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L 006235
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
L 006235图片
CAS NO:294623-49-7
规格:98%
分子量:466.6
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Cathepsin K inhibitor
CAS:294623-49-7
分子式:C24H30N6O2S
分子量:466.6
纯度:98%
存储:Store at -20°C

Background:

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 [1].


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 [1].


Clinical trial: N/A


Reference:
[1] 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.