VP-14637
目录号 : GC11893
An RSV inhibitor
Cas No.:235106-62-4
Sample solution is provided at 25 µL, 10mM.
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EC50: 5.4 nM for RSV fusion
VP-14637 is an inhibitor of RSV.
Respiratory syncytial virus (RSV) is the leading cause of respiratory tract infections in humans. RSV F protein that mediates fusion of the viral envelope with the host cell membrane has become a target of anti-RSV treatment.
In vitro: Previous study demonstrated that VP-14637 did not block RSV adsorption but inhibited RSV-induced cell-cell fusion and specifically bound to RSV-infected cells. VP-14637 was capable of specifically interacting with the RSV fusion protein. RSV variants resistant to VP-14637 were selected, in which no mutations arose in HR1, indicating a mechanism other than direct disruption of the heptad repeat interaction. The F proteins containing the resistance mutations exhibited greatly reduced binding of VP-14637 [1].
In vivo: In cotton rats, animals given as little as 126 microg/kg of VP-14637 by small droplet aerosol starting 1 day after experimental virus infection with either a RSV A or B subtype consistently had significantly lower mean pulmonary RSV titers and reduced histopathological findings than mock-treated animals or cotton rats given placebo. In addition, no cotton rat treated with VP14637 had any evident untoward responses [2].
Clinical trial: So far, no clinical study has been conducted.
References:
[1] Douglas, J. L.,Panis, M.L.,Ho, E., et al. Inhibition of respiratory syncytial virus fusion by the small molecule VP-14637 via specific interactions with F protein. Journal of Virology 77(9), 5054-5064 (2003).
[2] Wyde PR, Laquerre S, Chetty SN, Gilbert BE, Nitz TJ, Pevear DC. Antiviral efficacy of VP14637 against respiratory syncytial virus in vitro and in cotton rats following delivery by small droplet aerosol. Antiviral Res. 2005 Oct;68(1):18-26.
| Cas No. | 235106-62-4 | SDF | |
| 化学名 | 2,2’-[(4-hydroxyphenyl)methylene]bis[4-[[(5-methyl-1H-tetrazol-1-yl)imino]methyl]-phenol | ||
| Canonical SMILES | OC1=CC=C(C(C2=CC(/C=N/N3C(C)=NN=N3)=CC=C2O)C4=CC(/C=N\N5N=NN=C5C)=CC=C4O)C=C1 | ||
| 分子式 | C25H22N10O3 | 分子量 | 510.5 |
| 溶解度 | ≤10mg/ml in ethanol;10mg/ml in DMSO | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.9589 mL | 9.7943 mL | 19.5886 mL |
| 5 mM | 0.3918 mL | 1.9589 mL | 3.9177 mL |
| 10 mM | 0.1959 mL | 0.9794 mL | 1.9589 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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet