HCV protease inhibitor
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.
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.
Target: NS3/4A protease [1] 14nM
Chemical name: 3-Azabicyclo[3.1.0]hexane-2-carboxamide, N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[(2S)-2-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-, (1R,2S,5S)-
Formula: C27H45N5O5
Molecular weight: 519.68
Purity: 99.6 %
Solubility: 100 mg/mL (DMSO), 100 mg/mL (ethanol)
Size: 5 mg
Storage: 3 years -20°C powder, 2 years -80°C in solvent
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].
References:
[1] Marchetti C, et al. J Cardiovasc Pharmacol. 2014, 63(4):316-322.