Tegobuvir
Based on 5 publication(s) in Google Scholar
Tegobuvir is a specific, covalent inhibitor of the HCV NS5B polymerase.
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- 純度: 98.01%
- CAS 番号: 1000787-75-6
- 分子式: C25H14F7N5
- 分子量:517.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Tegobuvir
More
生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
0.005 μM
Compound: 1, GS-9190
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Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells after 48 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells after 48 hrs by luciferase reporter gene assay
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[PMID: 24224729] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1000787-75-6
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性状 Solid
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分子量 517.40
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分子式 C25H14F7N5
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Color White to off-white
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SMILES
FC1=CC=CC=C1C2=NC3=CN(CC4=NN=C(C5=CC=C(C(F)(F)F)C=C5C(F)(F)F)C=C4)C=CC3=N2
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別名
GS 333126; GS-9190
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (5)
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Journal Impact Factor
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Most Recent
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Cell Rep Med
Human liver-derived organoids recapitulate Oropouche virus infection and manifestation, enabling antiviral drug discovery. [Abstract]2026 Mar 9:102646. PMID: 41806841 -
Proc Natl Acad Sci U S A
Quantifying antiviral activity optimizes drug combinations against hepatitis C virus infection. [Abstract]2017 Feb 21;114(8):1922-1927. PMID: 28174263 -
Antiviral Res
Antiviral candidates against the hepatitis E virus (HEV) and their combinations inhibit HEV growth in in vitro. [Abstract]2019 Oct:170:104570. PMID: 31362004 -
Antimicrob Agents Chemother
2019 May 24;63(6):e00003-19. PMID: 30885901 -
Biochem Biophys Res Commun
2016 Jan 22;469(4):930-5. PMID: 26723253
溶剤 & 溶解度
DMSO : ≥ 50 mg/mL (96.64 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (274 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Bae AS, et al. Allele-specific real-time PCR system for detection of subpopulations of genotype 1a and 1b hepatitis C NS5B Y448H mutant viruses in clinical samples. J Clin Microbiol. 2011 Sep;49(9):3168-74. [Content Brief]
[2]. Hebner CM, et al. The HCV non-nucleoside inhibitor Tegobuvir utilizes a novel mechanism of action to inhibit NS5B polymerase function. PLoS One. 2012;7(6):e39163. [Content Brief]
[3]. Wong KA, et al. Tegobuvir (GS-9190) potency against HCV chimeric replicons derived from consensus NS5B sequences from genotypes 2b, 3a, 4a, 5a, and 6a. Virology. 2012 Jul 20;429(1):57-62. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9327 mL | 9.6637 mL | 19.3274 mL | 48.3185 mL |
| 5 mM | 0.3865 mL | 1.9327 mL | 3.8655 mL | 9.6637 mL | |
| 10 mM | 0.1933 mL | 0.9664 mL | 1.9327 mL | 4.8319 mL | |
| 15 mM | 0.1288 mL | 0.6442 mL | 1.2885 mL | 3.2212 mL | |
| 20 mM | 0.0966 mL | 0.4832 mL | 0.9664 mL | 2.4159 mL | |
| 25 mM | 0.0773 mL | 0.3865 mL | 0.7731 mL | 1.9327 mL | |
| 30 mM | 0.0644 mL | 0.3221 mL | 0.6442 mL | 1.6106 mL | |
| 40 mM | 0.0483 mL | 0.2416 mL | 0.4832 mL | 1.2080 mL | |
| 50 mM | 0.0387 mL | 0.1933 mL | 0.3865 mL | 0.9664 mL | |
| 60 mM | 0.0322 mL | 0.1611 mL | 0.3221 mL | 0.8053 mL | |
| 80 mM | 0.0242 mL | 0.1208 mL | 0.2416 mL | 0.6040 mL |
Tegobuvir 関連分類
HY-10544 関連分類
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