Boceprevir

For research use only.

Catalog No.S3733

Boceprevir Chemical Structure

CAS No. 394730-60-0

Boceprevir 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.

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Biological Activity

Description Boceprevir 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

Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: CD1 mice
  • Dosages: 100 mg/kg
  • Administration: i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL (192.42 mM)
Water Insoluble
Ethanol '100 mg/mL

* 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.

Chemical Information

Molecular Weight 519.68
Formula

C27H45N5O5

CAS No. 394730-60-0
Storage powder
in solvent
Synonyms N/A
Smiles CC1(C2C1C(N(C2)C(=O)C(C(C)(C)C)NC(=O)NC(C)(C)C)C(=O)NC(CC3CCC3)C(=O)C(=O)N)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01909401 Completed Drug: boceprevir Liver Transplantation Indiana University|Merck Sharp & Dohme Corp. June 2013 Early Phase 1
NCT01821625 Terminated Drug: Eltrombopag Thrombocytopenia|Hepatitis C University of Texas Southwestern Medical Center|GlaxoSmithKline April 2013 Phase 2|Phase 3
NCT01499498 Completed Drug: Sildenafil and Boceprevir Hepatitis C Imperial College London December 2012 Phase 1
NCT01663922 Completed Drug: Boceprevir|Drug: St John''s Wort Hepatitis C St Stephens Aids Trust|University of Liverpool|University of Turin Italy August 2012 Phase 1
NCT01657552 Completed Drug: Eltrombopag|Drug: Boceprevir|Drug: Telaprevir Thrombocytopaenia GlaxoSmithKline August 1 2012 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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HCV Protease Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID