Daclatasvir dihydrochloride

Names

[ Name ]:
Daclatasvir dihydrochloride

[Synonym ]:
Daclatasvir dihydrochloride (USAN)
daclatasvir hydrochloride
Carbamic acid, N,N'-[[1,1'-biphenyl]-4,4'-diylbis[1H-imidazole-5,2-diyl(2S)-2,1-pyrrolidinediyl[(1S)-1-(1-methylethyl)-2-oxo-2,1-ethanediyl]]]bis-, dimethyl ester, hydrochloride (1:2)
BMS-790052 dihydrochloride
UNII-50ZO25C11D
methyl N-[(2S)-1-[(2S)-2-[5-[4-[4-[2-[(2S)-1-[(2S)-2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]phenyl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamate,dihydrochloride
MFCD18251440
Daklinza
CS-0270
Daclatasvir dihydrochloride
Daclatasvir hydrochloride (JAN)
Daclatasvir HCL
Methyl [(2S)-1-{(2S)-2-[4-(4'-{2-[(2S)-1-{(2S)-2-[(methoxycarbonyl)amino]-3-methylbutanoyl}-2-pyrrolidinyl]-1H-imidazol-4-yl}-4-biphenylyl)-1H-imidazol-2-yl]-1-pyrrolidinyl}-3-methyl-1-oxo-2-butanyl]carbamate dihydrochloride
BMS 790052
Daclatasvir (dihydrochloride)

Biological Activity

[Description]:

BMS-790052 is a highly selective inhibitor of HCV NS5A with EC50 of 9-50 pM, for a broad range of HCV replicon genotypes and the JFH-1 genotype 2a infectious virus in cell culture.IC50 Value: 9-50 pMTarget: HCV NS5ABMS-790052 has broad genotype coverage and exhibits picomolar in vitro potency against genotypes 1a (EC50 50pm) and 1b (EC50 9pm). BMS-790052 produces a robust decline in HCV RNA (-3.6 logs after 48 hours from a single 100 mg) dosefollowing a single dose in patients chronically infected with HCV genotype 1.

[Related Catalog]:

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

Signaling Pathways >> Anti-infection >> HCV

Research Areas >> Infection

[References]

[1]. Suzuki F, Sezaki H, Akuta N, Suzuki Y, Seko Y, Kawamura Y, Hosaka T, Kobayashi M, Saito S, Arase Y, Ikeda K, Kobayashi M, Mineta R, Watahiki S, Miyakawa Y, Kumada H.Prevalence of hepatitis C virus variants resistant to NS3 protease inhibitors or the NS5A inhibitor (BMS-790052) in hepatitis patients with genotype 1b.J Clin Virol. 2012 Aug;54(4):352-4. Epub 2012 Jun 1.

[2]. Jiang H, Zeng J, Kandoussi H, Liu Y, Wang X, Bifano M, Cojocaru L, Ryan J, Arnold ME.A sensitive and accurate liquid chromatography-tandem mass spectrometry method for quantitative determination of the novel hepatitis C NS5A inhibitor BMS-790052 (daclastasvir) in human plasma and urine.J Chromatogr A. 2012 Jul 6;1245:117-21. Epub 2012 May 14.

[3]. Sun JH, O'Boyle Ii DR, Zhang Y, Wang C, Nower P, Valera L, Roberts S, Nettles RE, Fridell RA, Gao M.Impact of a baseline polymorphism on the emergence of resistance to the hepatitis C virus nonstructural protein 5A replication complex inhibitor, BMS-790052.Hepatology. 2012 Jun;55(6):1692-9.

[4]. Wang C, Jia L, Huang H, Qiu D, Valera L, Huang X, Sun JH, Nower PT, O'Boyle DR 2nd, Gao M, Fridell RA.In vitro activity of BMS-790052 on hepatitis C virus genotype 4 NS5A.Antimicrob Agents Chemother. 2012 Mar;56(3):1588-90. Epub 2011 Dec 27.

[5]. Fridell RA et al. Resistance analysis of the hepatitis C virus NS5A inhibitor BMS-790052 in an in vitro replicon system. Antimicrob Agents Chemother. 2010 Sep;54(9):3641-50.

[Related Small Molecules]