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.
In Vitro Activity
Artefenomel (OZ439) (10 μg/mL, 2 h) can alkylate Plasmodium falciparum proteins.
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.
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.
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.
Storage & Handling
Storage
-20 °C, protect from light, stored under nitrogen
In solvent : -80 °C, 6 months; -20 °C, 1 month (protect from light, stored under nitrogen)
Shipping
Room temperature in continental US; may vary elsewhere.
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