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TKB248

Chemical Structure : TKB248

CAS No.: 2892688-17-2

TKB248 (TKB-248)

Catalog No.: PC-49865Not For Human Use, Lab Use Only.

TKB248 (TKB-248) is a potent, specific SARS-CoV-2 Mpro inhibitor with IC50 of 74 nM, exhibits highly potent anti-SARS-CoV-2 activity with EC50 and EC95 values of 0.22 and 0.87 µM, respectively.

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    Biological Activity

    TKB248 (TKB-248) is a potent, specific SARS-CoV-2 Mpro inhibitor with IC50 of 74 nM, exhibits highly potent anti-SARS-CoV-2 activity with EC50 and EC95 values of 0.22 and 0.87 µM, respectively.
    TKB248 does not inhibits human cysteine enzymes, cathepsin L and calpain.
    TKB248 demonstrates comparably active against a variety of SARS-CoV-2 variants including alpha, beta, gamma, delta, kappa, and omicron species (EC50=70-430 nM).
    TKB248 exerts potent anti-SARS-CoV-2 activity in VeroE6 cells in the presence of CP100356 with EC50 of 25 nM.
    TKB248 (120 mg/ kg BID, i.p.) exhibits significantly lower virus titer in human ACE2-knocked-in mice following SARS-CoV-2 exposure. 

    Physicochemical Properties

    M.Wt 669.75
    Formula C30H35F4N5O4S2
    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

    2,2,2-trifluoro-N-((S)-1-((1R,2S,5S)-2-(((S)-1-(4-fluorobenzo[d]thiazol-2-yl)-1-oxo-3-((S)-2-oxopyrrolidin-3-yl)propan-2-yl)carbamothioyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-3-yl)-3,3-dimethyl-1-oxobutan-2-yl)acetamide

    References

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

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