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3258-02-4
  • names:

    N4-Hydroxycytidine

  • CAS号:

    3258-02-4

    MDL Number:
  • MF(分子式): C3D11PV2O4 MW(分子量): 259.0804352
  • EINECS: Reaxys Number:
  • Pubchem ID:197020 Brand:BIOFOUNT
N4-羟基胞苷
货品编码 规格 纯度 价格 (¥) 现价(¥) 特价(¥) 库存描述 数量 总计 (¥)
HCQ000013-1kg 1kg 98.36% ¥ 0.00 ¥ 0.00 Get quote
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¥ 0.00
HCQ000013-100mg 100mg 98.36% ¥ 18000.00 ¥ 18000.00 Instock
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¥ 0.00
HCQ000013-50mg 50mg 98.36% ¥ 13200.00 ¥ 13200.00 Instock
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¥ 0.00
HCQ000013-25mg 25mg 98.36% ¥ 7920.00 ¥ 7920.00 Instock
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¥ 0.00
HCQ000013-10mg 10mg 98.36% ¥ 4400.00 ¥ 4400.00 Instock
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¥ 0.00
HCQ000013-5mg 5mg 98.36% ¥ 2800.00 ¥ 2800.00 Instock
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¥ 0.00
HCQ000013-1mg 1mg 98.36% ¥ 960.00 ¥ 960.00 Instock
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¥ 0.00
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中文别名 N4-羟基胞苷;4-N-羟基胞苷; β-D-N-4-羟基胞苷; β-D-N4-羟基胞苷; N(4)-羟基胞苷; NHC; 尿苷,4-肟; β-D-N4-羟基胞苷
英文别名 4-N-Hydroxycytidine; beta-D-N-4-Hydroxycytidine; Beta-D-N4-hydroxycytidine; N(4)-Hydroxycytidine; NHC; Uridine, 4-oxime; β-D-N4-hydroxycytidine;1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-4-(hydroxyamino)-1,2-dihydropyrimidin-2-one
CAS号 3258-02-4
SMILES OC[C@H]1O[C@H]([C@H](O)[C@@H]1O)N1C=CC(NO)=NC1=O
Inchi InChI=1S/C9H13N3O6/c13-3-4-6(14)7(15)8(18-4)12-2-1-5(11-17)10-9(12)16/h1-2,4,6-8,13-15,17H,3H2,(H,10,11,16)/t4-,6-,7-,8-/m1/s1
InchiKey XCUAIINAJCDIPM-XVFCMESISA-N
分子式 Formula C3D11PV2O4
分子量 Molecular Weight 259.0804352
闪点 FP 302.2±32.9 °C
熔点 Melting point NA
沸点 Boiling point 576.1±60.0 °C at 760 mmHg
Polarizability极化度 21.7±0.5 10-24cm3
密度 Density 1.9±0.1 g/cm3
蒸汽压 Vapor Pressure 0.0±3.6 mmHg at 25°C
溶解度Solubility
性状 固体粉末,Powder
储藏条件 Storage conditions Store at -4℃
 
Stock Solutions of N4-Hydroxycytidine 
Concentration\Solvent\Mass 1mg                 5mg                        10mg              
1 mM  3.8577 mL 19.2886 mL 38.5773 mL
5mM  0.7715 mL  3.8577 mL 7.7155 mL
10mM  0.3858 mL 1.9289 mL 3.8577 mL
DMSO:250 mg / mL(964.43 mM;需要超声);Water Solubility :34.4 mg/mL
产品说明 A cytidine analog being investigated to treat COVID-19.
IntroductionN4-Hydroxyctidine, or EIDD-1931, is a ribonucleoside analog which induces mutations in RNA virions.1,2 N4-hydroxycytidine was first described in the literature in 1980 as a potent mutagen of bacteria and phage.5 It has shown antiviral activity against Venezuelan equine encephalitis virus,1 and the human coronavirus HCoV-NL63 in vitro.4 N4-hydroxycytodine has been shown to inhibit SARS-CoV-2 as well as other human and bat coronaviruses in mice and human airway epithelial cells.3 It is orally bioavailable in mice and distributes into tissue before becoming the active 5’-triphosphate form, which is incorporated into the genome of new virions, resulting in the accumulation of inactivating mutations.2 In non-human primates, N4-hydroxycytidine was poorly orally bioavailable.6 A remdesivir resistant mutant mouse hepatitis virus has also been shown to have increased sensitivity to N4-hydroxycytidine.3 The prodrug of N4-hydroxycytidine, EIDD-2801, is also being investigated for its broad spectrum activity against the coronavirus family of viruses.3
Application1潜在冠状病毒抑制剂Experimental Unapproved Treatments for COVID-19
Application2
Application3
关于N4-羟基胞苷过量的数据不容易获得。 N4-羟基胞苷对SARS-CoV-2临床分离株的治疗指数有望> 100,体外IC50为0.3µM,CC50> 10µM。
Data regarding overdose of N4-hydroxycytidine is not readily available. The therapeutic index of N4-hydroxycytidine against a clinical isolate of SARS-CoV-2 is expected to be >100, with an in vitro IC50 of 0.3µM and a CC50 of >10µM.
Urakova N, Kuznetsova V, Crossman DK, Sokratian A, Guthrie DB, Kolykhalov AA, Lockwood MA, Natchus MG, Crowley MR, Painter GR, Frolova EI, Frolov I: beta-d-N (4)-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). pii: JVI.01965-17. doi: 10.1128/JVI.01965-17. Print 2018 Feb 1. [PubMed:29167335]
Painter GR, Bowen RA, Bluemling GR, DeBergh J, Edpuganti V, Gruddanti PR, Guthrie DB, Hager M, Kuiper DL, Lockwood MA, Mitchell DG, Natchus MG, Sticher ZM, Kolykhalov AA: The prophylactic and therapeutic activity of a broadly active ribonucleoside analog in a murine model of intranasal venezuelan equine encephalitis virus infection. Antiviral Res. 2019 Nov;171:104597. doi: 10.1016/j.antiviral.2019.104597. Epub 2019 Sep 5. [PubMed:31494195]
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.. 4.Pyrc K, Bosch BJ, Berkhout B, Jebbink MF, Dijkman R, Rottier P, van der Hoek L: Inhibition of human coronavirus NL63 infection at early stages of the replication cycle. Antimicrob Agents Chemother. 2006 Jun;50(6):2000-8. doi: 10.1128/AAC.01598-05. [PubMed:16723558]
Sledziewska E, Janion C: Mutagenic specificity of N4-hydroxycytidine. Mutat Res. 1980 Mar;70(1):11-6. doi: 10.1016/0027-5107(80)90053-6. [PubMed:7366595]
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. 
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