R-1479
Based on 3 publication(s) in Google Scholar
R-1479 (4'-Azidocytidine), a nucleoside analogue, is a specific inhibitor of RNA-dependent RNA polymerase (RdRp) of HCV. R-1479 inhibits HCV replication in the HCV subgenomic replicon system (IC50=1.28 μM). R-1479 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- Pureté: 99.46%
- CAS No.: 478182-28-4
- Formule: C9H12N6O5
- Masse moléculaire:284.23
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Publications Citing Use of MedChemExpress (MCE) R-1479
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Activité biologique
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RNA Polymerase |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | CC50 |
>80 μM
Compound: 1b
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Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay
Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay
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[PMID: 25667954] |
| HeLa | EC50 |
0.67 μM
Compound: 1b
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Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay
Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay
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[PMID: 25667954] |
| Huh-5-2 | CC50 |
>33 μM
Compound: 4'-Azidocytidine
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Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay
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[PMID: 18625766] |
| Huh-5-2 | EC50 |
1.4 μM
Compound: 4'-Azidocytidine
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Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay
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[PMID: 18625766] |
| Huh-7 | CC50 |
>100 μM
Compound: 4'-azidocytidine
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Cytotoxicity against human HuH7 cells
Cytotoxicity against human HuH7 cells
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[PMID: 20579888] |
| Huh-7 | CC50 |
>100 μM
Compound: R-1479
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Cytotoxicity against human HuH7 cells
Cytotoxicity against human HuH7 cells
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[PMID: 18285474] |
| Huh-7 | CC50 |
>200 μM
Compound: 4'azidocytidine
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Cytotoxicity against human HuH7 cells after3 days by MTT assay
Cytotoxicity against human HuH7 cells after3 days by MTT assay
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[PMID: 20337460] |
| Huh-7 | CC50 |
>98.4 μM
Compound: 3, R-1479
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Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay
Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay
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[PMID: 21033671] |
| Huh-7 | EC50 |
1.28 μM
Compound: R-1479
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Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay
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[PMID: 18285474] |
| Huh-7 | EC50 |
1.4 μM
Compound: 4'azidocytidine
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Antiviral activity against HCV 1b infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay
Antiviral activity against HCV 1b infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay
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[PMID: 20337460] |
| Huh-7 | EC50 |
1.4 μM
Compound: 4'-Azidocytidine
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Antiviral activity against HCV subtype 1a in Huh7 cells assessed as reduction of viral RNA replication
Antiviral activity against HCV subtype 1a in Huh7 cells assessed as reduction of viral RNA replication
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[PMID: 18801660] |
| Huh-7 | EC50 |
4.3 μM
Compound: 3, R-1479
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Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay
Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay
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[PMID: 21033671] |
| MT4 | CC50 |
>98.4 μM
Compound: 3, R-1479
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Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay
Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay
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[PMID: 21033671] |
R-1479 (R1479) inhibits HCV RNA replication with a mean IC50 value of 1.28 μM when measured as 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 most potent and non-cytotoxic derivative is R-1479 with an IC50 of 1.28 μM in the HCV replicon system. 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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 478182-28-4
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Appearance Solid
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Masse moléculaire 284.23
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Formule C9H12N6O5
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Color White to off-white
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SMILES
OC[C@]1(N=[N+]=[N-])[C@@H](O)[C@@H](O)[C@H](N2C(N=C(N)C=C2)=O)O1
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Synonyms
4'-Azidocytidine
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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J Infect Dis
2016 Sep 1;214(5):707-11. PMID: 27234417 -
Antiviral Res
Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro. [Abstract]2020 Jun;178:104786. PMID: 32251767 -
Antiviral Res
Antiviral candidates against the hepatitis E virus (HEV) and their combinations inhibit HEV growth in in vitro. [Abstract]2019 Oct;170:104570. PMID: 31362004
Solvant et solubilité
DMSO : 100 mg/mL (351.83 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.80 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (282 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
[3]. Nguyen NM, et al. A randomized, double-blind placebo controlled trial of balapiravir, a polymerase inhibitor, in adult dengue patients. J Infect Dis. 2013 May 1;207(9):1442-1450. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.5183 mL | 17.5914 mL | 35.1828 mL | 87.9569 mL |
| 5 mM | 0.7037 mL | 3.5183 mL | 7.0366 mL | 17.5914 mL | |
| 10 mM | 0.3518 mL | 1.7591 mL | 3.5183 mL | 8.7957 mL | |
| 15 mM | 0.2346 mL | 1.1728 mL | 2.3455 mL | 5.8638 mL | |
| 20 mM | 0.1759 mL | 0.8796 mL | 1.7591 mL | 4.3978 mL | |
| 25 mM | 0.1407 mL | 0.7037 mL | 1.4073 mL | 3.5183 mL | |
| 30 mM | 0.1173 mL | 0.5864 mL | 1.1728 mL | 2.9319 mL | |
| 40 mM | 0.0880 mL | 0.4398 mL | 0.8796 mL | 2.1989 mL | |
| 50 mM | 0.0704 mL | 0.3518 mL | 0.7037 mL | 1.7591 mL | |
| 60 mM | 0.0586 mL | 0.2932 mL | 0.5864 mL | 1.4659 mL | |
| 80 mM | 0.0440 mL | 0.2199 mL | 0.4398 mL | 1.0995 mL | |
| 100 mM | 0.0352 mL | 0.1759 mL | 0.3518 mL | 0.8796 mL |
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