产品描述: | Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC90 value of 40 nM. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease. Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM |
靶点: |
Ki: 6 nM (NS3 protease) EC90: 40 nM (NS3 protease) Ki: 7 nM (ketoamide) EC90: 40 nM (replicon RNA) |
体内研究: |
Pharmacokinetic AnalysisNarlaprevir (SCH 900518) exhibits middle oral bioavailability (rat 46%, dog 29%, monkey 46 %) following oral administration (rat 10 mg/kg, dog 3 mg/kg, monkey 3 mg/kg ). Narlaprevir (SCH 900518) exhibits moderate half-lives (rat 4.8 and dog 2 h) following intravenous administration (rat 4 and dog 1 mg/kg). Animal Model: rats, dogs, monkeys Dosage: Rat PO/IV 10/4 mg/kg; dog PO/IV 3/1 mg/kg; monkey PO 3 mg/kg Administration: Intravenous (i.v.) or oral gavage Result: T1/2s of 4.8 and 2 h for rats and dogs, respectively. |
参考文献: |
1. Ashok Arasappan, et al. Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor. ACS Med Chem Lett. 2010 Feb 15;1(2):64-9. 2. X Tong, et al. Preclinical characterization of the antiviral activity of SCH 900518 (narlaprevir), a novel mechanism-based inhibitor of hepatitis C virus NS3 protease. Antimicrob Agents Chemother. 2010 Jun;54(6):2365-70. 3. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.413 ml |
7.063 ml |
14.125 ml |
5 mM |
0.283 ml |
1.413 ml |
2.825 ml |
10 mM |
0.141 ml |
0.706 ml |
1.413 ml |
50 mM |
0.028 ml |
0.141 ml |
0.283 ml |
|
注意: |
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