Referencia número: HY-12353A

Pimodivir

(Synonyms: VX-787)

8 Cited Publications

Revisión del cliente

Based on 8 publication(s) in Google Scholar

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

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Pureza: 99.62%
No. CAS: 1629869-44-8
Fòrmula: C₂₀H₁₉F₂N₅O₂
Peso molecular:399.39

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Pimodivir Chemical Structure

No. CAS: 1629869-44-8

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Actividad biológica
- Descripciòn
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (8)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

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

Cellular Effect

Cell Line	Type	Value	Description	References
A549	CC₅₀	20 μM Compound: 3; JNJ-63623872	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 31493987]
CCRF-CEM	CC₅₀	48.9 μM Compound: 3; JNJ-63623872	Cytotoxicity against human CEM cells Cytotoxicity against human CEM cells	[PMID: 31493987]
Huh-7	CC₅₀	95.8 μM Compound: 3; JNJ-63623872	Cytotoxicity against human HuH7 cells Cytotoxicity against human HuH7 cells	[PMID: 31493987]
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	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	<0.00015 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	EC₅₀	<0.15 nM 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	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	0.32 nM 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	0.59 nM 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	0.002 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	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	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]
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	>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]
PBMC	CC₅₀	>100 μM Compound: 3; JNJ-63623872	Cytotoxicity against human PBMC cells Cytotoxicity against human PBMC cells	[PMID: 31493987]
Vero	CC₅₀	>100 μM Compound: 3; JNJ-63623872	Cytotoxicity against African green monkey Vero cells Cytotoxicity against African green monkey Vero cells	[PMID: 31493987]

In Vitro

Pimodivir rescues macrophages from virus-mediated death at non-cytotoxic concentrations 24 hpi. The EC₅₀ value for Pimodivir are 8 and 12 nM for A(H1N1) and A(H3N2) strains, respectively, whereas the CC₅₀ values are >1 μM, giving selectivity indexes (SI) > 125 and > 83 for A(H1N1) and A(H3N2) strains, respectively. Pimodivir significantly attenuates the transcription of viral M1 RNA in macrophages, which are infected with A(H1N1) or A(H3N2) strains for 8 h. Pimodivir inhibits the transcription of viral but not cellular genes. Pimodivir allows some activation of IAV-mediated expression of several cellular genes, which are involved in tryptophan and nucleotide metabolism. Pimodivir possesses excellent anti-IAV but not immuno/metabolo-modulating effect^[2].
Pimodivir (VX-787) is very potent against influenza A strains, including pandemic 2009 H1N1 and avian H5N1^[3].
Pimodivir (VX-787) shows potent activity against all influenza A virus strains tested, with an EC₅₀ range of 0.13 to 3.2 nM. Pimodivir-selected PB2 variant viruses maintain susceptibility to neuraminidase inhibitors in vitro^[4].

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

In Vivo

Pimodivir (2, 6, and 20 mg/kg/day, p.o.) and GS 4071 (20 mg/kg/day) completely prevent death in the H1N1pdm virus infection in mice. Pimodivir (20 mg/kg/day) is more effective than GS 4071 (20 mg/kg/day) in improving body weight and reducing the severity of lung infection^[1].
Moreover, Pimodivir (VX-787) shows 100% survival in a +48 h delay to treatment mouse influenza model at 10, 3 and 1 mpk (BID × 10 days) whereas the SOC, GS 4071, provide no survival benefit in this model at 10 mpk^[3].
Pimodivir (VX-787; 1, 3, or 10 mg/kg, bid) provided complete survival, with a dose-dependent reduction in BW loss of the mice^[4].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1629869-44-8
Appearance Solid
Peso molecular 399.39
Fòrmula C₂₀H₁₉F₂N₅O₂
Color White to light yellow
SMILES

O=C([C@H]1C(CC2)CCC2[C@@H]1NC3=NC(C4=CNC5=NC=C(F)C=C54)=NC=C3F)O
Synonyms

VX-787
Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (8)

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NPJ Digit Med

Predictive modeling & mechanistic validation of synergistic pimodivir combinations for anti-influenza therapy via PB2cap affinity boost. [Abstract]

2025 Nov 21;8(1):712. PMID: 41272280
Nucleic Acids Res

Capped RNA primer binding to influenza polymerase and implications for the mechanism of cap-binding inhibitors. [Abstract]

2018 Jan 25;46(2):956-971. PMID: 29202182
Cell Rep Med

Human liver-derived organoids recapitulate Oropouche virus infection and manifestation, enabling antiviral drug discovery. [Abstract]

2026 Mar 9:102646. PMID: 41806841
Antiviral Res

High-throughput screening for identification of influenza a inhibitors using a cell-based immunofluorescence assay. [Abstract]

2025 Aug:240:106209. PMID: 40484321
Antiviral Res

Susceptibility of widely diverse influenza a viruses to PB2 polymerase inhibitor pimodivir. [Abstract]

2021 Apr:188:105035. PMID: 33581212
ACS Infect Dis

Development of a Universal Type A Influenza Viral RdRp-Induced Reporter System with Potential for Antiviral Drug Screening. [Abstract]

2025 Jun 13;11(6):1437-1447. PMID: 40421776
SLAS Discov

High-Throughput cell-based immunofluorescence assays against influenza. [Abstract]

2024 Jan;29(1):66-76. PMID: 37925159
bioRxiv

2021 Jan 5.

Solvente y solubilidad

In Vitro:

DMSO : 5 mg/mL (12.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.26 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

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.

MedChemExpress (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.

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (286 KB)
SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

Keywords

Pimodivir

8 Cited Publications

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Pimodivir

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Pimodivir

Actividad biológica

Chemical Information

Publications (8)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pimodivir

Anti-Infection Compound Library

Clinical Compound Library

Antiviral Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

Orally Active Compound Library

Heterocyclic Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Pimodivir

Actividad biológica

Chemical Information

Publications (8)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Pimodivir Related Classifications

HY-12353A Related Classifications