354813-19-7Balicatib

产品属性：

Cas No.354813-19-7

别名

化学名 N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide

分子式 C23H33N5O2

分子量 411.54

溶解度 ≥ 17mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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.