Balicatib is an inhibitor of cathepsin K with IC50 value of 1.4nM [1].

Balicatib is highly selective against cathepsin K over cathepsin B, L and S in the in vitro enzyme assay. However, the selectivity is not so high in cell-based enzyme assay. The lysosomotropic character of balicatib results in its accumulation in lysosomes and the subsequent nonselective off-target effects. The off-target effects also cause the skin adverse events of balicatib [1, 2].

As a cathepsin K inhibitor, balicatib is developed for osteoporosis. It has been reported to reduce the biochemical markers of bone resorption and increase bone mineral density in ovariectomized monkeys. In addition, balicatib shows benefits in new bone formation of postmenopausal women [2].

References:

[1] Black WC. Peptidomimetic inhibitors of cathepsin K. 2010;10(7):745-51.

[2] Br?mme D, Lecaille F. Cathepsin K inhibitors for osteoporosis and potential off-target effects. Expert Opin Investig Drugs. 2009 May;18(5):585-600.

特别提醒：                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗，食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康，请穿好实验服并佩戴一次性手套和口罩操作。