Lomibuvir
Based on 2 publication(s) in Google Scholar
Lomibuvir (VX-222), a selective, non-nucleoside polymerase inhibitor, targets thumb pocket 2 of the HCV NS5B polymerase (RdRp) with a Kd of 17 nM. Lomibuvir inhibits the 1b/Con1 HCV subgenomic replicon with an EC50 of 5.2 nM. Lomibuvir preferentially inhibits elongative RNA synthesis rather than de novo-initiated RNA synthesis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.71%
- No. CAS: 1026785-55-6
- Fòrmula: C25H35NO4S
- Peso molecular:445.61
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Anti-Hepatitis C Virus Compound Library
HY-L073
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Targeted Diversity Library
HY-L099
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Human Metabolite Library
HY-L123
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Heterocyclic Compound Library
HY-L138
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Highly Selective Inhibitors Library
HY-L158
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Drug Repurposing Compound Library Plus
HY-L035P
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Clinical Compound Library Plus
HY-L026P
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Mass Spectrometry Human Metabolite Library
HY-L215
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Alkyne Compound Library
HY-L258
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Anti-Infection Compound Library
HY-L002
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Cell Cycle/DNA Damage Compound Library
HY-L004
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Clinical Compound Library
HY-L026
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Antiviral Compound Library
HY-L027
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Anti-Aging Compound Library
HY-L034
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Drug Repurposing Compound Library
HY-L035
Publications Citing Use of MedChemExpress (MCE) Lomibuvir
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | CC50 |
>20 μM
Compound: 1
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Cytotoxicity against human Huh-7 cells transfected with HCV subgenomic replicon for NS5B polymerase assessed as reduction in cell viability
Cytotoxicity against human Huh-7 cells transfected with HCV subgenomic replicon for NS5B polymerase assessed as reduction in cell viability
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[PMID: 28197321] |
| Huh-7 | CC50 |
>=20 μM
Compound: 3, Lomibuvir
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Cytotoxicity against human HuH7 cells after 3 days by Cell Titre Glo assay
Cytotoxicity against human HuH7 cells after 3 days by Cell Titre Glo assay
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[PMID: 24144213] |
| Huh-7 | EC50 |
13 nM
Compound: 3, Lomibuvir
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Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as observed antiviral potency after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as observed antiviral potency after 72 hrs by luciferase reporter gene assay
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[PMID: 24144213] |
| Huh-7 | EC50 |
15 nM
Compound: lomibuvir
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Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus genotype 1a infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay
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[PMID: 23768906] |
| Huh-7 | EC50 |
2.8 nM
Compound: 3, Lomibuvir
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Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as intrinsic antiviral potency after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus H77 genotype 1a infected in human HuH7 cells assessed as intrinsic antiviral potency after 72 hrs by luciferase reporter gene assay
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[PMID: 24144213] |
| Huh-7 | EC50 |
23 nM
Compound: lomibuvir
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Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7.5 cells after 3 days by luciferase reporter gene assay
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[PMID: 23768906] |
| Huh-7 | EC50 |
6 nM
Compound: 3, Lomibuvir
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Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay
Antiviral activity against Hepatitis C virus Con1 genotype 1b infected in human HuH7 cells after 72 hrs by luciferase reporter gene assay
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[PMID: 24144213] |
| MT4 | CC50 |
>20 μM
Compound: 3, Lomibuvir
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Cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay
Cytotoxicity against human MT4 cells after 5 days by Cell Titre Glo assay
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[PMID: 24144213] |
Lomibuvir (VX-222) inhibits WT HCV 1b/Con1 replicon with an EC50 of 5.2 nM. Lomibuvir inhibits M423T, L419M and I482L (mutant replicons) with EC50s of 79.8, 563.1, 45.3 nM, respectively. Lomibuvir reduces de novo initiation slightly but also shows strong inhibition of primer extension. The IC50 of Lomibuvir for primer-extended RNA synthesis is 31 nM[1].
Lomibuvir is a non-nucleoside, allosteric inhibitor of the hepatitis C virus NS5B polymerase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1026785-55-6
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Appearance Solid
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Peso molecular 445.61
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Fòrmula C25H35NO4S
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Color White to off-white
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SMILES
O=C(C1=C(N([C@@H]2CC[C@@H](O)CC2)C([C@H]3CC[C@H](C)CC3)=O)C=C(C#CC(C)(C)C)S1)O
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Synonyms
VX-222
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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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 -
J Virol Methods
2019 Aug:270:1-11. PMID: 31004661
Solvente y solubilidad
DMSO : 100 mg/mL (224.41 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.5 mg/mL (5.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Pureza y Documentación
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Ficha de datos (276 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Yi G, Deval J, et al. Biochemical study of the comparative inhibition of hepatitis C virus RNA polymerase by VX-222 and filibuvir. Antimicrob Agents Chemother. 2012;56(2):830-837. [Content Brief]
[2]. Li P, Dorsch W, et al. Discovery of Novel Allosteric HCV NS5B Inhibitors. 2. Lactam-Containing Thiophene Carboxylates. ACS Med Chem Lett. 2017;8(2):251-255. Published 2017 Jan 31. [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 | 2.2441 mL | 11.2205 mL | 22.4409 mL | 56.1023 mL |
| 5 mM | 0.4488 mL | 2.2441 mL | 4.4882 mL | 11.2205 mL | |
| 10 mM | 0.2244 mL | 1.1220 mL | 2.2441 mL | 5.6102 mL | |
| 15 mM | 0.1496 mL | 0.7480 mL | 1.4961 mL | 3.7402 mL | |
| 20 mM | 0.1122 mL | 0.5610 mL | 1.1220 mL | 2.8051 mL | |
| 25 mM | 0.0898 mL | 0.4488 mL | 0.8976 mL | 2.2441 mL | |
| 30 mM | 0.0748 mL | 0.3740 mL | 0.7480 mL | 1.8701 mL | |
| 40 mM | 0.0561 mL | 0.2805 mL | 0.5610 mL | 1.4026 mL | |
| 50 mM | 0.0449 mL | 0.2244 mL | 0.4488 mL | 1.1220 mL | |
| 60 mM | 0.0374 mL | 0.1870 mL | 0.3740 mL | 0.9350 mL | |
| 80 mM | 0.0281 mL | 0.1403 mL | 0.2805 mL | 0.7013 mL | |
| 100 mM | 0.0224 mL | 0.1122 mL | 0.2244 mL | 0.5610 mL |
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