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    N4-羥基胞苷

    貨品編碼 規格 純度 價格 (¥) 現價(¥) 特價(¥) 庫存描述 數量 總計 (¥)
    HCQ000013-1kg 1kg 98.36% ¥ 0.00 ¥ 0.00 Get quote
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    中文別名 N4-羥基胞苷;4-N-羥基胞苷; β-D-N-4-羥基胞苷; β-D-N4-羥基胞苷; N(4)-羥基胞苷; NHC; 尿苷,4-肟; β-D-N4-羥基胞苷
    英文別名 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號 3258-02-4
    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 Molecular Weight C3D11PV2O4
    分子量 Formula 259.0804352
    溶解度Solubility Water Solubility,34.4 mg/mL;
    性狀 固體粉末,Powder
    儲藏條件 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;需要超聲);Water Solubility :34.4 mg/mL
    產品說明 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潛在冠狀病毒抑制劑Experimental Unapproved Treatments for COVID-19
    Application2
    Application3
    關于N4-羥基胞苷過量的數據不容易獲得。 N4-羥基胞苷對SARS-CoV-2臨床分離株的治療指數有望> 100,體外IC50為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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