R-1479 is an HCV replication inhibitor in the HCV subgenomic replicon system (IC50: 1.28 μM).

R-1479 inhibits HCV RNA replication with a mean IC50 value of 1.28 μM when measured as the dose-dependent reduction of Renillaluciferase activity after a 72 h incubation of proliferating replicon cells. R-1479 shows no effect on cell viability or proliferation of HCV replicon or Huh-7 cells at concentrations up to 2 mM [1]. The triphosphate of R-1479 is prepared and shown to be an inhibitor of RNA synthesis mediated by NS5B (IC50: 320 nM), the RNA polymerase encoded by HCV. R-1479 displays good activity in the replicon assay with no measurable cytotoxic or cytostatic effect [2].

The membrane-associated, native HCV replicase complex is isolated from 2209-23 HCV replicon cells and a derived cell line carrying HCV replicon RNA with an S282T mutation in the NS5B coding sequence. The in vitro replicase assay contain 10 μL of cytoplasmic membrane fraction, 50 mM HEPES (pH 7.5), 10 mM KCl, 10 mM dithiothreitol, 5 mM MgCl2, 20 μg/mL actinomycin D, 1 mM ATP, 1 mM GTP, 1 mM UTP, 30 μCi of [α-33P]CTP (3000 Ci/mmol, 10 mCi/mL), 1 unit/μL SUPERase?In, 10 mM creatine phosphate, and 200 μg/mL creatine phosphokinase in a final volume of 25 μL [1].

478182-28-4

C9H12N6O5

284.23

4'-叠氮基胞嘧啶核苷;4'-Azidocytidine

DMSO:48 mg/mL (168.87 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years