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Relacatib

Chemical Structure : Relacatib

CAS No.: 362505-84-8

Relacatib (SB-462795;GSK-462795)

Catalog No.: PC-62962Not For Human Use, Lab Use Only.

Relacatib (SB-462795, GSK-462795) is a potent and orally bioavailable small molecule cathepsin inhibitor with Ki of 41, 68 and 53 pM for cathepsin K, L and V, respectively.

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    Biological Activity

    Relacatib (SB-462795, GSK-462795) is a potent and orally bioavailable small molecule cathepsin inhibitor with Ki of 41, 68 and 53 pM for cathepsin K, L and V, respectively.
    Relacatib displays 39-300-fold selectivity over other cathepsins.
    Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC50 of 45 nM and 70 nM, respectively.
    Relacatib inhibits bone resorption both in vitro in human tissue and in vivo in cynomolgus monkeys.

    Physicochemical Properties

    M.Wt 540.635
    Formula C27H32N4O6S
    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

    N-((S)-4-methyl-1-(((4S,7R)-7-methyl-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl)amino)-1-oxopentan-2-yl)benzofuran-2-carboxamide

    References

    1. Yamashita DS, et al. J Med Chem. 2006 Mar 9;49(5):1597-612.

    2. Kumar S, et al. Bone. 2007 Jan;40(1):122-31.

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