ASAP-0036543
ASAP-0036543 is an orally active virus NS2B-NS3 protease inhibitor. ASAP-0036543 exhibits activity againse Zika virus (ZIKV) and West Nile virus (WNV). ASAP-0036543 reduces ZIKV RNA load in plasma and spleen, and inhibits ZIKV and WNV replication in mammalian cells. ASAP-0036543 can be used for the research of zika virus infection, west nile virus infection.
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- Formule: C20H20F5N3O
- Masse moléculaire:413.38
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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
ASAP-0036543 potently inhibits ZIKV NS2B-NS3 protease (Ki = 0.0029 μM) and WNV NS2B-NS3 protease (Ki = 0.058 μM), but weakly inhibits DENV-2 NS2B-NS3 protease (Ki = 22 μM)[1].
ASAP-0036543 exhibits potent ZIKV antiviral activity in VeroE6 (EC50 = 0.47 μM), SH-SY5Y (EC50 = 0.45 μM), and JEG-3 (EC50 = 0.78 μM) cells, and WNV antiviral activity in VeroE6 cells (EC50 = 1.0 μM), with low cytotoxicity[1].
ASAP-0036543 binds to the active site of ZIKV NS2B-NS3 protease via specific aromatic and electrostatic interactions, with its configuration assigned as (S) via crystallography[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | F | Vdss | CLplasma |
|---|---|---|---|---|---|
| Mice[1] | 150 mg/kg | p.o. | 96 % | 7.9 L/kg | 87 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AG129 mice (129/Sv background, deficient in both IFN-α/β and IFN-γ receptors, 7-15 weeks old, 20-25 g) intraperitoneally inoculated with Zika virus[1]
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Dosage:150 mg/kg
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Administration:p.o.; twice daily; 3 days
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Result:Reduced viral RNA load significantly in both plasma and spleen.
Lowered viral RNA levels in many samples below the lower level of quantitation.
Chemical Information
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Masse moléculaire 413.38
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Formule C20H20F5N3O
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SMILES
CC1=CC([C@@H](C(NCC(F)F)=O)NC2=CC(CNC3)=C3C=C2)=CC(C(F)(F)F)=C1
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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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