产品说明书

Zanamivir

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Chemical Structure| 139110-80-8 同义名 : GG 167;GR 121167X
CAS号 : 139110-80-8
货号 : A124461
分子式 : C12H20N4O7
纯度 : 98%
分子量 : 332.31
MDL号 : MFCD00866966
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 30 mg/mL(90.28 mM)
动物实验配方：
生物活性
描述 Zanamivir is a potent competitive inhibitor of viral neuraminidase, and inhibits a wide range of influenza A and B types in vitro . The drug is selective for the viral form of the neuraminidase enzyme and does not interact to any significant extent with its human lysosomal equivalent[3]. In Madin-Darby canine kidney (MDCK) cell cultures, IC50 values for zanamivir (i.e. the drug concentration required to inhibit plaque formation of influenza A and B viruses by 50%) in laboratory passaged isolates (0.004 to 0.014 μmol/L) and clinical isolates (0.002 to 16 μmol/L) were largely lower than values for amantadine >25 μmol/L), rimantadine (<0.27 to >25 μmol/L) and ribavirin (6.1 to 54 μmol/L)[4]. Zanamivir was also effective in the inhibition of influenza A [A/Virginia/88 (H3N2) and A/Texas/36/91 (H1N1)] and B (B/Hong Kong/5/72) strains in yield reduction assays in human respiratory epithelium, with concentrations required for 90% inhibition of viral replication (IC90) of <0.03 and 0.75 μmol/L, respectively[5]. In MDCK cell cultures,IC50 values for zanamivir ranged from <0.01 to >100 μmol/L and <0.01 to 21 μmol/L against influenza A strains, from 0.03 to 1.3 μmol/L against influenza B strains[6]. Intranasal zanamivir was 100 to 1000 times more active against influenza A [A/Singapore/1/57(H2N2) and A/Mississippi/1/85 (H3N3)] and B(B/Victoria/102/85) than were amantadine and ribavirin in animal studies. In addition, delayed administration of the drug (for up to 22 hours postinfection) reduced viral replication in ferrets[5].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00705406 Acute, Uncomplicated Human Inf... 展开 >>luenza 收起 << Phase 2 Completed - -
NCT00958776 Cough Sore Th... 展开 >>roat Nasal Congestion Headache Fever Seasonal Influenza 收起 << Phase 3 Terminated(This study was term... 展开 >>inated for futility) 收起 << - -
NCT00705406 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.05mL

3.01mL

1.50mL

30.09mL

6.02mL

3.01mL
参考文献

[1]McKimm-Breschkin JL. Management of influenza virus infections with neuraminidase inhibitors: detection, incidence, and implications of drug resistance. Treat Respir Med. 2005;4(2):107-16.

[2]Gubareva LV, Webster RG, et al. Comparison of the activities of zanamivir, oseltamivir, and RWJ-270201 against clinical isolates of influenza virus and neuraminidase inhibitor-resistant variants. Antimicrob Agents Chemother. 2001 Dec;45(12):3403-8.

[3] Susan M Cheer ,et al. Zanamivir: an update of its use in influenza. Drugs. 2002;62(1):71-106.

[4]Woods JM, et al. 4-Guanidino-2,4-dideoxy-2,3-dehydro-N-acetylneuraminic acid is a highly effective inhibitor both of the sialidase (neuraminidase) and of growth of a wide range of influenza A and B viruses in vitro . Antimicrob Agents Chemother 1993 Jul: 1473-9.

[5]Hayden FG, Rollins BS, Madren LK. Anti-influenza virus activity of the neuraminidase inhibitor 4-guanidino-Neu5Ac2en in cell culture and in human respiratory epithelium. Antiviral Res 1994; 25: 123-31

[6]Smee DF, Huffman JH, Morrison AC, et al. Cyclopentane neuraminidase inhibitors with potent in vitro anti-influenza virus activities. Antimicrob Agents Chemother 2001 Mar; 45 (3):743-8