Elbasvir

Modify Date: 2024-01-04 12:28:33

Elbasvir Structure
Elbasvir structure
Common Name Elbasvir
CAS Number 1370468-36-2 Molecular Weight 882.017
Density 1.4±0.1 g/cm3 Boiling Point N/A
Molecular Formula C49H55N9O7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Elbasvir


Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.

 Names

Name elbasvir
Synonym More Synonyms

 Elbasvir Biological Activity

Description Elbasvir (MK-8742) is a hepatitis C virus nonstructural protein 5A (HCV NS5A) inhibitor with EC50s of 4, 3 and 3 nM against genotype 1a, 1b, and 2a, respectively.
Related Catalog
Target

EC50: 4 nM (HCV 1a), 3 nM (HCV 1b), 3 nM (HCV 2a)[1]

In Vitro Elbasvir shows potent activity against genotype 1a and 1b replicons, with EC90 of 0.006 nM for both the wild-type 1a_H77 and 1b_con1 replicons. Elbasvir inhibits genotype 3 replicons with EC90 of 0.12 nM. Elbasvir (0.06 nM, 0.6 nM, and 6 nM) demonstrates dose-dependent suppression of resistant genotype 1a replicons, illustrated by the reductions in colony counts at higher doses[1]. Elbasvir is highly potent against HCV replicons bearing NS5A sequences from GT1a, -1b, -2a(31L), -3a, -4a, -5a, and -6, with EC50s in the low-picomolar range[2].
References

[1]. Liu R, et al. Susceptibilities of genotype 1a, 1b, and 3 hepatitis C virus variants to the NS5A inhibitor Elbasvir. Antimicrob Agents Chemother. 2015 Nov;59(11):6922-6929.

[2]. Lahser FC, et al. The Combination of Grazoprevir, a Hepatitis C Virus (HCV) NS3/4A Protease Inhibitor, and Elbasvir, an HCV NS5A Inhibitor, Demonstrates a High Genetic Barrier to Resistance in HCV Genotype 1a Replicons. Antimicrob Agents Chemother. 2016 A

 Chemical & Physical Properties

Density 1.4±0.1 g/cm3
Molecular Formula C49H55N9O7
Molecular Weight 882.017
Exact Mass 881.422424
PSA 188.80000
LogP 6.98
Index of Refraction 1.701
Storage condition -20℃

 Synonyms

dimethyl N,N'-([(6S)-6-phenylindolo[1,2-c][1,3]benzoxazine-3,10-diyl]bis{1H-imidazole-5,2-diyl-(2S)-pyrrolidine-2,1-diyl[(2S)-3-methyl-1-oxobutane-1,2-diyl]})dicarbamate
Elbasvir(MK8742)
Carbamic acid, N,N'-[[(6S)-6-phenyl-6H-indolo[1,2-c][1,3]benzoxazine-3,10-diyl]bis[1H-imidazole-4,2-diyl(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]bis-, dimethyl ester
Methyl {(2S)-1-[(2S)-2-{4-[(6S)-3-{2-[(2S)-1-{(2S)-2-[(methoxycarbonyl)amino]-3-methylbutanoyl}-2-pyrrolidinyl]-1H-imidazol-4-yl}-6-phenylindolo[1,2-c][1,3]benzoxazin-10-yl]-1H-imidazol-2-yl}-1-pyrrolidinyl]-3-methyl-1-oxo-2-butanyl}carbamate
MK-8742
UNII-632L571YDK
Elbasvir
((2S,2'S)-((2S,2'S)-2,2'-(5,5'-((S)-6-phenyl-6H-benzo[5,6][1,3]oxazino[3,4-a]indole-3,10-diyl)bis(1H-imidazole-5,2-diyl))bis(pyrrolidine-2,1-diyl))bis(3-methyl-1-oxobutane-2,1-diyl))dicarbamate
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