产品说明书

((2R,3S,4R,5R)-3,4-Dihydroxy-5-(4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)methyl isobutyrate

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Chemical Structure| 2635324-86-4 同义名 : -
CAS号 : 2635324-86-4
货号 : A1241514
分子式 : C13H19N3O7
纯度 : 98%
分子量 : 329.306
MDL号 : N/A
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
描述 Coronaviruses (CoVs) traffic frequently between species resulting in novel disease outbreaks, most recently exemplified by the newly emerged SARS-CoV-2, the causative agent of COVID-19. EIDD-2801, an orally bioavailable prodrug of NHC (β-D-N4-hydroxycytidine-5′-isopropyl ester), has broad spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. Beginning on 3 days post-infection (dpi), body weight loss compared to vehicle treatment was significantly diminished (50 mg/kg) or prevented (150, 500 mg/kg) with EIDD-2801 prophylaxis in C57BL/6 mice. Lung hemorrhage was also significantly reduced 5 dpi with 500 mg/kg EIDD-2801 treatment. Interestingly, there was a dose-dependent reduction in SARS-CoV lung titer with significant differences among the vehicle, 150 mg/kg (P = 0.03) and 500 mg/kg (P = 0.006) groups suggesting that prophylactic orally administered EIDD-2801 was robustly antiviral and able to prevent SARS-CoV replication and disease. Similar to SARS-CoV data, all doses of prophylactic EIDD-2801 (50, 150 and 500 mg/kg) protected hDPP4 288/330 mice from significant body weight loss, lung hemorrhage, and virus replication which was undetectable regardless of drug dose following intranasal infection with 5E+04 PFU mouse-adapted MERS-CoV. Interestingly, when viral genomic RNA was quantified in paired samples of lung tissue, EIDD-2801 significantly reduced quantities of viral RNA in an initiation time-dependent manner for all groups except for +48 hours. Collectively, EIDD-2801 robustly reduces MERS-CoV infectious titers, viral RNA, and pathogenesis under both prophylactic and early therapeutic conditions. Lastly, the EIDD-2801 dose-dependent mutagenesis of viral RNA correlated with an increase in codon change frequency, including stop codons, in mice where treatment was initiated 12 hours or before[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.04mL

0.61mL

0.30mL

15.18mL

3.04mL

1.52mL

30.37mL

6.07mL

3.04mL
参考文献

[1]Sheahan TP, Sims AC, Zhou S, et al. An orally bioavailable broad-spectrum antiviral inhibits SARS-CoV-2 in human airway epithelial cell cultures and multiple coronaviruses in mice. Sci Transl Med. 2020;12(541):eabb5883