PSI-6130

CEI-1487

PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase

PSI-6130 is a selective and effective inhibitor of hepatitis C virus (HCV) RNA replication with an EC50 of 0.46 μM. It is a potent nucleoside analog which incorporates into nascent RNA by the HCV NS5B polymerase and leads to chain termination. NS5B is a viral protein discovered in hepatitis c virus. It plays a significant role in the replication of HCV, which uses HCV'S viral positive RNA strand as the template and catalyzes the polymerization of rNTP during RNA replication. PSI-6130 is a nucleotide analog and it can be activated by converting into nucleotide triphosphate form, which can be an alternative substrate in the synthesis of viral RNA. As a result PSI-6130 reduces the efficacy of further elongation of HCV RNA by NS5B. Studies reported PSI-6130 HCV replication inhibition effects. PSI-6130 activity of HCV replication was determined in Huh7 cells with a subgenomic genotype 1b Con1 strain. And the mean IC50 was 0.6 μM. And another study showed that PSI-6130 inhibited HCV GT-1b (Con1 strain) and GT-1a (H77 strain) subgenomic RNA replication, with similar levels of potency, whose mean EC 50 values are 0.51 and 0.30 μM, respectively. PSI-6130 could be transformed into two active metabolites, RO2433 and PSI-6026 respectively, in human primary hepatocytes by enzymes. Moreover, PSI-6130 showed little or no cytotoxicity against different cells, including human peripheral blood mononuclear and human bone marrow progenitor cells. Assessments of PSI-6130's activity against other viruses in the Flaviviridae family were conducted, which illustrated that PSI-6130 was not active against viruses including BVDV, WNV, YFV, HBV, and HIV. The results also showed that PSI-6130 is a selective HCV inhibitor.

817204-33-4

259.23

0.98

Store at -20°C

R 1656; PSI 6130; PSI6130; R-1656

Hepatitis C Virus Nucleoside

C10H14FN3O4

4-amino-1-[(2R,3R,4R,5R)-3-fluoro-4-hydroxy-5-(hydroxymethyl)-3-methyloxolan-2-yl]pyrimidin-2-one

Soluble in DMSO

Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request