Artefenomel
Based on 2 publication(s) in Google Scholar
Artefenomel (OZ439) is an orally active, synthetic anti-malarial compound containing an artemisinin pharmacophore with a mechanism of action similar to that of artemisinin. Artefenomel has antiviral activity against SARS-CoV-2.
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 : 98.56%
- CAS 番号: 1029939-86-3
- 分子式: C28H39NO5
- 分子量:469.61
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保管条件:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
MedChemExpress(MCE)の使用を引用している文献 Artefenomel
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生物活性
製品説明
IC50 & Target
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Plasmodium |
体外実験
Artefenomel (OZ439) (10 μg/mL, 2 h) can alkylate Plasmodium falciparum proteins[1].
Artefenomel (0.3-300 μM) reduces ACE2 expression in Vero cells in a dose-dependent manner and does not induce any cytotoxicity at concentrations up to 300 μM[2].
Artefenomel (33-100 μM) can completely prevent the virus-induced CPE and inhibit SARS-CoV-2 in a dose-dependent manner with an IC50 of 2.9 μM[2].
Artefenomel (0-10 μg/mL) affects red blood cells and induces anaemia, thereby inducing histological changes (cell death) and macroscopic abnormalities in the embryo from pregnant Crl:CD(SD)BR rats[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:embryos from pregnant Crl:CD(SD)BR rats
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Concentration:0.1, 1, 2, 5, 7.5, and 10 µg/mL
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Incubation Time:
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Result:Showed a slightly shortened tail or slightly delayed telencephalic vesicles at 5 μg/mL, a decrease in the number of circulating red blood cells at 7.5 μg/mL and an arrhythmogenic heartbeat at 10 μg/mL.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1029939-86-3
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性状 Solid
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分子量 469.61
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分子式 C28H39NO5
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Color White to off-white
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SMILES
[H][C@@]1(C[C@H](C2)C3)C4([C@@]3([H])C[C@H]2C1)O[C@]5(OO4)CC[C@H](CC5)C6=CC=C(C=C6)OCCN7CCOCC7
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別名
OZ439
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Publications (2)
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Journal Impact Factor
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Most Recent
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Travel Med Infect Dis
Artemisinin resistance-associated gene mutations in Plasmodium falciparum: A case study of severe malaria from Mozambique. [Abstract]2024 Jan-Feb:57:102684. PMID: 38159875 -
Vet Parasitol
Inhibitory effects on bovine babesial infection by iron chelator, 1-(N-acetyl-6-aminohexyl)- 3-hydroxy-2-methylpyridin-4-one (CM1), and antimalarial drugs. [Abstract]2023 Dec:324:110055. PMID: 37931475
溶剤 & 溶解度
体外:
DMSO : 4.2 mg/mL (8.94 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, stored under nitrogen). 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, stored under nitrogen). 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 (274 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
[1]. Joëlle Jourdan, et al. Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel). ACS Infect Dis. 2016 Jan 8;2(1):54-61. [Content Brief]
[3]. Robert L Clark, et al. Improved safety margin for embryotoxicity in rats for the new endoperoxide artefenomel (OZ439) as compared to artesunate. Birth Defects Res. 2018 Apr 17;110(7):553-578. [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, 6 months; -20°C, 1 month (protect from light, stored under nitrogen). 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 | 2.1294 mL | 10.6471 mL | 21.2943 mL | 53.2357 mL |
| 5 mM | 0.4259 mL | 2.1294 mL | 4.2589 mL | 10.6471 mL |