同义名 :	AAE581
	CAS号 :	354813-19-7
	货号 :	A254787
	分子式 :	C23H33N5O2
	纯度 :	98%+
	分子量 :	411.54
	MDL号 :	MFCD19443790
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性
描述	Cathepsin K is a member of the papain family of cysteine proteases which is associated with osteopetrosis, impaired resorption of bone matrix, impaired processing of thyroglobulin and reduced release of thyroid hormone. Balicatib is a very potent and selective inhibitor of human cathepsin K, with a Ki value of 0.7 nM. 140 postmenopausal women administered of AAE-581 once a day orally (10-50 mg per day) showed successful reduced bone resorption and improved bone formation[3]. Balicatib treatment for 18 months in female cynomolgus monkeys (orally twice daily by nasogastric intubation, 10/30/50 mg/kg/day) partially prevented ovariectomy-induced changes in bone mass and inhibited cancellous bone turnover[4].
作用机制	Balicatib targets to lysosomes by conjugating with poly(ethylene glycol) polymers.

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.43mL 0.49mL 0.24mL	12.15mL 2.43mL 1.21mL	24.30mL 4.86mL 2.43mL

参考文献

[1]Vasiljeva O, Reinheckel T, et al. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403. [2]Falgueyret JP, Desmarais S, et al. Lysosomotropism of basic cathepsin K inhibitors contributes to increased cellular potencies against off-target cathepsins and reduced functional selectivity. J Med Chem. 2005 Dec 1;48(24):7535-43. [3]Vasiljeva O, Reinheckel T, Peters C, Turk D, Turk V, Turk B. Emerging roles of cysteine cathepsins in disease and their potential as drug targets. Curr Pharm Des. 2007;13(4):387-403. doi: 10.2174/138161207780162962. PMID: 17311556. [4]Jerome C, Missbach M, Gamse R. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2012 Jan;23(1):339-49. doi: 10.1007/s00198-011-1593-2. Epub 2011 Mar 5. PMID: 21380636.