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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C20H20F5N3O
- 分子量:413.38
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
-
生物活性
-
化学情報
- 純度とドキュメンテーション
- 参考文献
-
Help & FAQs
生物活性
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.
-
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.
化学情報
-
分子量 413.38
-
分子式 C20H20F5N3O
-
SMILES
CC1=CC([C@@H](C(NCC(F)F)=O)NC2=CC(CNC3)=C3C=C2)=CC(C(F)(F)F)=C1
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Powered by Bioz