Description
As a highly selective inhibitor, BMS-790052 can inhibit HCV NS5A with EC50 of 9-50 pM.
Storage
2 years at -20 centigrade
Molecular Formula
C40H50N8O6
Chemical Name
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-, C,C-dimethyl ester
Solubility
DSMO 148 mg/mL Water
In vitro
BMS-790052 is the most potent hepatitis C virus (HCV) inhibitor. By targeting nonstructural protein 5A (NS5A), BMS-790052 is different from most HCV inhibitors. BMS-790052 is highly effective against genotype 1 replicons and also displays robust genotype 1 anti-HCV activity in the clinic. BMS-790052 can inhibit genotype 1 replicons with EC50 of less than 50 pM. BMS-790052 inhibits genotype 2a JFH1 replicon cells and cell culture infectious virus with EC50 of 46.8 pM and 16.1 pM. BMS-790052 blocks the cis-acting function of NS5A. Since BMS-790052 also impairs JFH1 NS5A hyperphosphorylation, it likely also blocks the trans-acting function.
In vivo
BMS-790052 shows potent antiviral effect in vivo. Although resistance emerged during monotherapy with BMS-790052, the substantial anti-HCV effect of this compound makes it an excellent candidate for effective combination therapy.
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