Favipiravir (Synonyms:法匹拉韦; T-705)
目录号 : KM7590 CAS No. : 259793-96-9 纯度 : 98%

Favipiravir (T-705) 是一种病毒 RNA 聚合酶 (RNA polymerase) 抑制剂,可转变为其活性形式 Favipiravir-ribofuranosyl-5′-triphosphate (RTP)。Favipiravir-RTP 抑制流感病毒RNA依赖性的RNA聚合酶 (RdRP) 活性,IC50 为 341 nM。

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10mg
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50mg
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100mg
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200mg 询价 In-stock
500mg 询价 In-stock

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生物活性

Favipiravir (T-705) is a potent 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 an IC50 of 341 nM.

体外研究

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. 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%).

体内研究

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.

分子式
C5H4FN3O2
分子量
157.10
CAS号
259793-96-9
中文名称
法匹拉韦
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 100 mg/mL (636.54 mM)

H2O : 6.25 mg/mL (39.78 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 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
*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制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

  • 1.

    请依序添加每种溶剂: PBS

    Solubility: 4.55 mg/mL (28.96 mM); Clear solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (15.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (15.91 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (15.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (15.91 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

  • 4.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (15.91 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (15.91 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 5.

    请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% saline

    Solubility: ≥ 2.5 mg/mL (15.91 mM); Clear solution

  • 6.

    请依序添加每种溶剂: 5% DMSO    95% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (15.91 mM); Clear solution

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