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Boceprevir HCV Protease inhibitor

Cat.No.S3733

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.
Boceprevir HCV Protease inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 519.68

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Quality Control

Batch: Purity: >97%
97

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (192.42 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 100 mg/mL

Water : Insoluble

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In vivo
Batch:

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Working concentration: mg/ml;

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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight 519.68 Formula

C27H45N5O5

 Storage (From the date of receipt)
CAS No. 394730-60-0 Download SDF Storage of Stock Solutions

Synonyms EBP 520, SCH 503034 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

Mechanism of Action

Targets/IC50/Ki
NS3/4A protease
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.
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.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01909401 Completed
Liver Transplantation
Indiana University|Merck Sharp & Dohme LLC
 June 2013 Early Phase 1
NCT01821625 Terminated
Thrombocytopenia|Hepatitis C
University of Texas Southwestern Medical Center|GlaxoSmithKline
 April 2013 Phase 2|Phase 3
NCT01499498 Completed
Hepatitis C
Imperial College London
 December 2012 Phase 1
NCT01663922 Completed
Hepatitis C
St Stephens Aids Trust|University of Liverpool|University of Turin Italy
 August 2012 Phase 1
NCT01657552 Completed
Thrombocytopaenia
GlaxoSmithKline
 August 1 2012 Phase 1

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