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3CLpro inhibitor 6j

Chemical Structure : 3CLpro inhibitor 6j

CAS No.: 2477631-46-0

3CLpro inhibitor 6j (GC376 analog 6j)

Catalog No.: PC-72204Not For Human Use, Lab Use Only.

3CLpro inhibitor 6j (GC376 analog 6j) is a potent, selective inhibitor of Coronavirus 3C-like proteases (3CLpro) with IC50 of 0.08, 1.2, and 0.48 uM against MERS-CoV, SARS-CoV, and SARS-CoV-2 FRET 3CLpro in enzyme assays, respectively.

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    Biological Activity

    3CLpro inhibitor 6j (GC376 analog 6j) is a potent, selective inhibitor of Coronavirus 3C-like proteases (3CLpro) with IC50 of 0.08, 1.2, and 0.48 uM against MERS-CoV, SARS-CoV, and SARS-CoV-2 FRET 3CLpro in enzyme assays, respectively.
    3CLpro inhibitor 6j blocked replication of the human coronaviruses MERS-CoV (EC50=0.04 uM) and SARS-CoV-2 (EC50=0.8 uM) in cultured cells, without significant cytotoxicity (CC50>100 uM).
    3CLpro inhibitor 6j demonstrated in vivo antiviral effects, increased survival and recovery of body weight in hDPP4-KI mice infected with MERSMA-CoV, with reduced lung virus titers and histopathology。

    Physicochemical Properties

    M.Wt 445.508
    Formula C21H33F2N3O5
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    (4,4-difluorocyclohexyl)methyl ((S)-4-methyl-1-oxo-1-(((S)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)amino)pentan-2-yl)carbamate

    References

    1. Athri D Rathnayake, et al. Sci Transl Med. 2020 Aug 19;12(557):eabc5332.

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