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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.53%
- CAS 番号: 2647441-36-7
- 分子式: C16H19N5O5
- 分子量:361.35
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
MedChemExpress(MCE)の使用を引用している文献 Obeldesivir
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生物活性
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Hepatocyte | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| HepG2 | CC50 |
71 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| Huh-7 | CC50 |
>44 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| MRC5 | CC50 |
>44 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| MT4 | CC50 |
>50 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| PBMC | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| PBMC | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
|
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
|
[PMID: 37596939] |
| PC-3 | CC50 |
>100 μM
Compound: 3; GS-5245, ODV
|
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 |
化学情報
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CAS 番号 2647441-36-7
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性状 Solid
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分子量 361.35
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分子式 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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別名
ATV006
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
溶剤 & 溶解度
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (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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取扱説明書 (2659 KB)
参考文献
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 |