Tegobuvir
Modify Date: 2024-01-11 21:32:27
Tegobuvir structure
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Common Name | Tegobuvir | ||
|---|---|---|---|---|
| CAS Number | 1000787-75-6 | Molecular Weight | 517.401 | |
| Density | 1.5±0.1 g/cm3 | Boiling Point | 558.0±60.0 °C at 760 mmHg | |
| Molecular Formula | C25H14F7N5 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 291.3±32.9 °C | |
Use of TegobuvirTegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase. |
| Name | 5-[[6-[2,4-bis(trifluoromethyl)phenyl]pyridazin-3-yl]methyl]-2-(2-fluorophenyl)imidazo[4,5-c]pyridine |
|---|---|
| Synonym | More Synonyms |
| Description | Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase. |
|---|---|
| Related Catalog | |
| In Vitro | Tegobuvir rapidly increases the proportion of replicons with the Y448H mutation in a dose-dependent manner. After 3 days of treatment, 1.2%, 6.8%, and > 50% of the replicon population expresses Y448H with the use of Tegobuvir at 1, 10, and 20 times its 50% effective concentration, respectively[1]. Tegobuvir exerts anti-HCV activity utilizing a unique chemical activation and subsequent direct interaction with the NS5B protein. Treatment of HCV subgenomic replicon cells with Tegobuvir results in a modified form of NS5B with a distinctly altered mobility on a SDS-PAGE gel[2]. Tegobuvir is potent in GT1a and 1b with mean EC50s of 19.8 and 1.5 nM respectively. For genotype 3a, 4a, and 6a Con chimeras, tegobuvir EC50s are all greater than 100 nM. The F445C NS5B mutations in GT3a, 4a, and 6a chimeric replicons restore tegobuvir potency to EC50 levels comparable to GT1a[3]. |
| Cell Assay | Replicon-containing cells are trypsinized and seeded in cell culture media without G418 in white 96-well plates for EC50 analysis. Stable replicon carrying cell lines are seeded at a density of 5,000 cells per well. Serial threefold dilutions (10 concentrations) of compounds are performed in DMSO followed by further dilution in cell culture media and subsequent addition to cell plates. Compound-treated cells are incubated 72 hours at 37°C in a 5% CO2 incubator. |
| References |
| Density | 1.5±0.1 g/cm3 |
|---|---|
| Boiling Point | 558.0±60.0 °C at 760 mmHg |
| Molecular Formula | C25H14F7N5 |
| Molecular Weight | 517.401 |
| Flash Point | 291.3±32.9 °C |
| Exact Mass | 517.113770 |
| PSA | 56.49000 |
| LogP | 4.07 |
| Vapour Pressure | 0.0±1.5 mmHg at 25°C |
| Index of Refraction | 1.605 |
| Storage condition | 2-8℃ |
| 5-({6-[2,4-Bis(trifluoromethyl)phenyl]-3-pyridazinyl}methyl)-2-(2-fluorophenyl)-5H-imidazo[4,5-c]pyridine |
| 5H-Imidazo[4,5-c]pyridine, 5-[[6-[2,4-bis(trifluoromethyl)phenyl]-3-pyridazinyl]methyl]-2-(2-fluorophenyl)- |
| tegobuvir |
| 5-({6-[2,4-bis(trifluoromethyl)phenyl]pyridazin-3-yl}methyl)-2-(2-fluorophenyl)-5H-imidazo[4,5-c]pyridine |
| Tegobuvir [USN:INN] |
| Tegobuvir (USAN/INN) |