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2349386-89-4
  • names:

    EIDD 2801

  • CAS號:

    2349386-89-4

    MDL Number:
  • MF(分子式): C13H19N3O7 MW(分子量): 329.1223
  • EINECS: Reaxys Number:
  • Pubchem ID: Brand:BIOFOUNT
EIDD-2801
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中文別名 EIDD-2801(cas:2349386-89-4),EIDD2801,EIDD 2801
英文別名 2349386-89-4,EIDD 2801,[(2R,3S,4R,5R)-3,4-dihydroxy-5-[(4Z)-4-(hydroxyimino)-2-oxo-1,2,3,4-tetrahydropyrimidin-1-yl]oxolan-2-yl]methyl 2-methylpropanoate
CAS號 2349386-89-4
Inchi InChI=1S/C13H19N3O7/c1-6(2)12(19)22-5-7-9(17)10(18)11(23-7)16-4-3-8(15-21)14-13(16)20/h3-4,6-7,9-11,17-18,21H,5H2,1-2H3,(H,14,15,20)/t7-,9-,10-,11-/m1/s1
InchiKey HTNPEHXGEKVIHG-QCNRFFRDSA-N
分子式 Formula C13H19N3O7
分子量 Molecular Weight 329.1223
溶解度Solubility
性狀 固體粉末
儲藏條件 Storage conditions Store at -4℃;干燥避光存儲,短期運輸時(-4℃)長期存儲-20℃。
Tag:Influenza Virus;Viral Immunology;Inhibitor;抑制劑;EIDD-2801廠家;EIDD 2801抑制劑
產(chǎn)品說明 EIDD-2801(CAS:2349386-89-4) is an orally bioavailable isopropylester cytidine analog being investigated to treat COVID-19.
IntroductionEIDD-2801 is the isopropylester prodrug of N4-hydroxycytidine.1,2 With improved oral bioavailability in non human primates, it is hydrolyzed in vivo, and distributes into tissues where it becomes the active 5’-triphosphate form.2 The active drug incorporates into the genome of RNA viruses, leading to an accumulation of mutations known as viral error catastrophe.3 Recent studies have shown EIDD-2801 inhibits replication of human and bat coronaviruses, including SARS-CoV-2, in mice and human airway epithelial cells.1 A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine.1
Application1潛在冠狀病毒抑制劑Experimental Unapproved Treatments for COVID-19
Application2EIDD-2801 is a potent broad-spectrum antiviral agent. It is a useful tool for newly emerging coronavirus infections of the future.
Application3

EIDD-2801在體內(nèi)水解成為為N4-羥基胞苷,N4-羥胞苷在組織中被磷酸化為活性5'-三磷酸形式,并摻入新病毒體的基因組中,導致病毒失活突變的積累。
A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine

EIDD-2801 is an orally bioavailable prodrug of the ribonucleoside analog EIDD-1931. It has broad-spectrum antiviral activity against influenza virus and multiple coronaviruses, such as SARS-CoV-2, MERS-CoV, SARS-CoV. EIDD-2801 has the potential for COVID-19, and seasonal and pandemic influenza treatment.
EIDD-2801是核糖核苷類似物EIDD-1931的口服生物可利用的前藥。它具有針對流感病毒和多種冠狀病毒(如SARS-CoV-2,MERS-CoV,SARS-CoV)的廣譜抗病毒活性。 EIDD-2801具有抑制COVID-19以及季節(jié)性和大流行性流感病毒的潛在能力。
EIDD-2801 is the isopropylester prodrug of N4-hydroxycytidine.1,2 With improved oral bioavailability in non human primates, it is hydrolyzed in vivo, and distributes into tissues where it becomes the active 5’-triphosphate form.The active drug incorporates into the genome of RNA viruses, leading to an accumulation of mutations known as viral error catastrophe. Recent studies have shown EIDD-2801 inhibits replication of human and bat coronaviruses, including SARS-CoV-2, in mice and human airway epithelial cells.1 A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine.

In vivo:
         
50, 150, or 500 mg/kg EIDD-2801 orally administered in the intranasal infection mouse-adapted SARS-CoV (SARS-MA15). The body weight loss compared to vehicle treatment was significantly diminished (50 mg/kg) or prevented (150, 500 mg/kg) with EIDD-2801 prophylaxis. Therefore, EIDD-2801 is robustly antiviral and able to prevent SARS-CoV replication and disease. Altogether, therapeutic EIDD-2801 is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit was dependent on the time of initiation postinfection.


 

警示圖
危險性
危險性警示 Not Available
安全聲明 NA
安全防護 實驗過程防止食如、吸入
備注 NA
T. P. Sheahan 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.. 2.Toots M, Yoon JJ, Cox RM, Hart M, Sticher ZM, Makhsous N, Plesker R, Barrena AH, Reddy PG, Mitchell DG, Shean RC, Bluemling GR, Kolykhalov AA, Greninger AL, Natchus MG, Painter GR, Plemper RK: Characterization of orally efficacious influenza drug with high resistance barrier in ferrets and human airway epithelia. Sci Transl Med. 2019 Oct 23;11(515). pii: 11/515/eaax5866. doi: 10.1126/scitranslmed.aax5866. [PubMed:31645453]
Hampton T: New Flu Antiviral Candidate May Thwart Drug Resistance. JAMA. 2020 Jan 7;323(1):17. doi: 10.1001/jama.2019.20225. [PubMed:31910262]
Sheahan TP, et al. Sci Transl Med. 2020 Apr 6. pii: eabb5883.
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