"目录号: HY-15236
Anti-infection-
PSI-6206 是 PSI-6130 的脱氨衍生物，PSI-6130 是一种有效的选择性 HCV NS5B 聚合酶抑制剂。PSI-6206 低效抑制HCV复制，EC90为 >100 μM。
HCV
相关产品
Asunaprevir-PSI-7977-Simeprevir-Daclatasvir-Paritaprevir-Telaprevir-Boceprevir-Ledipasvir-Ombitasvir-MK-5172-Elbasvir-ABT-333-Ribavirin-R-1479-Balapiravir-
生物活性
Description
PSI-6206 is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase. PSI-6206 low potently inhibitsHCV repliconwithEC90of >100 μM.
IC50& Target
EC90：>100 μM (HCV replicon)[1]
In Vitro
PSI-6206 (RO2433) is tested for anti-HCV activity in both a cell-based quantitative real-time RT-PCR assay and surrogate bovine viral diarrhea virus (BVDV) assays. PSI-6206 demonstrates no activity or cytoxicity in any assay[1]. The formation of the 5′-triphosphate (TP) of PSI-6130 (PSI-6130-TP) and RO2433 (RO2433-TP) increases with time and reached steady state levels at 48 h. RO2433-TP also inhibits RNA synthesis by the native HCV replicase isolated from HCV replicon cells and the recombinant HCV polymerase NS5B[2]. PSI-6206 (RO2433) is the deaminated derivative of PSI-6130, which is a potent and selective inhibitor of HCV NS5B polymerase[3].
References
[1].Clark JL, et al. Design, Synthesis, and Antiviral Activity of 2'-Deoxy-2'-fluoro-2'-C-methyl-cytidine, a Potent Inhibitor of Hepatitis C Virus Replication. J Med Chem. 2005 Aug 25;48(17):5504-8.
[2].Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29
[3].Wang P, et al. An efficient and diastereoselective synthesis of PSI-6130: a clinically efficacious inhibitor of HCV NS5B polymerase. J Org Chem. 2009 Sep 4;74(17):6819-24.