Beclabuvir

Names

[ Name ]:
Beclabuvir

[Synonym ]:
Beclabuvir
(1aR,12bS)-8-Cyclohexyl-N-(dimethylsulfamoyl)-11-methoxy-1a-{[(1R,5S)-3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl]carbonyl}-1,1a,2,12b-tetrahydrocyclopropa[d]indolo[2,1-a][2]benzazepine-5-carboxamide
Cycloprop[d]indolo[2,1-a][2]benzazepine-5-carboxamide, 8-cyclohexyl-N-[(dimethylamino)sulfonyl]-1,1a,2,12b-tetrahydro-11-methoxy-1a-[[(1R,5S)-3-methyl-3,8-diazabicyclo[3.2.1]oct-8-yl]carbonyl]-, (1aR,12bS)-
MYW1X5CO9S
BMS-791325

Biological Activity

[Description]:

Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.

[Related Catalog]:

Signaling Pathways >> Metabolic Enzyme/Protease >> HCV Protease

Signaling Pathways >> Anti-infection >> HCV

Research Areas >> Infection

[Target]

IC50: < 28 nM (NS5B protein)

[In Vitro]

Beclabuvir demonstrates additive or synergistic antiviral activity with pegIFN/RBV and in 2- or 3-drug combinations with a range of DAAs, such as HCV NS3 protease inhibitors, NS5A inhibitors' and/or nucleoside NS5B inhibitors[2].

[In Vivo]

The combination of beclabuvir with asunaprevir and daclatasvir achieves very high rates of viral eradication (about 90%) in patients infected with HCV genotype 1, which is the most common genotype worldwide[1].

[References]

[1]. Gentile I, et al. Beclabuvir for the treatment of hepatitis C. Expert Opin Investig Drugs. 2015;24(8):1111-21.

[2]. Tatum H, et al. A randomized, placebo-controlled study of the NS5B inhibitor beclabuvir with peginterferon/ribavirin for HCV genotype 1. J Viral Hepat. 2015 Aug;22(8):658-64.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.5±0.1 g/cm3

[ Molecular Formula ]:
C₃₆H₄₅N₅O₅S

[ Molecular Weight ]:
659.838

[ Exact Mass ]:
659.314148

[ LogP ]:
4.71

[ Index of Refraction ]:
1.722

[ Storage condition ]:
2-8℃

Related Compounds

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