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流感病毒 Neuraminidase
/ Zanamivir/扎那米韦

Zanamivir/扎那米韦 {[allProObj[0].p_purity_real_show]}

货号：A124461 同义名： GG 167; GR 121167X

Zanamivir 是一种神经氨酸酶抑制剂，广泛用于流感病毒复制机制的研究，同时也被报道可抑制 SARS-CoV-2 的 3CLpro 主蛋白酶。

Zanamivir/扎那米韦 化学结构 CAS号：139110-80-8
Zanamivir/扎那米韦 化学结构
CAS号：139110-80-8
Zanamivir/扎那米韦 3D分子结构
CAS号：139110-80-8
Zanamivir/扎那米韦 化学结构 CAS号：139110-80-8
Zanamivir/扎那米韦 3D分子结构 CAS号：139110-80-8
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Zanamivir/扎那米韦 纯度/质量文件 产品仅供科研

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全球学术期刊中引用的产品

• Nature, 2025, 645, 793-800. Ambeed. [ A201204 , A444152 , A344107 , A952055 ]
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• Sig. Transduct. Target. Ther., 2025, 10, 257. Ambeed. [ A104916 ]
• Nat. Nanotechnol., 2025. Ambeed. [ A243018 , A1216705 , A522597 , A125401 , A1355641 ]
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Zanamivir/扎那米韦 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].

Zanamivir/扎那米韦 细胞实验

Cell Line
Concentration Treated Time Description References
Madin-Darby canine kidney cells 8.5 to 14.0 µM (EC50) 18 hours Zanamivir inhibited the replication of H6N1 and H9N2 influenza viruses in MDCK cells, with EC50 ranging from 8.5 to 14.0 μM. Antimicrob Agents Chemother. 2001 Apr;45(4):1216-24.
Madin-Darby canine kidney cells (MDCK) 0.418 ng/ml (1.254 nM) 24 hours Evaluate the inhibitory effect of Zanamivir on A/Hong Kong (H275Y) virus, results showed the virus was susceptible to Zanamivir Antimicrob Agents Chemother. 2011 Apr;55(4):1747-53.
Calu-3 cells 35 μg/mL 48 hours Inhibition of H1N1 virus replication Int J Mol Sci. 2022 Dec 30;24(1):678.
A549 cells 35 μg/mL 48-72 hours Inhibition of H1N1 virus replication Int J Mol Sci. 2022 Dec 30;24(1):678.
MDCK cells 35 μg/mL 48-72 hours Inhibition of H1N1 virus replication Int J Mol Sci. 2022 Dec 30;24(1):678.

Zanamivir/扎那米韦 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Mice and ferrets Influenza virus infection model Intranasal administration 0.028 µmol/kg Dosing at 6, 24, and 48 hours post-infection, lasting for 72 hours To evaluate the inhibitory effect of polymer-attached Zanamivir (5a) on influenza virus infection in vivo. Results showed that 5a was more effective than small-molecule Zanamivir (1), reducing viral load by 190-fold in mice and 30-fold in ferrets. Pharm Res. 2014 Feb;31(2):466-74
BALB/c mice Avian influenza virus infection model Intranasal administration 10, 50, and 100 mg/kg Twice daily for 5 days Zanamivir significantly reduced virus titers in the lungs and completely blocked the spread of virus to the brain, increasing the mean survival day and the number of survivors infected with H6N1 and H5N1 viruses. Antimicrob Agents Chemother. 2001 Apr;45(4):1216-24.
C57BL/6 mice H1N1 infection model Intranasal administration 35 μg/mL Once daily for seven days Prevented weight loss, increased survival rate, and improved lung fibrosis Int J Mol Sci. 2022 Dec 30;24(1):678.
DBA/1J mice Collagen-induced arthritis (CIA) Intraperitoneal injection 50 mg/kg and 100 mg/kg Once daily, starting two days before immunization until the end of the experiment Zanamivir significantly ameliorated the clinical symptoms of CIA, delayed disease onset, and reduced the numbers of B-lineage cells, accompanied by inhibition of the humoral immune response. Int J Mol Sci. 2021 Jan 31;22(3):1428

Zanamivir/扎那米韦 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 - -

Zanamivir/扎那米韦 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

Zanamivir/扎那米韦 实验方案

计算器
存储液制备 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

Zanamivir/扎那米韦 技术信息

CAS号139110-80-8
分子式C12H20N4O7
分子量 332.31
SMILES Code O=C(C1=C[C@H](NC(N)=N)[C@@H](NC(C)=O)[C@H]([C@H](O)[C@H](O)CO)O1)O
MDL No. MFCD00866966
别名 GG 167; GR 121167X
运输蓝冰
InChI Key ARAIBEBZBOPLMB-UFGQHTETSA-N
Pubchem ID 60855
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C
溶解方案

H2O: 30 mg/mL(90.28 mM)

配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Zanamivir | GG 167;GR 121167X | Drug Standard | Influenza Virus | 3CLpro | Neuraminidase | AmBeed-信号通路专用抑制剂 | Zanamivir/扎那米韦 纯度/质量文件 | Zanamivir/扎那米韦 生物活性 | Zanamivir/扎那米韦 临床数据 | Zanamivir/扎那米韦 参考文献 | Zanamivir/扎那米韦 实验方案 | Zanamivir/扎那米韦 技术信息

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