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PB2-IN-2

Catalog No. T214847 Copy Product Info
🥰Excellent
PB2-IN-2 is an orally active PB2 inhibitor with RNP inhibitory activity (IC50) of 0.2 nM, cellular level replication inhibition activity (LRAEC50) of 0.8 nM, and cytopathic effect inhibition activity (CPEEC50) of 0.1 nM. It demonstrates nanomolar range broad-spectrum antiviral efficacy against various influenza A strains, including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, and rPR8(H1N1)/H7N9, with EC50 values of 1.5, 3.6, 3.7, 13.8, 2.9, and 9.8 nM, respectively, and CC50 values all greater than 2 μM. PB2-IN-2 also shows excellent metabolic stability and pharmacokinetic properties, making it suitable for influenza research.

PB2-IN-2

Copy Product Info
🥰Excellent
Catalog No. T214847

PB2-IN-2 is an orally active PB2 inhibitor with RNP inhibitory activity (IC50) of 0.2 nM, cellular level replication inhibition activity (LRAEC50) of 0.8 nM, and cytopathic effect inhibition activity (CPEEC50) of 0.1 nM. It demonstrates nanomolar range broad-spectrum antiviral efficacy against various influenza A strains, including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, and rPR8(H1N1)/H7N9, with EC50 values of 1.5, 3.6, 3.7, 13.8, 2.9, and 9.8 nM, respectively, and CC50 values all greater than 2 μM. PB2-IN-2 also shows excellent metabolic stability and pharmacokinetic properties, making it suitable for influenza research.

PB2-IN-2
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Product Introduction

Bioactivity
Description
PB2-IN-2 is an orally active PB2 inhibitor with RNP inhibitory activity (IC50) of 0.2 nM, cellular level replication inhibition activity (LRAEC50) of 0.8 nM, and cytopathic effect inhibition activity (CPEEC50) of 0.1 nM. It demonstrates nanomolar range broad-spectrum antiviral efficacy against various influenza A strains, including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, and rPR8(H1N1)/H7N9, with EC50 values of 1.5, 3.6, 3.7, 13.8, 2.9, and 9.8 nM, respectively, and CC50 values all greater than 2 μM. PB2-IN-2 also shows excellent metabolic stability and pharmacokinetic properties, making it suitable for influenza research.
In vitro
PB2-IN-2 (compound 3) exhibits low lipophilicity with a LogD value of 1.27. In A549 lung cells, PB2-IN-2 demonstrates excellent inhibitory activity against a range of wild-type and lab-adapted influenza A viruses, including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, and rPR8(H1N1)/H7N9 strains, with EC50 values of 1.5, 3.6, 3.7, 13.8, 2.9, and 9.8 nM, respectively. All IC50 values are greater than 2 μM, indicating a favorable safety profile.
In vivo
PB2-IN-2 (compound 3) exhibits a high free plasma fraction (1.2%) in mice. Administered orally at 0.05-1 mg/kg twice daily for 5 days, PB2-IN-2 demonstrates a low effective dose, a gradual dose-response relationship, and a wide therapeutic window in a mouse model of influenza A virus infection.
Chemical Properties
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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% Saline/PBS/ddH2O

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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