Boceprevir

Catalog No.S3733 Batch:S373302

Technical Data

Formula	C₂₇H₄₅N₅O₅
Molecular Weight	519.68	CAS No.	394730-60-0
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (192.42 mM)
		Ethanol	100 mg/mL (192.42 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

Boceprevir (EBP 520, SCH 503034) is an oral, direct acting hepatitis C virus (HCV) protease inhibitor with Ki value of 14 nM for NS3. It is used in combination with other antiviral agents in the treatment of chronic hepatitis C, genotype 1.

Targets

NS3/4A protease ^[1]

14 nM(Ki)

In vitro

Treatment with NLRP3 Inflammasome Inhibitor I significantly limits IL-1β release after LPS and ATP challenge. NLRP3 Inflammasome Inhibitor I is not a caspase-1 inhibitor^[1].

In vivo

The small molecule NLRP3 Inflammasome Inhibitor I, an intermediate substrate in the glyburide synthesis free of the cyclohexylurea moiety, inhibits the formation of the NLRP3 inflammasome in cardiomyocytes and limits the infarct size following myocardial ischemia/reperfusion in the mouse, without affecting glucose metabolism^[1].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines J774A.1 cells Concentrations 400 μM Incubation Time 30 mins Method J774A.1 cells, a murine macrophage cell line, are plated at 5×10⁴ cells/well in a 96 multiwell plate for 24 hours in RPMI medium supplemented with 10% of fetal bovine serum (FBS). The cells are primed with Escherichia coli 0111:B4 LPS(1 μg/ml) for 4 hours and then ATP (5 mM) for 30 minutes to induce the NLRP3 inflammasome formation. The supernatants are collected and levels of IL-1β are measured with a mouse IL-1β ELISA kit. To test the inhibitory effects of 16673-34-0 on NLRP3 inflammasome activation, cells are co-treated with 16673-34-0 (400μM) or Glyburide (400μM) at the time of ATP for 30 minutes, and IL-1β levels are used as read-out.
Animal Study:^{^[1]}	Animal Models CD1 mice Dosages 100 mg/kg Administration i.p.

Cell Assay:^{^[1]}

Cell lines
J774A.1 cells
Concentrations
400 μM
Incubation Time
30 mins
Method
J774A.1 cells, a murine macrophage cell line, are plated at 5×10⁴ cells/well in a 96 multiwell plate for 24 hours in RPMI medium supplemented with 10% of fetal bovine serum (FBS). The cells are primed with Escherichia coli 0111:B4 LPS(1 μg/ml) for 4 hours and then ATP (5 mM) for 30 minutes to induce the NLRP3 inflammasome formation. The supernatants are collected and levels of IL-1β are measured with a mouse IL-1β ELISA kit. To test the inhibitory effects of 16673-34-0 on NLRP3 inflammasome activation, cells are co-treated with 16673-34-0 (400μM) or Glyburide (400μM) at the time of ATP for 30 minutes, and IL-1β levels are used as read-out.

Animal Study:^{^[1]}

Animal Models
CD1 mice
Dosages
100 mg/kg
Administration
i.p.

References

[1] Marchetti C, et al. J Cardiovasc Pharmacol. 2014, 63(4):316-322.

Selleck's Boceprevir has been cited by 15 publications

Design, synthesis, and biological evaluation of first-in-class indomethacin-based PROTACs degrading SARS-CoV-2 main protease and with broad-spectrum antiviral activity [ Eur J Med Chem, 2024, 268:116202]	PubMed: 38394929
Development of a Biosafety Level 1 Cellular Assay for Identifying Small-Molecule Antivirals Targeting the Main Protease of SARS-CoV-2: Evaluation of Cellular Activity of GC376, Boceprevir, Carmofur, Ebselen, and Selenoneine [ Int J Mol Sci, 2024, 25(11)5767]	PubMed: 38891954
SARS-CoV-2 Mpro inhibitor identification using a cellular gain-of-signal assay for high-throughput screening [ SLAS Discov, 2024, S2472-5552(24)00043-1]	PubMed: 39173830
Discovery of novel SARS-CoV-2 inhibitors targeting the main protease Mpro by virtual screenings and hit optimization [ Antiviral Res, 2022, 204:105350]	PubMed: 35688349
From Repurposing to Redesign: Optimization of Boceprevir to Highly Potent Inhibitors of the SARS-CoV-2 Main Protease [ Molecules, 2022, 27(13)4292]	PubMed: 35807537
Integrative multiomics and in silico analysis revealed the role of ARHGEF1 and its screened antagonist in mild and severe COVID-19 patients [ J Cell Biochem, 2022, 10.1002/jcb.30213]	PubMed: 35037717
BRET-Based Self-Cleaving Biosensors for SARS-CoV-2 3CLpro Inhibitor Discovery [ Microbiol Spectr, 2022, 10(4):e0255921]	PubMed: 35758897
Hepatitis C virus drugs that inhibit SARS-CoV-2 papain-like protease synergize with remdesivir to suppress viral replication in cell culture [ Cell Rep, 2021, 35(7):109133]	PubMed: 33984267
Ugonin J Acts as a SARS-CoV-2 3C-like Protease Inhibitor and Exhibits Anti-inflammatory Properties [ Front Pharmacol, 2021, 12:720018]	PubMed: 34512347
Pre-Steady-State Kinetics of the SARS-CoV-2 Main Protease as a Powerful Tool for Antiviral Drug Discovery [ Front Pharmacol, 2021, 12:773198]	PubMed: 34938188

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SHIPPING AND STORAGE
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