PB2-IN-2
PB2-IN-2 is an orally active PB2 inhibitor with RNA-dependent RNA Polymerase (RNP) IC50 = 0.2 nM, LRA (Ligand Receptor Assay) EC50 = 0.8 nM, Cytopathic Effect (CPE) EC50 = 0.1 nM. PB2-IN-2 exhibits broad-spectrum, nanomolar antiviral potency against a panel of influenza A strains (including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, rPR8(H1N1)/H7N9 with EC50 = 1.5, 3.6, 3.7, 13.8, 2.9 and 9.8 nM and all the CC50 values > 2 μM. PB2-IN-2 possesses an excellent pharmacokinetic profile and metabolic stability. PB2-IN-2 can be used for anti-influenza research.
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- Formule: C20H18F2N6O2
- Masse moléculaire:412.39
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
PB2-IN-2 (compound 3) exhibits low lipophilicity (LogD 1.27)[1].
PB2-IN-2 has superior inhibitory activity against a range of wild-type and laboratory-adapted influenza A viruses (including H1N1pdm09, Lyon/1337/2007/H1N1, Tex12-Like/H3N2, PR/8/34/H1N1, WSN/1933/H1N1, rPR8(H1N1)/H7N9 with EC50= 1.5, 3.6, 3.7, 13.8, 2.9 and 9.8 nM and all the IC50 values > 2 μM) and good safety margin in A549 lung cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CL | Vss | T1/2 (Elimination) | F |
|---|---|---|---|---|---|---|
| Mice[1] | 2.0 mg/kg | i.v. | 9.2 mL/min/kg | 1.6 L/kg | 1.6 h | 62.4 % |
PB2-IN-2 (0.05-1 mg/kg, p.o., twice daily for 5 days) has low efficacious dose, shallow efficacy cliff and wide therapeutic window in the mouse influenza A virus infection model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:A/Puerto Rico/8/34 (3 × 105 TCID50, i.n.) induced-male BALB/c mice[1]
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Dosage:0.05, 0.1, 0.3, and 1 mg/kg
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Administration:p.o., twice daily for 5 days
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Result:Provided 100% protection at a minimum dose of 0.3 mg/kg.
Achieved full protection maintaining in vitro EC50 coverage for more than 18 h.
Lost peak body weight at 10% by day 7 and recovered by day 14 at 0.3 mg/kg.
Chemical Information
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Masse moléculaire 412.39
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Formule C20H18F2N6O2
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SMILES
FC1=CN=C(N=C1N[C@H]2[C@@H]3CC[C@H]([C@@H]2C(O)=O)[C@@]4([H])[C@@]3(C4)[H])C5=NNC6=C5C=C(C=N6)F
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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