ALS-8112
Based on 3 publication(s) in Google Scholar
ALS-8112 is a potent and selective respiratory syncytial virus (RSV) polymerase inhibitor. The 5'-triphosphate form of ALS-8112 inhibits RSV polymerase with an IC50 of 0.02 μM.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.40%
- CAS. Nr.: 1445379-92-9
- Formel: C10H13ClFN3O4
- Molecular Weight:293.68
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) ALS-8112
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Customer Validation & Images
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Cell Proliferation/Viability Assay
Biologische Aktivität
IC50: 0.02 μM (RSV)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | CC50 |
>100 μM
Compound: 2c
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Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay
Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay
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[PMID: 25667954] |
| HeLa | EC50 |
0.15 μM
Compound: 2c
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Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay
Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay
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[PMID: 25667954] |
| HEp-2 | CC50 |
>100 μM
Compound: ALS-8112
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Cytotoxicity against human Hep2 cells assessed as reduction in cell viability measured after 5 days by MTS assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability measured after 5 days by MTS assay
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[PMID: 32143992] |
| HEp-2 | EC50 |
0.92 μM
Compound: 15
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Antiviral activity against RSV A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay
Antiviral activity against RSV A2 infected in human Hep2 cells assessed as protection against virus-induced cytopathic effect after 4 days by Cell-Titer Glo assay
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[PMID: 25978965] |
| HEp-2 | EC50 |
2.6 μM
Compound: ALS-8112
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Antiviral activity against Respiratory syncytial virus A strain Long infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis
Antiviral activity against Respiratory syncytial virus A strain Long infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis
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[PMID: 32143992] |
| HEp-2 | EC50 |
2.6 μM
Compound: ALS-8112
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Antiviral activity against Respiratory syncytial virus B infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis
Antiviral activity against Respiratory syncytial virus B infected in Hep2 cells assessed as reduction in virus-induced cytopathic effect after 5 days by microscopic analysis
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[PMID: 32143992] |
| HEp-2 | IC50 |
1 μM
Compound: 15
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Inhibition of RSV A2 RNA-dependent RNA polymerase expressed in human Hep2 cells using ATP, GTP, UTP, CTP and 1.5 uCi [alpha-32P] NTP as substrate assessed as reduction of total radiolabled transcript after 90 mins by agarose gel electrophoresis
Inhibition of RSV A2 RNA-dependent RNA polymerase expressed in human Hep2 cells using ATP, GTP, UTP, CTP and 1.5 uCi [alpha-32P] NTP as substrate assessed as reduction of total radiolabled transcript after 90 mins by agarose gel electrophoresis
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[PMID: 25978965] |
| MT4 | CC50 |
21 μM
Compound: 15
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Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by Cell-Titer Glo assay
Cytotoxicity against human MT4 cells assessed as cell viability after 5 days by Cell-Titer Glo assay
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[PMID: 25978965] |
The 5'-triphosphate form of ALS-8112 (ALS-8112-TP) is the active form of the drug and selectively inhibits RSV polymerase through chain termination of RNA synthesis[2]. ALS-008112 enters various types of epithelial cells in the respiratory tract and is subsequently phosphorylated to form an intracellular nucleoside triphosphate with a half-life of approximately 29 hours. The nucleoside triphosphate analogue inhibits RSV replication by means of chain termination[3]. ALS-8112 is a pan-strain inhibitor of RSV replication in vitro. The RNA transcription activity of the RSV–RNP complex is dose-proportionally inhibited by ALS-8112-TP with an IC50 of 0.020 ± 0.008 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1445379-92-9
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Appearance Solid
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Molecular Weight 293.68
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Formel C10H13ClFN3O4
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Color White to off-white
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SMILES
OC[C@]1(CCl)[C@@H](O)[C@@H](F)[C@H](N2C(N=C(N)C=C2)=O)O1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Microorganisms
In Silico Identification and In Vitro Validation of Repurposed Compounds Targeting the RSV Polymerase. [Abstract]2023 Jun 18;11(6):1608. PMID: 37375110 -
Antiviral Res
Modular cell-based platform for high throughput identification of compounds that inhibit a viral interferon antagonist of choice. [Abstract]2018 Feb:150:79-92. PMID: 29037975
ALS-8112 purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2018 Feb:150:79-92. [Abstract]
To confirm the antiviral effect of StA-NS2-2, infectious titer produced from compound-treated A549 cells and IFN-deficient Vero cells are examined. The RSV polymerase inhibitor ALS-8112 potently inhibits RSV in both cell types.
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Lösungsmittel & Löslichkeit
DMSO : ≥ 47 mg/mL (160.04 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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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.
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.
Protokoll
ALS-8112 and its prodrug ALS-8176 are stored at 4°C in dimethyl sulfoxide (DMSO), and diluted in water. HEp-2 cells per well are plated in a 96-well plate. Each compound is serially diluted (1:3) up to 9 distinct concentrations. Cells are pre-incubated with compounds for 24 hours at 37°C in a 5% CO2 atmosphere. After 24 hours of pre-incubation with compounds, RSV A2, Long, or B1 at a multiplicity of infection (MOI) of 0.5 is added to the cells, except for the background controls. The plate is then incubated for additional 4 days in the same conditions and at the end of the incubation 50 μL the supernatant from each well of the plate is collected[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (282 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Wang G, et al. Discovery of 4'-chloromethyl-2'-deoxy-3',5'-di-O-isobutyryl-2'-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78. [Content Brief]
[2]. Jordan PC, et al. Activation Pathway of a Nucleoside Analog Inhibiting Respiratory Syncytial Virus Polymerase. ACS Chem Biol. 2017 Jan 20;12(1):83-91. [Content Brief]
[3]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58. [Content Brief]
[4]. Deval J, et al. Molecular Basis for the Selective Inhibition of Respiratory Syncytial Virus RNA Polymerase by 2'-Fluoro-4'-Chloromethyl-Cytidine Triphosphate. PLoS Pathog. 2015 Jun 22;11(6):e1004995. [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 | 3.4051 mL | 17.0253 mL | 34.0507 mL | 85.1267 mL |
| 5 mM | 0.6810 mL | 3.4051 mL | 6.8101 mL | 17.0253 mL | |
| 10 mM | 0.3405 mL | 1.7025 mL | 3.4051 mL | 8.5127 mL | |
| 15 mM | 0.2270 mL | 1.1350 mL | 2.2700 mL | 5.6751 mL | |
| 20 mM | 0.1703 mL | 0.8513 mL | 1.7025 mL | 4.2563 mL | |
| 25 mM | 0.1362 mL | 0.6810 mL | 1.3620 mL | 3.4051 mL | |
| 30 mM | 0.1135 mL | 0.5675 mL | 1.1350 mL | 2.8376 mL | |
| 40 mM | 0.0851 mL | 0.4256 mL | 0.8513 mL | 2.1282 mL | |
| 50 mM | 0.0681 mL | 0.3405 mL | 0.6810 mL | 1.7025 mL | |
| 60 mM | 0.0568 mL | 0.2838 mL | 0.5675 mL | 1.4188 mL | |
| 80 mM | 0.0426 mL | 0.2128 mL | 0.4256 mL | 1.0641 mL | |
| 100 mM | 0.0341 mL | 0.1703 mL | 0.3405 mL | 0.8513 mL |
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