Art. -Nr.: HY-19314

Azvudine

(Synonyms: RO-0622; FNC)

6 Cited Publications

Kundenbewertung

Based on 6 publication(s) in Google Scholar

Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC₅₀s ranging from 0.03 to 6.92 nM) and HIV-2 (EC₅₀s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains. Azvudine 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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Reinheit: 99.38%
CAS. Nr.: 1011529-10-4
Formel: C₉H₁₁FN₆O₄
Molecular Weight:286.22

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Azvudine Chemical Structure

CAS. Nr.: 1011529-10-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (6)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Azvudine (RO-0622) is a potent nucleoside reverse transcriptase inhibitor (NRTI), with antiviral activity on HIV, HBV and HCV. Azvudine exerts highly potent inhibition on HIV-1 (EC₅₀s ranging from 0.03 to 6.92 nM) and HIV-2 (EC₅₀s ranging from 0.018 to 0.025 nM). Azvudine inhibits NRTI-resistant viral strains^[1]. Azvudine 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^[1]

HIV-1

0.03-6.92 nM (EC₅₀)

HIV-2

0.018-0.02 nM (EC₅₀)

Alle HIV Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	CC₅₀	≥25 μM Compound: 1; FNC	Cytotoxicity against HEK293 cells assessed as cell viability by MTT assay Cytotoxicity against HEK293 cells assessed as cell viability by MTT assay	[PMID: 32678592]
MT2	EC₅₀	0.3 nM Compound: 10	Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus 1 NL4-3 infected in human MT2 cells assessed as inhibition of viral replication after 48 hrs by luciferase activity reporter gene assay Antiviral activity against vesicular stomatitis virus G-pseudotyped Human immunodeficiency virus 1 NL4-3 infected in human MT2 cells assessed as inhibition of viral replication after 48 hrs by luciferase activity reporter gene assay	[PMID: 21745701]
MT2	CC₅₀	>10 μM Compound: 1	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 23570720]
MT4	CC₅₀	0.09957 μM Compound: AFC	Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay Cytotoxicity against human MT4 cells treated for 3 days measured by Celltiter-glo luminescent assay	[PMID: 33214842]

In Vitro

Azvudine (RO-0622) displays strong inhibition on wild-type HIV-1_IIIB and HIV-1_RF with an EC₅₀ ranging from 30 to 110 pM. The EC₅₀ values of Azvudine against HIV-1_KM018, HIV-1_TC-1 and HIV-1_{WAN T69N} are 6.92, 0.34 and 0.45 nM, respectively. Azvudine is sensitive to NRTIs-resistant strain HIV-1_74V, PIs-resistant strains HIV-1_{L10R/M46I/L63P/V82T/I84V} and HIV-1_{RF V82F/184V}, and FIs-resistant strain pNL4-3 _{gp41 (36G) V38A/N42T}. The EC₅₀ values of Azvudine against these resistant strains are 0.11, 0.14, 0.37 and 0.36 nM respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 1011529-10-4
Appearance Solid
Molecular Weight 286.22
Formel C₉H₁₁FN₆O₄
Color White to off-white
SMILES

O[C@@H]1[C@](CO)(N=[N+]=[N-])O[C@@H](N2C(N=C(N)C=C2)=O)[C@H]1F
Synonyms

RO-0622; FNC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (6)

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Signal Transduct Target Ther

Real-world effectiveness and safety of oral azvudine versus nirmatrelvir‒ritonavir (Paxlovid) in hospitalized patients with COVID-19: a multicenter, retrospective, cohort study. [Abstract]

2025 Jan 17;10(1):30. PMID: 39819859
Acta Pharm Sin B

Selectively T cell phosphorylation activation of azvudine in the thymus tissue with immune protection effect. [Abstract]

2024 Jul;14(7):3140-3154. PMID: 39027259
Biomed Pharmacother

Azvudine exhibits potent differentiation-inducing effect by targeting the TERT/p21 axis in acute myeloid leukemia. [Abstract]

2025 May 27:188:118215. PMID: 40435838
Mikrochim Acta

Strain-promoted azide-alkyne cycloaddition-based fluorometric detection of azvudine using DBCO-functionalized carbon dots. [Abstract]

2025 Dec 8;193(1):10. PMID: 41359210
Antiviral Res

Metformin inhibits EV-A71 and CVA16 infections by regulating TRIB3-SCARB2 axis and activating AMPK. [Abstract]

2025 Jan 16:235:106081. PMID: 39826812
NAR Mol Med

Mechanism and spectrum of inhibition of viral polymerases by 2'-deoxy-2'-β-fluoro-4'-azidocytidine or azvudine. [Abstract]

2025 Aug 11;2(3):ugaf029. PMID: 40900943

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (349.38 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (174.69 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.4938 mL

17.4691 mL

34.9382 mL

5 mM

0.6988 mL

3.4938 mL

6.9876 mL

10 mM

0.3494 mL

1.7469 mL

3.4938 mL

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (8.73 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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (8.73 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (8.73 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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

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) .

Reinheit & Dokumentation

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Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang RR, et al. Azvudine, a novel nucleoside reverse transcriptase inhibitor showed good drug combination features and better inhibition on drug-resistant strains than lamivudine in vitro. PLoS One. 2014 Aug 21;9(8):e105617. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	3.4938 mL	17.4691 mL	34.9382 mL	87.3454 mL
	5 mM	0.6988 mL	3.4938 mL	6.9876 mL	17.4691 mL
	10 mM	0.3494 mL	1.7469 mL	3.4938 mL	8.7345 mL
	15 mM	0.2329 mL	1.1646 mL	2.3292 mL	5.8230 mL
	20 mM	0.1747 mL	0.8735 mL	1.7469 mL	4.3673 mL
	25 mM	0.1398 mL	0.6988 mL	1.3975 mL	3.4938 mL
	30 mM	0.1165 mL	0.5823 mL	1.1646 mL	2.9115 mL
	40 mM	0.0873 mL	0.4367 mL	0.8735 mL	2.1836 mL
	50 mM	0.0699 mL	0.3494 mL	0.6988 mL	1.7469 mL
	60 mM	0.0582 mL	0.2912 mL	0.5823 mL	1.4558 mL
	80 mM	0.0437 mL	0.2184 mL	0.4367 mL	1.0918 mL
	100 mM	0.0349 mL	0.1747 mL	0.3494 mL	0.8735 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Azvudine

6 Cited Publications

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Azvudine

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Publications Citing Use of MedChemExpress (MCE) Azvudine

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Azvudine

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

Glycoside Compound Library

Nucleotide Compound Library

NMPA-Approved Drug Library

FDA Approved & Pharmacopeial Drug Library

Anti-Hepatitis C Virus Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Azide Compound Library

Publications Citing Use of MedChemExpress (MCE) Azvudine

Alle HIV Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (6)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Azvudine Related Classifications

HY-19314 Related Classifications