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  2. Anti-infection
  3. Influenza Virus
  4. Pimodivir

Pimodivir (VX-787) 是一種可口服的甲型流感病毒聚合酶抑制劑，通過抑制PB2亞基起作用。

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Pimodivir Chemical Structure

Pimodivir Chemical Structure

CAS No. : 1629869-44-8

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規(guī)格 價(jià)格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥990
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5 mg ￥900
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10 mg ￥1500
In-stock
50 mg ￥5100
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100 mg 現(xiàn)貨 詢價(jià)
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500 mg   詢價(jià)  

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Customer Review

Other Forms of Pimodivir:

  • 生物活性

  • 實(shí)驗(yàn)參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

Pimodivir (VX-787) is an orally bioavailable inhibitor of influenza A virus polymerases through interaction with the viral PB2 subunit.

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
MDCK EC50
< 0.00015 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/Viet Nam/1203/2004(H5N1) infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/Viet Nam/1203/2004(H5N1) infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK CC50
> 100 μM
Compound: VX787
Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 72 hrs by alamar blue assay
Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 72 hrs by alamar blue assay
[PMID: 31053507]
MDCK CC50
> 100 μM
Compound: VX-787
Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 72 hrs by CCK8 analysis
Cytotoxicity against MDCK cells assessed as reduction in cell viability measured after 72 hrs by CCK8 analysis
[PMID: 34839161]
MDCK EC50
0.00032 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/Puerto Rico/8/34 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/Puerto Rico/8/34 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK EC50
0.00059 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/New York/18/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/New York/18/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK EC50
0.0018 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/California/07/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/California/07/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK IC50
0.002 μM
Compound: 1, VX-787
Antiviral activity against Influenza A virus A/PR/8/34 strain incubated with MDCK cells assessed as cell protection after 72 hrs by phenotypic cell protection assay
Antiviral activity against Influenza A virus A/PR/8/34 strain incubated with MDCK cells assessed as cell protection after 72 hrs by phenotypic cell protection assay
[PMID: 25827523]
MDCK EC50
0.002 μM
Compound: 1, VX-787
Antiviral activity against influenza A virus A/PR/8/34 strain incubated with MDCK cells assessed as reduction of viral RNA level equal to 1% of control level after 72 hrs by branched DNA assay
Antiviral activity against influenza A virus A/PR/8/34 strain incubated with MDCK cells assessed as reduction of viral RNA level equal to 1% of control level after 72 hrs by branched DNA assay
[PMID: 25827523]
MDCK EC50
0.0026 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/Georgia/20/2006 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/Georgia/20/2006 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK EC50
0.0027 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/Mexico/4108/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/Mexico/4108/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK EC50
0.0028 μM
Compound: 2, VX-787
Antiviral activity against Influenza A virus A/Texas/48/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
Antiviral activity against Influenza A virus A/Texas/48/2009 infected in MDCK cells assessed as cell protection after 3 days by cytopathic effect assay
[PMID: 25019388]
MDCK EC50
0.6 nM
Compound: VX-787
Inhibition of PB2 in Influenza A virus (A/Weiss/1943(H1N1)) infected in MDCK cells assessed as reduction in virus induced cell death after 5 days by CCK-8 assay
Inhibition of PB2 in Influenza A virus (A/Weiss/1943(H1N1)) infected in MDCK cells assessed as reduction in virus induced cell death after 5 days by CCK-8 assay
[PMID: 30448415]
MDCK CC50
12 μM
Compound: VX-787
Cytotoxicity against MDCK cells assessed as reduction in cell viability after 5 days by CCK-8 assay
Cytotoxicity against MDCK cells assessed as reduction in cell viability after 5 days by CCK-8 assay
[PMID: 30448415]
體外研究
(In Vitro)

Pimodivir 在 24 hpi 的非細(xì)胞毒性濃度下從病毒介導(dǎo)的死亡中拯救巨噬細(xì)胞。對于 A (H1N1) 和 A (H3N2) 毒株，Pimodivir 的 EC50 值分別為 8 和 12 nM，而 CC50 值 >1 μM，給出A (H1N1) 和 A (H3N2) 毒株的選擇性指數(shù) (SI) 分別 > 125 和 > 83。Pimodivir 顯著減弱巨噬細(xì)胞中病毒 M1 RNA 的轉(zhuǎn)錄，巨噬細(xì)胞被 A (H1N1) 或 A (H3N2) 毒株感染 8 小時(shí)。Pimodivir 抑制病毒而非細(xì)胞基因的轉(zhuǎn)錄。Pimodivir 允許 IAV 介導(dǎo)的幾種細(xì)胞基因表達(dá)的一些激活，這些基因參與色氨酸和核苷酸代謝。Pimodivir 具有出色的抗 IAV 但沒有免疫/代謝調(diào)節(jié)作用[2]。
Pimodivir (VX-787) 對甲型流感病毒株非常有效，包括大流行性 2009 H1N1 和禽 H5N1[3]。
Pimodivir (VX-787) 顯示出對所有測試的甲型流感病毒株的有效活性，EC50 范圍為 0.13 至 3.2 nM。Pimodivir 選擇的 PB2 變異病毒在體外保持對神經(jīng)氨酸酶抑制劑的敏感性[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

Pimodivir（2、6 和 20 mg/kg/天，口服）和 GS 4071（20 mg/kg/天）可完全預(yù)防 H1N1pdm 病毒感染小鼠的死亡。Pimodivir（20 mg/kg/天）在改善體重和降低肺部感染嚴(yán)重程度方面比 GS 4071（20 mg/kg/天）更有效[1]
。此外，Pimodivir (VX-787) 在延遲治療 48 小時(shí)的小鼠流感模型中，在 10、3 和 1 mpk（BID × 10 天）時(shí)顯示出 100% 的存活率，而 SOC、GS 4071 在 10 mpk時(shí)在此模型中沒有提供存活獲益[3]
。Pimodivir（VX-787；1、3 或 10 mg/kg，每日兩次）可提供完全存活，并且小鼠體重?fù)p失呈劑量依賴性減少[4]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

399.39

Formula

C20H19F2N5O2
CAS 號(hào)
性狀

固體

顏色

White to light yellow

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.
儲(chǔ)存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn)： 

DMSO 中的溶解度 : 5 mg/mL (12.52 mM; 超聲助溶 (<60°C); 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 2.5038 mL 12.5191 mL 25.0382 mL
5 mM 0.5008 mL 2.5038 mL 5.0076 mL
查看完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質(zhì)量
=
濃度
×
體積
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn)：

請根據(jù)您的 實(shí)驗(yàn)動(dòng)物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

  • 方案 一

    請依序添加每種溶劑： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.26 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水 定容至 1 mL。

    生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
  • 方案 二

    請依序添加每種溶劑： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.26 mM); 澄清溶液

    此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。

    以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液 中，混合均勻。

    2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
動(dòng)物溶解方案計(jì)算器
請輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只
由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量
請輸入您的動(dòng)物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。
方案所需 助溶劑 包括：DMSO， ，均可在 MCE 網(wǎng)站選購。 ，Tween 80，均可在 MCE 網(wǎng)站選購。
計(jì)算結(jié)果
工作液所需濃度 : mg/mL
儲(chǔ)備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。
連續(xù)給藥周期超過半月以上，請謹(jǐn)慎選擇該方案。
請確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱 （超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。
純度 & 產(chǎn)品資料

純度: 99.83%

參考文獻(xiàn)
Cell Assay
[2]

The compound cytotoxicity and efficacy testing is performed in 96-well plates with macrophages at 95% confluence. The compounds are added to the medium, and 30 min later, the cells are infected with virus or non-infected. The cell viability is analyzed with the Cell Titer Glo assay at 24 hpi. The luminescence is read with a PHERAstar FS plate reader.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

The mice are anesthetized, and the animals are infected intranasally with a 90-μL suspension of influenza virus. The virus challenge is approximately four 50% mouse lethal infectious doses. Treatments are given twice a day (at 12 h intervals) for 10 days starting 2 h before virus challenge. Parameters for assessing the infection are survival, mean day of death, body weight changes, and lung infection parameters (hemorrhage score, weight, and virus titer). Animals are weighed individually every other day through day 21 of the infection. Initially, there are 15 mice per group treated with compound and 25 placebos. Five mice in each group are subsequently sacrificed for determination of lung infection parameters. A larger number of placebos are used than compound-treated mice to achieve greater statistical power, especially if some animals in that group survive the infection. One mouse that dies during the treatment period is presumed to have died from treatment trauma because its death occurs well before other mice die from influenza. It is excluded from the total counts. Animals that die during infection are accounted for in the tabular data.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

Pimodivir 相關(guān)分類

完整儲(chǔ)備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請?jiān)?年內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5038 mL 12.5191 mL 25.0382 mL 62.5955 mL
5 mM 0.5008 mL 2.5038 mL 5.0076 mL 12.5191 mL
10 mM 0.2504 mL 1.2519 mL 2.5038 mL 6.2595 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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產(chǎn)品名稱：
Pimodivir
目錄號(hào)：
HY-12353A
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