Triazavirin
(Synonyms: Riamilovir, TZV) 目录号 : GC61348
An antiviral agent
Cas No.:928659-17-0
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Triazavirin is an antiviral agent.1 In vivo, triazavirin (1 mg/kg) inhibits lung viral accumulation in a mouse model of H5N1 influenza A infection. Triazavirin (20 mg/kg) inhibits platelet aggregation in a rat model of LPS-induced hypercytokinemia.2 Formulations containing triazavirin have been used in the treatment of influenza.
1.Loginova, S.I., Borisevich, S.V., Maksimov, V.A., et al.Therapeutic efficacy of Triazavirin, a novel Russian chemotherapeutic, against influenza virus A (H5N1)Antibiot. Khimioter.56(1-2)10-12(2011) 2.Spasov, A.A., Kucheryavenko, A.F., Sirotenko, V.S., et al.Antiplatelet activity of riamilovir under conditions of lipopolysaccharide intoxicationBull. Exp. Biol. Med.173(1)41-45(2022)
| Cas No. | 928659-17-0 | SDF | |
| 别名 | Riamilovir, TZV | ||
| Canonical SMILES | O=C1N([N-]C(SC)=N2)C2=NN=C1[N+]([O-])=O.[H]O[H].[H]O[H].[Na+] | ||
| 分子式 | C5H7N6NaO5S | 分子量 | 286.2 |
| 溶解度 | DMSO: 125 mg/mL (436.76 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.4941 mL | 17.4703 mL | 34.9406 mL |
| 5 mM | 0.6988 mL | 3.4941 mL | 6.9881 mL |
| 10 mM | 0.3494 mL | 1.747 mL | 3.4941 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Triazavirin-A Novel Effective Antiviral Drug
Int J Mol Sci 2022 Nov 22;23(23):14537.PMID:36498864DOI:10.3390/ijms232314537.
This review outlines the data of numerous studies relating to the broad-spectrum antiviral drug Triazavirin that was launched on the Russian pharmaceutical market in 2014 as an anti-influenza drug (the international non-patented name is Riamilovir). The range of antiviral activity of Triazavirin has been significantly expanded during recent years; in particular, it has been shown that Triazavirin exhibits activity against tick-borne encephalitis, Rift Valley fever, West Nile fever, and other infections of viral etiology. This drug has been approved for treatment of influenza and acute respiratory infections by the Russian Ministry of Health on the basis of comprehensive clinical trials involving over 450 patients. Triazavirin was found to be a highly effective and well-tolerated drug, allowing its over-the-counter sale. The recently published data on the use of Triazavirin in clinical practice for the treatment of patients with COVID-19 are discussed, with special attention paid to potential biological targets for this drug.
The efficacy of Triazavirin (riamilovir)-based treatment for coronavirus disease 2019 (COVID-19) in clinical trials and preliminary practical experiences
Ceska Slov Farm 2022 Fall;71(6):239-244.PMID:36513517doi
Coronavirus disease 2019 (COVID-19) caused by Severe Acute Respiratory Syndrome Coronavirus 2 (SARS-CoV-2) has plagued the human population as 2019 turned into 2020, when first cases were confirmed to be infected with the pathogen in Wuhan City, the largest mega-city and capital of Hubei Province in Central China. Since this time, many pharmacotherapeutic modalities were suggested and used to treat the patients suffering from COVID-19. Triazavirin (TZV; riamilovir) is a synthetic non-toxic broad-spectrum antiviral drug belonging into an azolotriazine class. Several hypotheses and suggestions based on the knowledge about morphology, structure of virion, genome, replication cycle and functions of particular proteins within SARS-CoV-2 as well as in silico analyzes were published aiming to employ TZV for the treatment of COVID-19. Results and conclusions from a well-known randomized controlled trial registered under the Registration No. ChiCTR2000030001, which was carried out in China in 2020, indicated not only the anti-SARS-CoV-2 efficacy of given aza analogue of guanine but also some limitations of these outcomes in the context of their general interpretability and applicability. Thus, a primary aim of this review article was to provide more complex view on pharmacotherapeutic interventions based on TZV against COVID-19/SARS-CoV-2. The focus was on relevant results and conclusions from clinical trials as well as practical experiences with given antiviral agent considering not only real benefits of chosen therapeutic strategies but also several obstacles connected with them.
Triazavirin - Potential Inhibitor for 2019-nCoV Coronavirus M Protease: A DFT Study
Curr Mol Med 2021;21(8):645-654.PMID:32436829DOI:10.2174/1566524020666200521075848.
Background: Triazavirin (2-methylsulfanyl-6-nitro[1,2,4]triazolo[5,1-c][1,2,4] triazin-7(4H)-one, TZV) is an antiviral drug synthesized. TZV is being investigated for potential application against the Coronavirus 2019-nCoV. Aims and objectives: In order to find candidate drugs for 2019-nCoV, we have carried out a computational study to screen for effective available drug Triazavirin (C5H4N6O3S) which may work as inhibitor for the Mpro of 2019-nCoV. Methods: In the present work, first time the molecular structure of title molecule has been investigated using Density Functional Theory (DFT/B3LYP/MidiX) in gas phase. Results: The molecular HOMO-LUMO, excitation energies and oscillator strengths of investigated compound have also been calculated and presented. The interaction of TZV compound with the Coronavirus was performed by molecular docking studies. Conclusion: Therefore, TZV can be used for potential application against the Coronavirus 2019-nCoV.
Synthetic approaches to 1,2,4-triazolo[5,1- c][1,2,4]triazin-7-ones as basic heterocyclic structures of the antiviral drug Riamilovir ("Triazavirin®") active against SARS-CoV-2 (COVID-19)
Org Biomol Chem 2022 Mar 2;20(9):1828-1837.PMID:35137762DOI:10.1039/d1ob02125g.
Fragments of 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-one are found in many compounds with various types of biological activities, including the antiviral drug Riamilovir (Triazavirin®), which shows activity against SARS-CoV-2 (COVID-19). Therefore, the development of convenient methods for the synthesis of new derivatives of 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-one is always in demand. This review systematizes the information on the most common synthetic methods for constructing the 1,2,4-triazolo[5,1-c][1,2,4]triazin-7-one heterocyclic system.
Aerosol Inhalation Delivery of Triazavirin in Mice: Outlooks for Advanced Therapy Against Novel Viral Infections
J Pharm Sci 2021 Mar;110(3):1316-1322.PMID:33249050DOI:10.1016/j.xphs.2020.11.016.
Under pandemic-caused emergency, evaluation of the potential of existing antiviral drugs for the treatment of COVID-19 is relevant. Triazavirin, an antiviral drug developed in Russia for per-oral administration, is involved in clinical trials against SARS-CoV-2 coronavirus. This virus has affinity to epithelial cells in respiratory tract, so drug delivery directly in lungs may enhance therapeutic effect and reduce side effects for stomach, liver, kidneys. We elaborated ultrasonic method of Triazavirin aerosol generation and investigated the inhalation delivery of this drug in mice. Mean particle size and number concentration of aerosol used in inhalation experiments are 560 nm and 4 × 105 cm-3, respectively. Aerosol mass concentration is 1.6 × 10-4 mg/cm3. Inhalation for 20 min in a nose-only chamber resulted in 2 mg/kg body delivered dose and 2.6 μg/mL Triazavirin concentration in blood plasma. Elimination rate constant determined in aerosol administration experiments was ke = 0.077 min-1, which agrees with the value measured after intravenous delivery, but per-oral administration resulted in considerably lower apparent elimination rate constant of pseudo-first order, probably due to non-linear dependence of absorption rate on Triazavirin concentration in gastrointestinal tract. The bioavailability of Triazavirin aerosol is found to be 85%, which is about four times higher than for per-oral administration.