| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
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| Targets |
Nucleoside analogue; Influenza virus
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| ln Vitro |
Triazavirin's effectiveness against the tick-borne encephalitis virus is measured in a sensitive cell culture. Triazavirin is effective in inhibiting the reproduction of the tick-borne encephalitis virus (strain Sofiin) by accumulation in the SKEV cell culture at a concentration of 128 mcg/mL[2].
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| ln Vivo |
Triazavirin's effectiveness as a treatment against experimental Forest-Spring encephalitis in albino mice is investigated. The findings indicate that triazavirin, at high doses (200–400 mg/kg), protects the infected animals in a moderate way. Test groups' animal lifespans increased significantly (from 4.1 to 4.8 days) and there was a statistically significant drop in the amount of virus accumulation in the target organ[3].
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| Cell Assay |
The efficacy of Triazavirin against the tick-borne encephalitis virus was estimated in the sensitive cell culture vs. the active drug Ribavirin. In a concentration of 128 mcg/ml Triazavirin was shown active in inhibition of the tick-borne encephalitis virus reproduction (strain Sofiin) by accumulation in the SKEV cell culture[2].
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| Animal Protocol |
The comparative study of the therapeutic efficacy of Triazavirin against experimental Forest-Spring encephalitis on albino mice vs. the active drug Ribavirin® showed that in high doses (200-400 mg/kg) Triazavirin moderately protected the infected animals. A significant increase of the animal lifespan in the test groups (from 4.1 to 4.8 days) and a statistically (p ≤ 0.05) valid decrease of the virus accumulation in the target organ (the brain) were observed[3].
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
In rabbits, intragastric triazavirin reaches a Cmax of 1.1±0.1mg/L, with a Tmax of 0.40±0.16h, and an AUC of 3.10±0.8mg\*h/L. In rabbits, intravenous triazavirin has an AUC of 1.2±0.3mg\*h/L. In humans, triazavirin reaches a Cmax of 4.8µg/mL, with a Tmax of 1-1.5h, and an AUC of 12.8µgµg/h\*mL. Data regarding the route of elimination of triazavirin is not readily available. In rabbits, intragastric triazavirin has a volume of distribution of 83.5±19.2L/kg while intravenous triazavirin has a volume of distribution of 1.2±0.3L/kg. In rabbits, intragastric triazavirin has a clearance of 37.0±11.2L/h\*kg while intravenous triazavirin has a clearance of 14.0±3.7L/h\*kg. The clearance of triazavirin is 246mL/min. Metabolism / Metabolites Data regarding the metabolism of triazavirin is not readily available. Biological Half-Life In rabbits, intragastric triazavirin has a half life of 1.1±0.1h while intravenous triazavirin has a half life of 0.50±0.09h. The half life of triazavirin is 1-1.5h. |
| Toxicity/Toxicokinetics |
Protein Binding
Data regarding the protein binding of triazavirin is not readily available. |
| References |
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| Additional Infomation |
Triazavirin is a guanine nucleotide analog antiviral originally developed in Russia that has shown efficacy against influenza A and B, including the H5N1 strain. It appears that Triazavirin has shown promise in reducing influenza disease severity and associated complications. Given the similarities between SARS-CoV-2 and H5N1, health officials are investigating Triazavirin as an option to combat SARS-CoV-2, the coronavirus responsible for COVID-19.
Riamilovir is a synthetic guanine derivative, with potential broad-spectrum antiviral activity. Upon administration, riamilovir inhibits viral RNA synthesis, thereby preventing viral transcription and replication. Riamilovir may also bind to severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) and human angiotensin-converting enzyme 2 (ACE2). This may block the entry of SARS-CoV-2 into human host cells. Drug Indication Triazavirin was developed in Russia as a potential treatment of Influenza A and B infections. Mechanism of Action Triazavirin is a guanosine nucleotide analog that inhibits RNA synthesis. |
| Molecular Formula |
C5H4N6O3S
|
|---|---|
| Molecular Weight |
232.22042
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| Exact Mass |
228.007
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| Elemental Analysis |
C, 26.32; H, 1.77; N, 36.83; O, 21.03; S, 14.05
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| CAS # |
123606-06-4
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| Related CAS # |
116061-59-7 (sodium);123606-06-4 (free);928659-17-0 (sodium hydrate);
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| PubChem CID |
3113817
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
2.0
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
15
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| Complexity |
435
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CSN1CCN2N(C(N=C2N1)=O)[N+]([O-])=O
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| InChi Key |
IDVQGNMSSHPZSJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H4N6O3S/c1-15-5-6-4-8-7-2(11(13)14)3(12)10(4)9-5/h1H3,(H,6,8,9)
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| Chemical Name |
7-(methylsulfanyl)-3-nitro[1,2,4]triazolo[5,1-c][1,2,4]triazin-
4(1H)-one
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| Synonyms |
Riamilovir Triazavirin TZV
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3063 mL | 21.5313 mL | 43.0626 mL | |
| 5 mM | 0.8613 mL | 4.3063 mL | 8.6125 mL | |
| 10 mM | 0.4306 mL | 2.1531 mL | 4.3063 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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