|((2R,3S,4R,5R)-3,4-二羟基-5-(4-(肟基)-2-氧代-3,4-二氢嘧啶-1(2H)-基)四氢呋喃-2-基)甲基异丁酸酯|CsnPharm

CAS No.: 2635324-86-4

((2R,3S,4R,5R)-3,4-Dihydroxy-5-(4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)methyl isobutyrate Catalog No. CSN25551

EIDD-2801 is an orally bioavailable prodrug of EIDD-1931, which has a broad-spectrum antiviral activity against 39 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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技术信息

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].
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

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
- 3.0367 mL
- 15.1835 mL
- 30.3669 mL
- 5 mM
- 0.6073 mL
- 3.0367 mL
- 6.0734 mL
- 10 mM
- 0.3037 mL
- 1.5183 mL
- 3.0367 mL

技术信息

CAS号

2635324-86-4

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

C13H19N3O7

运输

蓝冰

分子量

329.31

别名

溶解度

DMSO	63.0 mg/mL (191.3 mM)
Ethanol	22.0 mg/mL (66.8 mM)

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((2R,3S,4R,5R)-3,4-Dihydroxy-5-(4-(hydroxyimino)-2-oxo-3,4-dihydropyrimidin-1(2H)-yl)tetrahydrofuran-2-yl)methyl isobutyrate Catalog No. CSN25551

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