Nucleozin
(Synonyms: [4-(2-氯-4-硝基苯基)-1-哌嗪基](5-甲基-3-苯基-4-异噁唑基)-甲酮) 目录号 : GC15303An antiviral
Cas No.:341001-38-5
Sample solution is provided at 25 µL, 10mM.
Nucleozin Description:EC50: Nucleozin inhibited infection of MDCK cells by the viruses influenza A/WSN/33, H3N2 (clinical isolate) and Vietnam/1194/04 (H5N1) with an EC50 of 0.069±0.003 μM, 0.16±0.01 μM and 0.33±0.04 μM in PRA, respectively [1].
Influenza nucleoprotein is the most abundantly expressed protein during the course of infection with multiple functionalities. In the presence of nucleozin, a potent antagonist of NP accumulation in the nucleus, NP failed to enter the nucleus leading to the virus death [1].
In vitro: Nucleozin was found to effectively inhibite viral growth even when added within 6 h after inoculation of the MDCK cells with the virus, indicating that the antiviral activities of nucleozin reside on post-entry and post-nuclear events, suggesting that multiple processes involving NP may be affected, although only the nuclear import process of NP can be readily observed [1]. However, another in-vitro study demonstrated that the primary target of nucleozin was the viral ribonucleoprotein, not NP, and this work also provided proof of the principle that IAV replication can be effectively inhibited by blocking cytoplasmic trafficking of the viral genome [2].
In vivo: With respect to in vivo antiviral efficacy, mice treated with nucleozin had a considerably higher survival rate after inoculation by influenza A virus H5N1 strain A/Vietnam/1194/04 than untreated controls. Without any treatment, all mice had died 7 d after inoculation. In the nucleozin-treated group, 50% of those receiving two doses of nucleozin (100 μl of 2.3 mg/ml nucleozin) per day for 7 d survived for more than 21 d. The animal study results show that nucleozin protected mice against hypervirulent influenza A H5N1 virus in vivo and thus has the potential to be developed into useful anti-influenza therapeutics [1].
Clinical trial: Up to now, nucleozin is still in the preclinical development stage.
Reference:
[1] Kao RY, Yang D, Lau LS, Tsui WH, Hu L, Dai J, Chan MP, Chan CM, Wang P, Zheng BJ, Sun J, Huang JD, Madar J, Chen G, Chen H, Guan Y, Yuen KY. Identification of influenza A nucleoprotein as an antiviral target. Nat Biotechnol. 2010;28(6):600-5.
[2] Amorim MJ, Kao RY, Digard P. Nucleozin targets cytoplasmic trafficking of viral ribonucleoprotein-Rab11 complexes in influenza A virus infection. J Virol. 2013;87(8):4694-703.
Cas No. | 341001-38-5 | SDF | |
别名 | [4-(2-氯-4-硝基苯基)-1-哌嗪基](5-甲基-3-苯基-4-异噁唑基)-甲酮 | ||
化学名 | [4-(2-chloro-4-nitrophenyl)piperazin-1-yl]-(5-methyl-3-phenyl-1,2-oxazol-4-yl)methanone | ||
Canonical SMILES | CC1=C(C(=NO1)C2=CC=CC=C2)C(=O)N3CCN(CC3)C4=C(C=C(C=C4)[N+](=O)[O-])Cl | ||
分子式 | C21H19ClN4O4 | 分子量 | 426.86 |
溶解度 | ≥ 55.4 mg/mL in DMSO with ultrasonic, ≥ 3.28 mg/mL in EtOH with ultrasonic and warming | 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 | 2.3427 mL | 11.7134 mL | 23.4269 mL |
5 mM | 0.4685 mL | 2.3427 mL | 4.6854 mL |
10 mM | 0.2343 mL | 1.1713 mL | 2.3427 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。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet