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• 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

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *