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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.56%
- CAS. Nr.: 1029939-86-3
- Formel: C28H39NO5
- Molecular Weight:469.61
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Speicherung:
-20°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Artefenomel
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Biologische Aktivität
Beschreibung
IC50 & Target
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Plasmodium |
In Vitro
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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1029939-86-3
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Appearance Solid
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Molecular Weight 469.61
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Formel 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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Synonyms
OZ439
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-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
Lösungsmittel & Löslichkeit
In Vitro:
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.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
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Data Sheet (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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Handling Instructions (2659 KB)
Verweise
[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 |
Artefenomel Related Classifications
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