R-1479 (Synonyms: 4'-Azidocytidine)

Name: R-1479
Brand: MedChemExpress
SKU: HY-10444
Rating: 5.0 (3 reviews)

Cat. No.: HY-10444 Purity: 99.60%: FAQs
Data Sheet SDS COA Handling Instructions

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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.

For research use only. We do not sell to patients.

R-1479 Chemical Structure

CAS No. : 478182-28-4

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 462	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 462	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 600	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1800	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 2520	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE R-1479

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Biological Activity
Protocol
Purity & Documentation
References
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Description

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)^[1]^[2]^[3]. 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.

IC₅₀ & Target

IC50: 1.28 μM (HCV replication)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	CC₅₀	> 80 μM Compound: 1b	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	[PMID: 25667954]
HeLa	EC₅₀	0.67 μM Compound: 1b	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	[PMID: 25667954]
Huh-5-2	CC₅₀	> 33 μM Compound: 4'-Azidocytidine	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	1.4 μM Compound: 4'-Azidocytidine	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	[PMID: 18625766]
Huh-7	CC₅₀	> 200 μM Compound: 4'azidocytidine	Cytotoxicity against human HuH7 cells after3 days by MTT assay Cytotoxicity against human HuH7 cells after3 days by MTT assay	[PMID: 20337460]
Huh-7	CC₅₀	> 98.4 μM Compound: 3, R-1479	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	[PMID: 21033671]
Huh-7	EC₅₀	1.28 μM Compound: R-1479	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	[PMID: 18285474]
Huh-7	EC₅₀	1.4 μM Compound: 4'azidocytidine	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	[PMID: 20337460]
Huh-7	EC₅₀	4.3 μM Compound: 3, R-1479	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	[PMID: 21033671]
MT4	CC₅₀	> 98.4 μM Compound: 3, R-1479	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	[PMID: 21033671]

In Vitro

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.

Molecular Weight

284.23

Formula

C₉H₁₂N₆O₅

CAS No.

478182-28-4

Appearance

Solid

Color

White to off-white

SMILES

OC[C@]1(N=[N+]=[N-])[C@@H](O)[C@@H](O)[C@H](N2C(N=C(N)C=C2)=O)O1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.5183 mL	17.5914 mL	35.1828 mL
5 mM	0.7037 mL	3.5183 mL	7.0366 mL
10 mM	0.3518 mL	1.7591 mL	3.5183 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.80 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.60%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (254 KB) RP-HPLC (232 KB)

Handling Instructions (2659 KB)

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. [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]

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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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. [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

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

R-1479 Related Classifications

Infection

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R-1479478182-28-44'-AzidocytidineR1479R 1479HCVDNA/RNA SynthesisHepatitis C virusnucleosideRdRpreplicationBalapiravirR1626Inhibitorinhibitorinhibit

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R-1479 (Synonyms: 4'-Azidocytidine)

Customer Review

R-1479 Related Antibodies

3 Publications Citing Use of MCE R-1479

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Customer Review

R-1479 Related Antibodies

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Complete Stock Solution Preparation Table

R-1479 Related Classifications

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