

生物活性

EIDD-1931 (Beta-d-N4-hydroxycytidine, β-d-N4-hydroxycytidine, NHC)是EIDD-2801的活性代谢产物，它是一种很有前途的 COVID-19 抑制剂。 EIDD-1931（NHC）对 SARS-CoV-2、MERS-CoV、SARS-CoV 和 related zoonotic group 2b或2c Bat-CoVs，对应的平均IC50值为0.15 μM，并且对带有对核苷类似物抑制剂remdesivir耐药性突变的冠状病毒的效力增强。

体外研究

Beta-d-N4-hydroxycytidine is an anti-VEEV (venezuelan equine encephalitis virus) agent with EC 50 , EC 90 , and EC 99 are 0.426, 1.036, and 2.5 μM, respectively.Beta-d-N4-hydroxycytidine inhibits CHIKV replicon activity and the 50% effective concentration (EC 50 ) s 0.8 μM in the Huh-7–CHIKV replicon cell line. Similar results is presented with the replicon in BHK-21 cells (EC 50 =1.8 μM). NHC has no cytotoxicity for NHC in the Huh-7 cell culture system until up to 100 μM using MTT assays. The 50% cytotoxic concentration (CCsub>50) values for NHC are determined to be 30.6 μM, 7.7 μM, and 2.5 μM in peripheral blood mononuclear (PBM), Vero, and CEM cells, respectively.NHC behaves as a pyrimidine analog, NHC-mediated inhibition of the CHIKV replicon can be abrogated by the addition of exogenous nucleosides, such as pyrimidines C and U, but dA, dC, dG, dU, or T has no impact on the replicon. Pyrimidines A and G contributes to replicon inhibition both in the presence and in the absence of NHC.