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TKB245

Chemical Structure : TKB245

CAS No.: 2892688-16-1

TKB245 (TKB-245)

Catalog No.: PC-49864Not For Human Use, Lab Use Only.

TKB245 (TKB-245) is a potent, specific SARS-CoV-2 Mpro inhibitor with IC50 of 7 nM, exhibits highly potent anti-SARS-CoV-2 activity with EC50 and EC95 values of 0.03 and 0.53 µM, respectively.

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    Biological Activity

    TKB245 (TKB-245) is a potent, specific SARS-CoV-2 Mpro inhibitor with IC50 of 7 nM, exhibits highly potent anti-SARS-CoV-2 activity with EC50 and EC95 values of 0.03 and 0.53 µM, respectively.
    TKB245 does not inhibits human cysteine enzymes, cathepsin L and calpain.
    TKB245 demonstrates comparably active against a variety of SARS-CoV-2 variants including alpha, beta, gamma, delta, kappa, and omicron species (EC50=14-56 nM).
    TKB245 exerts potent activity against SARS-CoV-2TWK521 with EC50 values of 0.021 and 0.0027 µM, respectively in HeLa-ACE2-TMPRSS2 and A549-ACE2-TMPRSS2 cells.
    TKB245 exhibits significantly more potent activity than the two existing anti-SARS-CoV-2 drugs: molnupiravir and nirmatrelvir.

    Physicochemical Properties

    M.Wt 653.69
    Formula C30H35F4N5O5S
    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

    (1R,2S,5S)-3-((S)-3,3-dimethyl-2-(2,2,2-trifluoroacetamido)butanoyl)-N-((S)-1-(4-fluorobenzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide

    References

    1. Higashi-Kuwata N, et al. Nat Commun. 2023 Feb 25;14(1):1076.

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