Artefenomel

CAS No. 1029939-86-3

Artefenomel( OZ439 )

Catalog No. M10144 CAS No. 1029939-86-3

Artefenomel (OZ439) is a novel, next-generation antimalarial ozonide that demonstrates high potentcy against P. falciparum in vitro and P. berghei in vivo (K1/NF54, IC50=2.0/3.2 nM).

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    Artefenomel
  • Note
    Research use only, not for human use.
  • Brief Description
    Artefenomel (OZ439) is a novel, next-generation antimalarial ozonide that demonstrates high potentcy against P. falciparum in vitro and P. berghei in vivo (K1/NF54, IC50=2.0/3.2 nM).
  • Description
    Artefenomel (OZ439) is a novel, next-generation antimalarial ozonide that demonstrates high potentcy against P. falciparum in vitro and P. berghei in vivo (K1/NF54, IC50=2.0/3.2 nM).Parasite Infection Phase 2 Clinical.
  • In Vitro
    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. Cell Viability Assay Cell Line:embryos from pregnant Crl:CD(SD)BR rats Concentration:0.1, 1, 2, 5, 7.5, and 10 μg/mL Incubation Time: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.
  • In Vivo
    ——
  • Synonyms
    OZ439
  • Pathway
    Microbiology/Virology
  • Target
    Parasite
  • Recptor
    Parasite
  • Research Area
    Infection
  • Indication
    Parasite Infection

Chemical Information

  • CAS Number
    1029939-86-3
  • Formula Weight
    469.622
  • Molecular Formula
    C28H39NO5
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 4.2 mg/mL (8.94 mM)
  • SMILES
    C1CC2(CCC1C3=CC=C(C=C3)OCCN4CCOCC4)OC5(C6CC7CC(C6)CC5C7)OO2
  • Chemical Name
    4-[2-(4-cis-Dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.13,7]decan]-4-ylphenoxy)ethyl]morpholine

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Dong Y, et al. J Med Chem. 2017 Apr 13;60(7):2654-2668. 2. Kim HS, et al. J Med Chem. 2017 Apr 13;60(7):2651-2653. 3. Macintyre F, et al. BMC Med. 2017 Oct 9;15(1):181. 4. Yang T, et al. Antimicrob Agents Chemother. 2016 Jul 22;60(8):4501-10.
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