Zanamivir
(Synonyms: 扎那米韦) 目录号 : GC10984An inhibitor of influenza neuraminidase
Cas No.:139110-80-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment [1,2]: | |
Cell lines |
HeLa-CD4-LTR-βgal cells and HeLa-tat cell, CV-1 cell |
Preparation method |
The solubility of this compound in DMSO is >16.6mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition |
5 nM-10 mM |
Applications |
In HeLa-CD4-LTR-βgal cells, zananivir interfered with cell-cell fusion with the IC50 of 0.19 mM. In CV-1 cell monolayers, zananivir (0.5 mM) reduced plaque area by 97%. Zananivir caused a concentration-dependent inhibition of hemadsorption. Zananivir (5 mM) strikingly reduced lipid mixing. zanamivir suppressed the growth of influenza A and B viruses with IC50 values of 5 nM-14 nM for laboratory-passaged strains and from 20 nM-16 μM for clinical isolates. |
Animal experiment [2]: | |
Animal models |
Mice infected with influenza A |
Dosage form |
Intranasal, 0.01-4 mg/kg |
Application |
Intranasal zananivir treatment given prophylactically plus twice daily over days 0 to 3 in mice infected with influenza A reduced mortality and viral titres in lung homogenated and improved lung consolidation scores over 10 days. |
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Greengard O, Poltoratskaia N, Leikina E, et al. The anti-influenza virus agent 4-GU-DANA (zanamivir) inhibits cell fusion mediated by human parainfluenza virus and influenza virus HA[J]. Journal of virology, 2000, 74(23): 11108-11114. [2]. Elliott M. Zanamivir: from drug design to the clinic[J]. Philosophical Transactions of the Royal Society of London. Series B, 2001, 356(1416): 1885. |
Zanamivir is a selective inhibitor of influenza A and B virus neuraminidases with IC50 values of 0.64-7.9nM [1].
Influenza A and B viruses are negative-strand RNA viruses. Neuraminidase is one of the two glycoproteins present on the surface of the virus. It is important to the pathogenicity and infectivity of the virus. The neuraminidases inhibitor, zanamivir, is a sialic acid analogue. It inhibits neuraminidases to cleave sialic acid on the surface of host cells and influenza viral envelope. In the in vitro assay, zanamivir suppresses the growth of influenza A and B viruses with IC50 values ranging from 5nM to 14nM for laboratory-passaged strains and from 20nM to 16μM for clinical isolates. In animal models infected with influenza A and B, treatment of zanamivir reduces the mortality and viral titres in lung homogenates and improves lung consolidation scores [1].
References:
[1] Elliott M. Zanamivir: from drug design to the clinic. Philos Trans R Soc Lond B Biol Sci, 2001, 356(1416): 1885-93.
Cas No. | 139110-80-8 | SDF | |
别名 | 扎那米韦 | ||
化学名 | (2R,3R,4S)-3-acetamido-4-(diaminomethylideneamino)-2-[(1R,2R)-1,2,3-trihydroxypropyl]-3,4-dihydro-2H-pyran-6-carboxylic acid | ||
Canonical SMILES | CC(=O)NC1C(C=C(OC1C(C(CO)O)O)C(=O)O)N=C(N)N | ||
分子式 | C12H20N4O7 | 分子量 | 332.31 |
溶解度 | ≥ 8.99 mg/mL in Water; 66 mg/mL in DMSO ( Need ultrasonic) | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
||
Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.0092 mL | 15.0462 mL | 30.0924 mL |
5 mM | 0.6018 mL | 3.0092 mL | 6.0185 mL |
10 mM | 0.3009 mL | 1.5046 mL | 3.0092 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。