|L 006235Cathepsin K inhibitor|
Sample solution is provided at 25 µL, 10mM.
Publications citing ApexBio Products
|Potent, reversible cathepsin K inhibitor (IC50 = 0.25 nM) that displays > 4000-fold selectivity over cathepsins B, L and S.|
|Cas No.||294623-49-7||SDF||Download SDF|
|Solubility||Soluble in DMSO > 10 mM||Storage||Store at 4°C|
IC50: 0.25 nM
L-006235 is a potent and selective inhibitor of Cathepsin K.
In vitro: After dilution of L-006235 to 0.05 nM, the cathepsin K enzyme activity was initially inhibited, but slowly recovered with a first-order rate constant of 0.023 s-1. The final steady-state enzyme activity was 80-90% that of control, suggesting the complete reversibility of the L-006235-cathepsin K complex. L-006235 was found to be not a substrate for the nitrilase activity of Cat K .
In vivo: L-006235 was orally bioavailable in rats, with a terminal half-life of over 3 h. L-006235 was orally dosed in ovariectomized rhesus monkeys once per day for 7 days. Results showed that collagen breakdown products were dose-dependently reduced by up to 76%. Plasma concentrations of L-006235 above the bone resorption IC50 after 24 h indicated a correlation between functional cellular and in vivo assays. These findings suggested that the inhibition of collagen breakdown by cathepsin K inhibitors, such as L-006235, might be useful in osteoporosis and other indications involving bone resorption .
Clinical trial: N/A
 Palmer JT,Bryant C,Wang DX et al. Design and synthesis of tri-ring P3 benzamide-containing aminonitriles as potent, selective, orally effective inhibitors of cathepsin K. J Med Chem.2005 Dec 1;48(24):7520-34.