Pimodivir (Synonyms: VX-787)

目录号: HY-12353A 纯度: 99.83%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Pimodivir (VX-787) 是一种可口服的甲型流感病毒聚合酶抑制剂，通过抑制PB2亚基起作用。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Pimodivir Chemical Structure

CAS No. : 1629869-44-8

1. 客户无需承担相应的运输费用。

2. 同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

可免费申领三个不同产品的试用装。

3. 试用装只面向终端客户。

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥990	In-stock
5 mg	￥900	In-stock
10 mg	￥1500	In-stock
50 mg	￥5100	In-stock
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

Other Forms of Pimodivir:

Pimodivir hydrochlorid hemihydrate 询价

MCE 顾客使用本产品发表的 5 篇科研文献

Pimodivir 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

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

细胞效力
(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]

体外研究
(In Vitro)

Pimodivir 在 24 hpi 的非细胞毒性浓度下从病毒介导的死亡中拯救巨噬细胞。对于 A (H1N1) 和 A (H3N2) 毒株，Pimodivir 的 EC₅₀ 值分别为 8 和 12 nM，而 CC₅₀ 值 >1 μM，给出A (H1N1) 和 A (H3N2) 毒株的选择性指数 (SI) 分别 > 125 和 > 83。Pimodivir 显著减弱巨噬细胞中病毒 M1 RNA 的转录，巨噬细胞被 A (H1N1) 或 A (H3N2) 毒株感染 8 小时。Pimodivir 抑制病毒而非细胞基因的转录。Pimodivir 允许 IAV 介导的几种细胞基因表达的一些激活，这些基因参与色氨酸和核苷酸代谢。Pimodivir 具有出色的抗 IAV 但没有免疫/代谢调节作用^[2]。
Pimodivir (VX-787) 对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) 显示出对所有测试的甲型流感病毒株的有效活性，EC₅₀ 范围为 0.13 至 3.2 nM。Pimodivir 选择的 PB2 变异病毒在体外保持对神经氨酸酶抑制剂的敏感性^[4]。

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

体内研究
(In Vivo)

Pimodivir（2、6 和 20 mg/kg/天，口服）和 GS 4071（20 mg/kg/天）可完全预防 H1N1pdm 病毒感染小鼠的死亡。Pimodivir（20 mg/kg/天）在改善体重和降低肺部感染严重程度方面比 GS 4071（20 mg/kg/天）更有效^[1]
。此外，Pimodivir (VX-787) 在延迟治疗 48 小时的小鼠流感模型中，在 10、3 和 1 mpk（BID × 10 天）时显示出 100% 的存活率，而 SOC、GS 4071 在 10 mpk时在此模型中没有提供存活获益^[3]
。Pimodivir（VX-787；1、3 或 10 mg/kg，每日两次）可提供完全存活，并且小鼠体重损失呈剂量依赖性减少^[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 号

1629869-44-8

性状

固体

颜色

White to light yellow

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	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 5 mg/mL (12.52 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	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
10 mM	0.2504 mL	1.2519 mL	2.5038 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.26 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.26 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（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。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.26 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
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。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.83%

选择批次：

Data Sheet (660 KB) SDS (393 KB)

COA (203 KB) HNMR (287 KB) LCMS (265 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Smee DF, et al. Activities of JNJ63623872 and GS 4071 against influenza A H1N1pdm and H3N2 virus infections in mice. Antiviral Res. 2016 Dec;136:45-50. [Content Brief]

[2]. Fu Y, et al. JNJ872 inhibits influenza A virus replication without altering cellular antiviral responses. Antiviral Res. 2016 Sep;133:23-31. [Content Brief]

[3]. Boyd MJ, et al. Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. Bioorg Med Chem Lett. 2015 May 1;25(9):1990-4. [Content Brief]

[4]. Byrn RA, et al. Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit. Antimicrob Agents Chemother. 2015 Mar;59(3):1569-82. [Content Brief]

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.
参考文献	[1]. Smee DF, et al. Activities of JNJ63623872 and GS 4071 against influenza A H1N1pdm and H3N2 virus infections in mice. Antiviral Res. 2016 Dec;136:45-50. [Content Brief] [2]. Fu Y, et al. JNJ872 inhibits influenza A virus replication without altering cellular antiviral responses. Antiviral Res. 2016 Sep;133:23-31. [Content Brief] [3]. Boyd MJ, et al. Isosteric replacements of the carboxylic acid of drug candidate VX-787: Effect of charge on antiviral potency and kinase activity of azaindole-based influenza PB2 inhibitors. Bioorg Med Chem Lett. 2015 May 1;25(9):1990-4. [Content Brief] [4]. Byrn RA, et al. Preclinical activity of VX-787, a first-in-class, orally bioavailable inhibitor of the influenza virus polymerase PB2 subunit. Antimicrob Agents Chemother. 2015 Mar;59(3):1569-82. [Content Brief]

Pimodivir 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	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.

Keywords:

Pimodivir1629869-44-8VX-787VX787VX 787Influenza VirusInhibitorinhibitorinhibit

产品名称：			* 需求量：
* 客户姓名：			* Email：
* 电话：			* 公司或机构名称：
留言给我们：

产品名称：			* Lot #：
* 客户姓名：			* Email：
电话：			* 部门：
* 公司或机构名称：
留言给我们：

MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。	站点地图隐私声明
沪ICP备15051369号-4 上海工商沪公网安备31011502019417 沪(浦)应急管危经许[2021]201709(QFYS) 营业执照（三证合一）
Copyright © 2013-2024 MedChemExpress. All Rights Reserved.

Pimodivir (Synonyms: VX-787)

Customer Review

Other Forms of Pimodivir:

MCE 顾客使用本产品发表的 5 篇科研文献

Pimodivir 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

摩尔计算器

稀释计算器

Pimodivir 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

姓名
邮箱 *

Sorry, but the email address you supplied was invalid.

Pimodivir (Synonyms: VX-787)

Customer Review

Other Forms of Pimodivir:

Pimodivir 相关抗体

MCE 顾客使用本产品发表的 5 篇科研文献

Pimodivir 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

Pimodivir 相关抗体:

摩尔计算器

稀释计算器

Pimodivir 相关分类

完整储备液配制表

Keywords:

您最近查看的产品:

Request for HNMR Report

Request for HNMR Report

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z