Bioactivity | Dasabuvir (ABT-333) is a nonnucleoside hepatitis C virus (HCV) polymerase inhibitor. Dasabuvir inhibits RNA-dependent RNA polymerase encoded by the HCV NS5B gene. Dasabuvir inhibits genotype 1a (strain H77) and 1b (strain Con1) replicons, with EC50 values of 7.7 and 1.8 nM, respectively[1]. | ||||||||||||
Target | IC50: 2.2 ± 0.3 nM (HCV genotype 1b N), 2.8 ± 0.2 nM (HCV genotype 1a H77), 3.1 ± 0.21 nM (HCV genotype 1b BK), 0.7 ± 1.4 nM (HCV genotype 1b Con1) | ||||||||||||
Invitro | Dasabuvir (ABT-333) is at least 7,000-fold selective for the inhibition of HCV genotype 1 polymerases over human/mammalian polymerases[1]. Dasabuvir (ABT-333) inhibits the polymerase enzymatic activity of genotype 1 laboratory strain enzymes (H77, BK, N, and Con1 strains), as well as enzymes produced from polymerase genes from HCV genotype 1-infected subjects, with IC50s between 2.2 and 10.7 nM[1]. Dasabuvir (ABT-333) inhibits replication of HCV subgenomic replicons in cell culture assays, with EC50 values of 7.7 and 1.8 nM against genotype 1a (H77) and 1b (Con1), respectively. In the presence of 40% human plasma, there is a 12- to 13-fold decrease in inhibitory potency, yielding EC50s of 99 and 21 nM for HCV genotype 1a (H77) and 1b (Con1) replicons, respectively[1]. | ||||||||||||
Name | Dasabuvir | ||||||||||||
CAS | 1132935-63-7 | ||||||||||||
Formula | C26H27N3O5S | ||||||||||||
Molar Mass | 493.57 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Kati W, et al. In vitro activity and resistance profile of dasabuvir, a nonnucleoside hepatitis C virus polymerase inhibitor. Antimicrob Agents Chemother. 2015 Mar;59(3):1505-11. |