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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.
| Pack Size | Price | USA Stock | Global Stock | Quantity |
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| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| 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. |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
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.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
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 ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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