Obeldesivir
Based on 1 publication(s) in Google Scholar
Obeldesivir (ATV006) is a potent, orally active antiviral agent and ester proagents of GS-441524. Obeldesivir inhibits the replication of SARS-CoV-2 and its variants. Obeldesivir can be used for SARS-CoV-2 research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.53%
- No. CAS: 2647441-36-7
- Fòrmula: C16H19N5O5
- Peso molecular:361.35
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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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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Publications Citing Use of MedChemExpress (MCE) Obeldesivir
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against human primary hepatocytes assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human primary hepatocytes assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| HepG2 | CC50 |
71 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human HepG2 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| Huh-7 | CC50 |
>44 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against human Huh-7 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| MRC5 | CC50 |
>44 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against human MRC5 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human MRC5 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| MT4 | CC50 |
>50 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against human MT4 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| PBMC | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against quiescent human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against quiescent human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| PBMC | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against stimulated human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against stimulated human PBMC cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
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[PMID: 37596939] |
| PC-3 | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
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Cytotoxicity against human PC-3 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell growth measured after 5 days by CellTiter-Glo assay
|
[PMID: 37596939] |
Obeldesivir (0.001-100 μM; 48 h; Vero E6 cells) inhibits the replication of authentic SARS-CoV-2 and its variants of concern. Obeldesivir has an overall >4-fold and >12-fold potency improvement in inhibiting the replication of Delta and Omicron variants, with EC50 values of 0.349 μM and 0.106 μM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Obeldesivir (250-500 mg/kg; p.o.; daily, for 4 days; hACE2 knock-in and Ad5-hACE2 mice) has antiviral activity and inhibits SARS-CoV-2 replication in mouse models[1].
Obeldesivir (100-250 mg/kg; p.o.; daily, for 10 days) reduces lung damage and protects K18-hACE2 mice[1].
Obeldesivir (10-150 mg/kg; p.o.; daily, for 3 days) reduces virus titers and lung damage caused by Delta variant infection in K18-hACE2 mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague Dawley rats[1]
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Dosage:5 and 25 mg/kg
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Administration:Oral administration (25 mg/kg) and intravenous injection (5 mg/kg)
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Result:
1.19 parameters i.v. (5 mg/kg) p.o. (25 mg/kg) AUClast (μM·h) 5.6 22.8 T1/2 (h) 1.5 1.2 Tmax (h) 0.5 Cmax (μM) 8.7 8.2 F % 81.5
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Animal Model:hACE2 knock-in and Ad5-hACE2 mice[1]
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Dosage:250 and 500 mg/kg
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Administration:Oral administration; daily, for 4 days
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Result:Inhibited gRNA and sgRNA, which is Biomarkers of coronavirus replication. Reduced the viral load and pathological damage of the lung.
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Animal Model:K18-hACE2 mice[1]
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Dosage:100 and 250 mg/kg
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Administration:Oral administration; daily, for 10 days
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Result:Reduced viral RNA and increased the survival rate of mice. Reduced evidence of lung pathology and the production of inflammatory cytokines and chemokines in the lung tissues.
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Animal Model:K18-hACE2 mice[1]
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Dosage:10, 30, 80 and 150 mg/kg
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Administration:Oral administration; daily, for 3 days
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Result:Reduced viral load in a dose-dependent manner and alleviated the symptoms in the lung.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2647441-36-7
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Appearance Solid
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Peso molecular 361.35
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Fòrmula C16H19N5O5
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Color White to off-white
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SMILES
N#C[C@@]1(C2=CC=C3N2N=CN=C3N)O[C@@H]([C@H]([C@H]1O)O)COC(C(C)C)=O
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Synonyms
ATV006
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
DMSO : 250 mg/mL (691.85 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (285 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7674 mL | 13.8370 mL | 27.6740 mL | 69.1850 mL |
| 5 mM | 0.5535 mL | 2.7674 mL | 5.5348 mL | 13.8370 mL | |
| 10 mM | 0.2767 mL | 1.3837 mL | 2.7674 mL | 6.9185 mL | |
| 15 mM | 0.1845 mL | 0.9225 mL | 1.8449 mL | 4.6123 mL | |
| 20 mM | 0.1384 mL | 0.6918 mL | 1.3837 mL | 3.4592 mL | |
| 25 mM | 0.1107 mL | 0.5535 mL | 1.1070 mL | 2.7674 mL | |
| 30 mM | 0.0922 mL | 0.4612 mL | 0.9225 mL | 2.3062 mL | |
| 40 mM | 0.0692 mL | 0.3459 mL | 0.6918 mL | 1.7296 mL | |
| 50 mM | 0.0553 mL | 0.2767 mL | 0.5535 mL | 1.3837 mL | |
| 60 mM | 0.0461 mL | 0.2306 mL | 0.4612 mL | 1.1531 mL | |
| 80 mM | 0.0346 mL | 0.1730 mL | 0.3459 mL | 0.8648 mL | |
| 100 mM | 0.0277 mL | 0.1384 mL | 0.2767 mL | 0.6918 mL |
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