|1-((2R,3R,4S,5R)-3,4-二羟基-5-(羟甲基)四氢呋喃-2-基)-4-(肟基)-3,4-二氢嘧啶-2(1H)-酮|CsnPharm

CAS No.: 3258-02-4

1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-4-(hydroxyimino)-3,4-dihydropyrimidin-2(1H)-one Catalog No. CSN25552

Synonyms: β-D-N4-hydroxycytidine;NHC

EIDD-1931 has a broad-spectrum antiviral activity against multiple coronaviruses, including SARS-CoV2, MERS-CoV, SARS-CoV. and related zoonotic group 2b or 2c Bat-CoVs, as well as increased potency against a coronavirus bearing resistance mutations to another nucleoside analog inhibitor.

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生物活性

描述Venezuelan equine encephalitis virus (VEEV) can cause widespread epidemics among humans and domestic animals. VEEV infections result in severe meningoencephalitis and long-term sequilae. EIDD-1931 is a very potent antiviral agent which effectively inhibits the replication activity of VEEV, Chikungunya virus (CHIKV) and hepatitis C virus (HCV). EIDD-1931 inhibited VEEV with EC₅₀, EC₉₀, and EC₉₉ of 0.426, 1.036, and 2.5 μM, respectively. EIDD-1931 demonstrated a strong negative effect on replication of VEEV TC-83 in Vero cells. EIDD-1931 at 1 μM and 2.5 μM concentrations reduced titers of released virus progeny by 2 and 4 orders of magnitude, respectively. EIDD-1931 treatment at 2 μM concentration led to at least a 10-fold increase in accumulation of mutations. Notably, VEEV resistance to EIDD-1931 developed very inefficiently^[1]. EIDD-1931 inhibited CHIKV replicon activity with an EC₅₀ of 0.8 μM in the Huh-7-CHIKV replicon cell line. CC₅₀ values for NHC were determined to be 30.6, 7.7 and 2.5 μM in PBM, Vero, and CEM cells, respectively^[2].
参考文献

[1] Urakova N, et al. β-d-N⁴-Hydroxycytidine Is a Potent Anti-alphavirus Compound That Induces a High Level of Mutations in the Viral Genome. J Virol. 2018 Jan 17;92(3):e01965-17
[2] Ehteshami M, et al. Characterization of β-d-N4-Hydroxycytidine as a Novel Inhibitor of Chikungunya Virus. Antimicrob Agents Chemother. 2017 Mar 24;61(4):e02395-16

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.8578 mL
- 19.2889 mL
- 38.5779 mL
- 5 mM
- 0.7716 mL
- 3.8578 mL
- 7.7156 mL
- 10 mM
- 0.3858 mL
- 1.9289 mL
- 3.8578 mL

技术信息

CAS号	3258-02-4	储存条件	粉末 Inert atmosphere,2-8°C 液体 -20°C:3-6 月 -80°C:12月
分子式	C9H13N3O6	运输	蓝冰
分子量	259.22	别名	β-D-N4-hydroxycytidine;NHC

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1-((2R,3R,4S,5R)-3,4-Dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-4-(hydroxyimino)-3,4-dihydropyrimidin-2(1H)-one Catalog No. CSN25552

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