Riamilovir
(Synonyms: Triazavirin) 目录号 : GC25863Riamilovir (Triazavirin) is a broad-spectrum antiviral drug candidate, which can be used for potential application against the Coronavirus 2019-nCoV.
Cas No.:123606-06-4
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Riamilovir (Triazavirin) is a broad-spectrum antiviral drug candidate, which can be used for potential application against the Coronavirus 2019-nCoV.
[1] Shahab S, et al. Curr Mol Med. 2021;21(8):645-654.
| Cas No. | 123606-06-4 | SDF | Download SDF |
| 别名 | Triazavirin | ||
| 分子式 | C5H4N6O3S | 分子量 | 228.19 |
| 溶解度 | DMSO: 46 mg/mL (201.59 mM);Water: 46 mg/mL (201.59 mM);Ethanol: Insoluble | 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 | 4.3823 mL | 21.9116 mL | 43.8231 mL |
| 5 mM | 0.8765 mL | 4.3823 mL | 8.7646 mL |
| 10 mM | 0.4382 mL | 2.1912 mL | 4.3823 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。
Antiplatelet Activity of Riamilovir under Conditions of Lipopolysaccharide Intoxication
Bull Exp Biol Med 2022 May;173(1):41-45.PMID:35616790DOI:10.1007/s10517-022-05489-0.
We studied the effect of antiviral agent Riamilovir on ADP-induced platelet aggregation in the absence and presence of LPS. Unlike acetylsalicylic acid (reference drug), Riamilovir did not exhibit antiplatelet effect in vitro. However, it markedly suppressed platelet reactivity in LPS-treated blood samples and was 2.2-fold superior to acetylsalicylic acid in terms of IC50 value. In in vivo experiments, Riamilovir under conditions of hypercytokinemia blocked platelet aggregation in rats by 64%.
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.
[Evaluation of the effectiveness of Riamilovir in the complex therapy of patients with COVID-19]
Ter Arkh 2021 Mar 15;93(3):290-294.PMID:36286698DOI:10.26442/00403660.2021.03.200719.
Aim: In this study we evaluated the effects of Riamilovir on SARS-CoV-2 viral shedding and on admission duration in patients with moderate COVID-19. Materials and methods: We have used data from 69 health records of patients with moderate severe PCR confirmed SARS-CoV-2 infection. Control group included 34 patients treated with off-label Riamilovir 1250 mg per day for 5 days (250 mg 5 times a day), comparison groups 35 patients, who received ribavirin and umifenovir 800 mg a day for 5 days. The antiviral therapy was administered within 72 hours from the onset of the disease. The primary endpoints were elimination of virus in oropharyngeal and nasopharyngeal swabs on 7 day of admission and discharge from the hospital by 14 day. Results: Patients assigned to Riamilovir had significantly shorter time to clinical improvement as well as increased PCR negative rate by day 7. Conclusion: Yearly administration of Riamilovir as opposed to the umifenovir and ribavirin in therapy of moderate SARS-CoV-2 infection was associated with significant shorter time to clinical improvement by 14 day of hospitalization. PCR negative rate by 7 days of hospitalization is significantly more likely in Riamilovir group.
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.
Prospects of using the nucleoside analogue Riamilovir in patients with SARS-CoV-2 infection
Ter Arkh 2022 Nov 22;94(10):1171-1176.PMID:36468991DOI:10.26442/00403660.2022.10.201920.
Aim: To evaluate clinical efficacy of nucleoside analogues in therapy of moderate COVID-19 in in-patients. Materials and methods: Retrospective processing of 108 completed clinical cases with moderate novel coronavirus disease was carried out for the period 2020-2021. The duration of the disease at the time of admission did not exceed three days. Experimental group consisted of 53 patients who, in addition to standard therapy, were prescribed "off-label" Riamilovir at a daily dosage of 1250 mg for 5 days by the decision of the medical commission. Comparison group included 55 patients who received a combination of umifenovir and ribavirin as antiviral therapy for 5 days. The duration of the main clinical manifestations of the disease, the indicators of clinical and biochemical blood tests, results of the SARS-CoV-2 virus RNA study using the nucleic acid amplification method (NAAT diagnostics). Results: Significantly faster achievement of clinical improvement in the group of patients treated with Riamilovir was shown, as well as faster sanitation from SARS-CoV-2 virus based on the results of etiological testing. Conclusion: The use of Riamilovir for the treatment of patients with moderate novel coronavirus infection (COVID-19) resulted in a significant reduction of general infectious syndromes and respiratory symptoms. Patients from the experimental group significantly faster achieved clinical recovery and sanitation from the pathogen according to the results of NAAT diagnostics.