| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Description: Taribavirin (ICN-3142, Ribamidine, AVS-206, KD-024, Viramidine), a prodrug of Ribavirin, is an inosine monophosphate dehydrogenase inhibitor with antiviral activity against a wide range of RNA/DNA viruses, especially the hepatitis C virus and influenza virus. Taribavirin is a Ribavirin prodrug designed to be enriched within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia. Taribavirin has better liver-targeting capability than ribavirin, and has a shorter life in the body due to less penetration and storage in red blood cells.
| ln Vitro |
Taribavirin (0-2 μM; 24 hours) has been shown to strongly promote MCF-7 cell death, with an IC50 of 0.756 μM in MCF-7 cells [1].
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|---|---|
| Cell Assay |
Cell Viability Assay[1]
Cell Types: MCF-7 Cell Tested Concentrations: 0 μM, 0.1 μM, 1 μM, 2 μM Incubation Duration: 24 hrs (hours) Experimental Results: MCF-7 cell growth diminished. |
| References | |
| Additional Infomation |
Taribavirin is a nucleobase-containing molecular entity.
Taribavirin is an orally available prodrug of ribavirin, a synthetic nucleoside analog of ribofuranose with activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin is converted into ribavirin, which is incorporated into viral nucleic acid, thereby inhibiting viral RNA synthesis, inducing viral genome mutations, and inhibiting normal viral replication. Drug Indication Investigated for use/treatment in hepatitis (viral, C). Mechanism of Action The prodrug taribavirin (1-b-D-ribofuranosyl-1H-1, 2, 4-triazole-3-carboxamidine) is a synthetic nucleoside (guanosine) analog under development for the treatment of patients with chronic hepatitis C. Taribavirin is metabolized by the liver and converted into its active metabolite, ribavirin. This pathway reduces exposure to red blood cells (RBCs) and increases exposure to the liver, the site of HCV replication. [Valeant Website] Ribavirin is readily phosphorylated intracellularly by adenosine kinase to ribavirin mono-, di-, and triphosphate metabolites. Ribavirin triphosphate (RTP) is a potent competitive inhibitor of inosine monophosphate (IMP) dehydrogenase, viral RNA polymerase and messenger RNA (mRNA) guanylyltransferase (viral). Guanylyltranserase inhibition stops the capping of mRNA. These diverse effects result in a marked reduction of intracellular guanosine triphosphate (GTP) pools and inhibition of viral RNA and protein synthesis. Ribavirin is also incorporated into the viral genome causing lethal mutagenesis and a subsequent decrease in specific viral infectivity. |
| Molecular Formula |
C8H13N5O4
|
|---|---|
| Molecular Weight |
243.21992
|
| Exact Mass |
243.097
|
| CAS # |
119567-79-2
|
| Related CAS # |
Taribavirin hydrochloride;40372-00-7
|
| PubChem CID |
451448
|
| Appearance |
Typically exists as solid at room temperature
|
| Density |
2.08g/cm3
|
| Boiling Point |
595.5ºC at 760mmHg
|
| Flash Point |
313.9ºC
|
| Vapour Pressure |
5.01E-15mmHg at 25°C
|
| Index of Refraction |
1.851
|
| LogP |
-1.8
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
17
|
| Complexity |
304
|
| Defined Atom Stereocenter Count |
4
|
| SMILES |
C([C@@H]1[C@H]([C@H]([C@H](N2C=NC(=N2)C(=N)N)O1)O)O)O
|
| InChi Key |
NHKZSTHOYNWEEZ-AFCXAGJDSA-N
|
| InChi Code |
InChI=1S/C8H13N5O4/c9-6(10)7-11-2-13(12-7)8-5(16)4(15)3(1-14)17-8/h2-5,8,14-16H,1H2,(H3,9,10)/t3-,4-,5-,8-/m1/s1
|
| Chemical Name |
1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,2,4-triazole-3-carboximidamide
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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 | 4.1115 mL | 20.5575 mL | 41.1150 mL | |
| 5 mM | 0.8223 mL | 4.1115 mL | 8.2230 mL | |
| 10 mM | 0.4112 mL | 2.0558 mL | 4.1115 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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