T 705
(Synonyms: 法匹拉韦; T-705) 目录号 : GC12350
An antiviral agent
Cas No.:259793-96-9
Sample solution is provided at 25 µL, 10mM.
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Favipiravir (T-705) is a novel viral RNA polymerase inhibitor, it is phosphoribosylated by cellular enzymes to its active form, Favipiravir-ribofuranosyl-5′-triphosphate (RTP). Favipiravir-RTP inhibits the influenza viral RNA-dependent RNA polymerase (RdRP) activity with IC50 of 341 nM.
Favipiravir (T 705) is an antiviral drug that selectively inhibits the RNA-dependent RNA polymerase of influenza virus. Favipiravir (T 705) is a novel antiviral compound that selectively and potently inhibits the RNA-dependent RNA polymerase (RdRP) of influenza and many other RNA viruses. Favipiravir-RTP does not inhibit the human DNA polymerase α, β or γ with IC50>1 mM. The IC50 for the human RNA polymerase II is 905 μM; Favipiravir is therefore 2,650 times more selective for the influenza virus RdRP, consistent with the lack of inhibition of host-cell DNA and RNA synthesis[1]. Favipiravir (T 705) acts as a pro-drug, its cytotoxicity is expected to be cell-line dependent. Favipiravir inhibits in a dose-dependent manner MNV-induced CPE (EC50: 250±11 μM) and MNV RNA synthesis in cell culture (EC50:124±42 μM). Despite this rather modest antiviral activity, Favipiravir (T 705) is able to completely inhibit norovirus replication at a concentration of 100 μg/mL, which is a concentration that has little or no adverse effect on the host cell (cell viability >80%)[2].
Favipiravir (T 705) (30 mg/kg/day, orally) improves survival compare to placebo. Favipiravir (T 705) also provides significant protection against the A/Duck/MN/1525/81(H5N1) virus at a dose of 33 mg/kg/day or more, regardless of the number of daily doses. When given 4 times a day, all mice survive[1].
Reference:
[1]. Furuta Y, et al. Favipiravir (T-705), a novel viral RNA polymerase inhibitor. Antiviral Res. 2013 Nov;100(2):446-54.
[2]. Rocha-Pereira J, et al. Favipiravir (T-705) inhibits in vitro norovirus replication. Biochem Biophys Res Commun. 2012 Aug 10;424(4):777-80.
Cell experiment: | The antiviral activity of Favipiravir (T 705) is determined using an MTS-based CPE reduction assay in the MNV/RAW 264.7 cell line. To this end, RAW 264.7 cells are seeded (1×104 cells/well) in 96-well plates and infected with MNV at an MOI of 0,001 in the presence (or absence) of a dilution series of Favipiravir (T 705) (3.13-200 μg/mL). Following 3 days of incubation, i.e. until complete CPE is observed in infected untreated cells, cell culture supernatants are collected for quantification of viral RNA load by quantitative RT-PCR (qRT-PCR). For the MTS reduction assay an MTS/Phenazine methosulphate (PMS) stock solution (2 mg/mL MTS and 46 g/mL PMS in PBS at pH 6-6.5) is diluted 1/20 in MEM. To each well, 75 μL of MTS/PMS solution is added and the optical density (OD) is read at 498 nm 2 h later. The % CPE reduction is calculated as [(ODtreated)MNW−ODVC]/[ODCC-ODVC]×100, where ODCC represents the OD of the uninfected untreated cells, whereas ODVC and (ODtreated)CC represent the OD of infected untreated cells and virus-infected cells treated with a compound concentration, respectively. The EC50 is defined as the compound concentration that protected 50% of cells from virus-induced CPE. Adverse effects of the molecule on the host cell are also assessed by means of the MTS-method, by exposing uninfected cells to the same concentrations of Favipiravir for 3 days. The % cell viability is calculated as (ODtreated/ODCC)×100, where ODCC is the OD of uninfected untreated cells and ODtreated are uninfected cells treated with compound. The CC50 is defined as the compound concentration that reduces the number of viable cells by 50%. The selectivity index (SI) is calculated as CC50/EC50[2]. |
Animal experiment: | Mice[1] Favipiravir (T 705) has also been shown to protect mice against lethal infection by a variety of influenza virus strains. When Favipiravir is orally administered 2 or 4 times a day for 5 days in mice infected with lethal doses of influenza virus A/Victoria/3/75(H3N2), A/Osaka/5/70(H3N2) or A/Duck/MN/1525/81(H5N1). |
References: [1]. Furuta Y, et al. Favipiravir (T-705), a novel viral RNA polymerase inhibitor. Antiviral Res. 2013 Nov;100(2):446-54. | |
| Cas No. | 259793-96-9 | SDF | |
| 别名 | 法匹拉韦; T-705 | ||
| 化学名 | 5-fluoro-2-oxo-1H-pyrazine-3-carboxamide | ||
| Canonical SMILES | C1=C(N=C(C(=O)N1)C(=O)N)F | ||
| 分子式 | C5H4FN3O2 | 分子量 | 157.1 |
| 溶解度 | ≥ 6.2mg/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 | 6.3654 mL | 31.8269 mL | 63.6537 mL |
| 5 mM | 1.2731 mL | 6.3654 mL | 12.7307 mL |
| 10 mM | 0.6365 mL | 3.1827 mL | 6.3654 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
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet