Azvudine
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.38%
- CAS 番号: 1011529-10-4
- 分子式: C9H11FN6O4
- 分子量:286.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 Azvudine
More- Signal Transduct Target Ther. 2025 Jan 17;10(1):30. [Abstract]
- Acta Pharm Sin B. 2024 Jul;14(7):3140-3154. [Abstract]
- Biomed Pharmacother. 2025 May 27:188:118215. [Abstract]
- Mikrochim Acta. 2025 Dec 8;193(1):10. [Abstract]
- Antiviral Res. 2025 Jan 16:235:106081. [Abstract]
- NAR Mol Med. 2025 Aug 11;2(3):ugaf029. [Abstract]
生物活性
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HIV-1 0.03-6.92 nM (EC50) |
HIV-2 0.018-0.02 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | CC50 |
≥25 μM
Compound: 1; FNC
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Cytotoxicity against HEK293 cells assessed as cell viability by MTT assay
Cytotoxicity against HEK293 cells assessed as cell viability by MTT assay
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[PMID: 32678592] |
| MT2 | EC50 |
0.3 nM
Compound: 10
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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
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[PMID: 21745701] |
| MT2 | CC50 |
>10 μM
Compound: 1
|
Cytotoxicity against human MT2 cells by MTT assay
Cytotoxicity against human MT2 cells by MTT assay
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[PMID: 23570720] |
| MT4 | CC50 |
0.09957 μM
Compound: AFC
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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] |
Azvudine (RO-0622) displays strong inhibition on wild-type HIV-1IIIB and HIV-1RF with an EC50 ranging from 30 to 110 pM. The EC50 values of Azvudine against HIV-1KM018, HIV-1TC-1 and HIV-1WAN T69N are 6.92, 0.34 and 0.45 nM, respectively. Azvudine is sensitive to NRTIs-resistant strain HIV-174V, PIs-resistant strains HIV-1L10R/M46I/L63P/V82T/I84V and HIV-1RF 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.
化学情報
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CAS 番号 1011529-10-4
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性状 Solid
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分子量 286.22
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分子式 C9H11FN6O4
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Color White to off-white
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SMILES
O[C@@H]1[C@](CO)(N=[N+]=[N-])O[C@@H](N2C(N=C(N)C=C2)=O)[C@H]1F
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別名
RO-0622; FNC
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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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Journal Impact Factor
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Most Recent
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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
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (8.73 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.
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 (8.73 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.
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.
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.
純度とドキュメンテーション
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データシート (277 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
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, 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.