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Balicatib
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。
Balicatib图片
CAS NO:354813-19-7
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
Balicatib (AAE581) 是一种有效的、具有口服活性的选择性组织蛋白酶 K 抑制剂,对组织蛋白酶 K、组织蛋白酶 B、组织蛋白酶 L、组织蛋白酶 S 的 IC50 值分别为 22、61、48、2900 nM。
Cas No.354813-19-7
别名巴利卡替; AAE581
化学名N-[1-(cyanomethylcarbamoyl)cyclohexyl]-4-(4-propylpiperazin-1-yl)benzamide
Canonical SMILESCCCN1CCN(CC1)C2=CC=C(C=C2)C(=O)NC3(CCCCC3)C(=O)NCC#N
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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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] Bromme D, Lecaille F. Cathepsin K inhibitors for osteoporosis and potential off-target effects. Expert Opin Investig Drugs. 2009 May;18(5):585-600.