2. Anti-infection
  3. Virus Protease
  4. 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.

For research use only. We do not sell to patients.

ASAP-0036543

ASAP-0036543 Chemical Structure

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ASAP-0036543 Related Antibodies

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Description

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[1].

In Vitro

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.

ASAP-0036543 Related Antibodies
Parmacokinetics
Species Dose Route F Vdss CLplasma
Mice[1] 150 mg/kg p.o. 96 % 7.9 L/kg 87 mL/min/kg
In Vivo

ASAP-0036543 (150 mg/kg; p.o.; twice daily; 3 days) produces significant viral RNA load reduction in plasma and spleen of ZIKV-infected AG129 mice[1].

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

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]
Dosage: 150 mg/kg
Administration: p.o.; twice daily; 3 days
Result: Reduced viral RNA load significantly in both plasma and spleen.
Lowered viral RNA levels in many samples below the lower level of quantitation.
Molecular Weight

413.38

Formula

C20H20F5N3O
SMILES

CC1=CC([C@@H](C(NCC(F)F)=O)NC2=CC(CNC3)=C3C=C2)=CC(C(F)(F)F)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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ASAP-0036543 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ASAP-0036543ASAP0036543ASAP 0036543Virus ProteasemiceWest Nile virusAG129 miceSH-SY5Y cellsVeroE6 cellsZika virusDENV-2 NS2B-NS3 proteasemammalian cellsNS2B-NS3 proteaseJEG-3 cellsInhibitorinhibitorinhibit

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