BMS-790052 2HCl


Catalog No. size PriceQuantity
M60423-2S 2 mg solid $89
M60423-10S 10mg solid $352

Description

Product Information
Chemical Name: 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
Purity: >98%
CAS#: 1009119-65-6
Solubility: DMSO: ≥ 56 mg/mL
Formula: C40H52CI2N8O6
Molecular Weight: 811.8
Storage: Powder -20oC 3 years 4oC 2 years In solvent -80oC 6 months -20oC 1 month

 

Biological Activity:

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 pM Target: HCV NS5A BMS-790052 has broad genotype coverage and exhibits picomolar

How to use:

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.

Reference:

[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.

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