| Bioactivity | 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[1]. Narlaprevir also inhibits the HCV nonstructural protein 3 serine protease[2]. Narlaprevir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 2.3 μM[3]. | ||||||||||||
| Target | Ki: 6 nM (NS3 protease) EC90: 40 nM (NS3 protease) Ki: 7 nM (ketoamide) EC90: 40 nM (replicon RNA) | ||||||||||||
| Invitro | Narlaprevir (SCH 900518) potently inhibits ketoamide with a Ki value of 7 nM[2].Narlaprevir (SCH 900518) potently inhibits replicon RNA with an EC90 value of 40 nM[2]. | ||||||||||||
| In Vivo | Pharmacokinetic Analysis Narlaprevir (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 )[1].Narlaprevir (SCH 900518) exhibits moderate half-lives (rat 4.8 and dog 2 h) following intravenous administration (rat 4 and dog 1 mg/kg)[1]. Animal Model: | ||||||||||||
| Name | Narlaprevir | ||||||||||||
| CAS | 865466-24-6 | ||||||||||||
| Formula | C36H61N5O7S | ||||||||||||
| Molar Mass | 707.96 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
Narlaprevir
CAS: 865466-24-6 F: C36H61N5O7S W: 707.96
Narlaprevir (SCH 900518) is a selective and orally bioavailable NS3 protease inhibitor with a Ki value of 6 nM and an EC
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