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R-1479

Catalog No. TQ0162   CAS 478182-28-4
Synonyms: 4'-Azidocytidine

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

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R-1479, CAS 478182-28-4
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Purity 98%
Biological Description
Chemical Properties
Storage & Solubility Information
Description R-1479 is an HCV replication inhibitor in the HCV subgenomic replicon system (IC50: 1.28 μM).
In vitro 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].
Kinase Assay 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].
Synonyms 4'-Azidocytidine
Molecular Weight 284.23
Formula C9H12N6O5
CAS No. 478182-28-4

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 48 mg/mL (168.87 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Klumpp K, et al. The novel nucleoside analog R1479 (4'-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture. J Biol Chem. 2006 Feb 17;281(7):3793-9. 2. Smith DB, et al. Design, synthesis, and antiviral properties of 4'-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479. Bioorg Med Chem Lett. 2007 May 1;17(9):2570-6.

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