Balicatib

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Chemical Structure| 354813-19-7 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 :

DMSO: 80 mg/mL(194.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
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.