R-1479

HCV replication inhibitor CAS# 478182-28-4

R-1479

Catalog No. BCC1878----Order now to get a substantial discount!

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Chemical structure

R-1479

3D structure

Chemical Properties of R-1479

Cas No. 478182-28-4 SDF Download SDF
PubChem ID 457388 Appearance Powder
Formula C9H12N6O5 M.Wt 284.23
Type of Compound N/A Storage Desiccate at -20°C
Synonyms 4'-Azidocytidine
Solubility DMSO : ≥ 50 mg/mL (175.91 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 4-amino-1-[(2R,3R,4S,5R)-5-azido-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one
SMILES C1=CN(C(=O)N=C1N)C2C(C(C(O2)(CO)N=[N+]=[N-])O)O
Standard InChIKey ODLGMSQBFONGNG-JVZYCSMKSA-N
Standard InChI InChI=1S/C9H12N6O5/c10-4-1-2-15(8(19)12-4)7-5(17)6(18)9(3-16,20-7)13-14-11/h1-2,5-7,16-18H,3H2,(H2,10,12,19)/t5-,6+,7-,9-/m1/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of R-1479

DescriptionR1479 (4'-azidocytidine) is a potent and highly specific inhibitor of HCV replication with an IC50 value of 1.28 μM in the HCV subgenomic replicon system.
TargetsHCV    
IC501.28 μM     

Protocol

Kinase Assay [1]
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 a 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. Inhibition by nucleotide analogs is determined[1].

Cell Assay [1]
The effect of R-1479 on the incorporation of tritiated thymidine into cellular DNA is measured using the [3H]thymidine incorporation scintillation proximity assay system. MTT and WST-1 assay systems are used to measure cell viability. The ATP bioluminescence assay kit HSII is used to measure intracellular ATP levels[1].

References:
[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.

R-1479 Dilution Calculator

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R-1479 Molarity Calculator

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Preparing Stock Solutions of R-1479

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.5183 mL 17.5914 mL 35.1828 mL 70.3655 mL 87.9569 mL
5 mM 0.7037 mL 3.5183 mL 7.0366 mL 14.0731 mL 17.5914 mL
10 mM 0.3518 mL 1.7591 mL 3.5183 mL 7.0366 mL 8.7957 mL
50 mM 0.0704 mL 0.3518 mL 0.7037 mL 1.4073 mL 1.7591 mL
100 mM 0.0352 mL 0.1759 mL 0.3518 mL 0.7037 mL 0.8796 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on R-1479

R1479 is a specific inhibitor of HCV replication in cell culture with IC50 value of 1.28 μM [1].

Hepatitis C virus (HCV) is an enveloped (+)-single stranded RNA virus, and the viral RNA is replicated in host cell via RNA-dependent RNA polymerase of HIV, which is the cause of hepatitis C and some cancer lymphomas [2].

R1479 is a potent and specific inhibitor of HCV NS5B RNA polymerase to inhibit HCV replication in the HCV subgenomic replicon system. In proliferating replicon cells of 2209-23 cell line, 72 h incubation of R1479 showed inhibition of HCV RNA replication (IC 50 = 1.28 μM), which had the similar potency with 2_-C-methylcytidine (IC 50 = 1.13 μM). R1479 had no influence on cell proliferation and viability of Huh-7 cells at concentration up to 2 mM, which suggested the inhibition by R1479 was a direct antiviral mechanism [2]. Furthermore, prolong incubation of R1479 for HCV replicon cells led to a continuous reduction of HCV RNA to an undetectable level within 15 days of incubation [2].Finally, R1479 showed no cytotoxicity in replicon cells [1].

References:
[1] Smith D B, 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, 17(9): 2570-6.
[2] 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, 281(7): 3793-9.

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References on R-1479

R-1626, a specific oral NS5B polymerase inhibitor of hepatitis C virus.[Pubmed:18828074]

IDrugs. 2008 Oct;11(10):738-49.

Roche Holding AG is developing R-1626, an oral nucleoside inhibitor of HCV RNA polymerase. R-1626 has been demonstrated to be well absorbed and rapidly converted to the active component R-1479. The compound has demonstrated a strong capacity to inhibit HCV replication in vitro and in vivo, without the rapid development of viral resistance. After 4 weeks of treatment with R-1626 in combination with PEG-IFN plus ribavirin in treatment-naive patients with genotype 1 HCV infection, HCV RNA could no longer be detected in approximately 74% of patients, compared with 5% of patients treated with PEG-IFN plus ribavirin alone, indicating the high potency of R-1626 to induce HCV RNA viral load reductions. R-1626 was generally well tolerated, although severe side effects of neutropenia were observed at high doses. A phase IIb clinical trial was ongoing at the time of publication to test the efficacy of R-1626 in combination with a standard or lower dose of PEG-IFN and ribavirin in HCV genotype 1-infected patients. Given its potent antiviral effect with an apparent high genetic barrier, R-1626 represents an important advancement in improving the outcome of patients with chronic HCV infection.

Description

R-1479 is a specific inhibitor of HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM).

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