1. Anti-infection Cell Cycle/DNA Damage
  2. HCV DNA/RNA Synthesis
  3. R-1479

R-1479  (Synonyms: 4'-Azidocytidine)

Cat. No.: HY-10444 Purity: 99.60%
COA Handling Instructions

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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

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

R-1479 Chemical Structure

R-1479 Chemical Structure

CAS No. : 478182-28-4

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 462 In-stock
Solution
10 mM * 1 mL in DMSO USD 462 In-stock
Solid
5 mg USD 420 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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. Strain-promoted alkyne-azide cycloaddition (SPAAC) can also occur with molecules containing DBCO or BCN groups.

IC50 & Target

IC50: 1.28 μM (HCV replication)[1]

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.
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
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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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%

References
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

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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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.

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R-1479
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