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Boceprevir

MCE China：Boceprevir

Brand：MedChemExpress (MCE)

Cat. No.HY-10237

CAS：394730-60-0

Synonyms：EBP 520; SCH 503034

Purity：98.79%

Storage：Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Boceprevir (EBP 520) is a potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with a Ki of 14 nM in both enzyme assay and an EC90 of 350 nM in cell-based replicon assay. Boceprevir inhibits SARS-CoV-2 3CLpro activity.

In Vitro：In the HCV NS3 protease continuous assay, Boceprevir (SCH 503034) has a potency of 14 nM (Ki) average over a large number of runs. In the 72-h bicistronic subgenomic cell-based replicon assay in HuH-7 cells, the EC50 and EC90 values are determined to be 0.20 μM and 0.35 μM, respectively. Boceprevir is also found to be a very weak inhibitor of HNE (Ki=26 μM) representing a selectivity of 2200[1].

In Vivo：Boceprevir, an HCV Protease Inhibitor for the Treatment of Hepatitis C Virus Infection. The pharmacokinetic profile of Boceprevir is evaluated in several animal species. Following oral administration, Boceprevir is moderately absorbed in rats (10 mg/kg), dogs (3 mg/kg), and monkeys (3 mg/kg). Absorption is relatively rapid in dogs but slower in mice (10 mg/kg), rats, and monkeys, as evidenced by mean absorption times (MAT) ranging from 0.5 to 1.4 h. The AUC is good in dogs and rats, moderate in mouse, and low in monkeys. The absolute oral bioavailability is modest in mouse, rats, and dogs (26-34%) but low in monkeys (4%)[1]. Boceprevir (100 mg/kg, orally) inhibit HCV NS3/4A protease activity in triple-transgenic mice[2].

Animal Administration：Mice[2] Boceprevir is purchased from MedChem Express. To evaluate the effect of Boceprevir, triple-transgenic mice are induced with Doxycycline (Dox) for 10 days (n=5 per group). On the third day after Dox induction, when plasma Gluc activity reaches its peak, the mice are administered either Boceprevir (100 mg/kg) or DMSO via oral gavage twice daily for 7 days. During this period, blood is collected from the caudal vein daily to detect plasma Gluc activity.

IC50 & Target：Ki: 14 nM (HCV NS3 protease)[1] Cellular Effect Cell Line Type Value Description References

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References：

[1]. Njoroge FG, et al. Challenges in modern drug discovery: a case study of boceprevir, an HCV protease inhibitor for the treatment of hepatitis C virus infection. Acc Chem Res. 2008 Jan;41(1):50-9.  [Content Brief]

[2]. Yao M, et al. Conditional Inducible Triple-Transgenic Mouse Model for Rapid Real-Time Detection of HCV NS3/4A ProteaseActivity. PLoS One. 2016 Mar 4;11(3):e0150894.  [Content Brief]

[3]. Coilly A, et al. Practical management of boceprevir and immunosuppressive therapy in liver transplant recipients with hepatitis C virus recurrence. Antimicrob Agents Chemother. 2012 Nov;56(11):5728-34.  [Content Brief]

[4]. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56.  [Content Brief]

[5]. Burton MJ, et al. Telaprevir and boceprevir in african americans with genotype 1 chronic hepatitis C: implications for patients and providers. South Med J. 2012 Aug;105(8):431-6.  [Content Brief]

[6]. 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.  [Content Brief]