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Boceprevir

Catalog No. T4988 CAS 394730-60-0

Synonyms: SCH 503034, EBP 520

Boceprevir (SCH 503034) is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

Boceprevir, CAS 394730-60-0

Pack Size	Availability	Price/USD
5 mg	In stock	$ 65.00
10 mg	In stock	$ 98.00
25 mg	In stock	$ 153.00
50 mg	In stock	$ 197.00
100 mg	In stock	$ 318.00
1 mL * 10 mM (in DMSO)	In stock	$ 74.00

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Purity: 99.16%

Purity: 97.33%

Purity: 95%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Boceprevir (SCH 503034) is a novel, potent, highly selective, orally bioavailable HCV NS3 protease inhibitor with Ki of 14 nM in both enzyme assay and EC90 of 350 nM in cell-based replicon assay.
Targets&IC50	HCV NS3 protease:14nM(Ki）
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.
In vivo	Boceprevir is a chemical compound designed as an HCV Protease Inhibitor for treating Hepatitis C Virus Infection. Its pharmacokinetic properties have been assessed across different animal species. Following oral administration, Boceprevir exhibits moderate absorption in rats (10 mg/kg), dogs (3 mg/kg), and monkeys (3 mg/kg), with absorption being relatively quicker in dogs compared to slower rates in mice (10 mg/kg), rats, and monkeys, as indicated by mean absorption times (MAT) of 0.5 to 1.4 hours. The compound demonstrates effective area under the curve (AUC) values in dogs and rats, moderate values in mice, and lower values in monkeys. Its absolute oral bioavailability ranges from modest (26-34%) in mice, rats, and dogs, to low (4%) in monkeys. Additionally, Boceprevir, at a dosage of 100 mg/kg orally, effectively inhibits HCV NS3/4A protease activity in triple-transgenic mice.

Synonyms	SCH 503034, EBP 520
Molecular Weight	519.68
Formula	C27H45N5O5
CAS No.	394730-60-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 91 mg/mL(175.1 mM)

References and Literature

1. 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):e20150894. 2. 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. 3. 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. 4. 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. 5. Berenguer M, et al. New developments in the management of hepatitis C virus infection: focus on boceprevir. Biologics. 2012;6:249-56. 6. Fical L. Vývoj UHPLC-MS/MS metody pro analýzu vybraných antivirotik v HILIC a RP módu[J]. 2020 7. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes[J]. Molecules. 2021, 26(8): 2123.

Citations

1. Bai Y, Ye F, Feng Y, et al. Structural basis for the inhibition of the SARS-CoV-2 main protease by the anti-HCV drug narlaprevir. Signal Transduction and Targeted Therapy. 2021, 6(1): 1-3 2. Fical L, Khalikova M, Kočová Vlčková H, et al. Determination of Antiviral Drugs and Their Metabolites Using Micro-Solid Phase Extraction and UHPLC-MS/MS in Reversed-Phase and Hydrophilic Interaction Chromatography Modes. Molecules. 2021, 26(8): 2123.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Inhibitor Library EMA Approved Drug Library Anti-COVID-19 Compound Library Anti-Infection Compound Library FDA-Approved Drug Library Drug-induced Liver Injury (DILI) Compound Library Pediatric Drug Library Bioactive Compounds Library Max Anti-Viral Compound Library

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Boceprevir 394730-60-0 Microbiology/Virology Proteases/Proteasome HCV Protease SARS-CoV HCV SCH 503034 SARS coronavirus Inhibitor Hepatitis C virus EBP520 EBP 520 SCH503034 inhibit SCH-503034 EBP-520 inhibitor

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.