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CAS No.: 354813-19-7

Balicatib/巴利卡替 Catalog No. CSN16928

Synonyms: AAE581;巴利卡替

Balicatib is a potent and selective inhibitor of cathepsin K ,with 10-100 fold more potent in cell-based enzyme occupancy assays than against cathepsin B, L, and S.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

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 K_i 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.
动物研究
剂量
Cynomolgus monkey: 3 mg/kg - 50 mg/kg^[3] (p.o.) Rat: 10 mg/kg^[2] (p.o.)

给药途径
p.o.
临床研究

动物研究
剂量	Cynomolgus monkey: 3 mg/kg - 50 mg/kg^[3] (p.o.) Rat: 10 mg/kg^[2] (p.o.)
给药途径	p.o.

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT00371670	Knee Osteoarthritis	Phase 2	Completed	-	United States, Alabama ... more >> Pinnacle Research Group Anniston, Alabama, United States, 36207 Germany Novartis Nuernberg, Germany Collapse <<

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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4299 mL
- 12.1495 mL
- 24.2990 mL
- 5 mM
- 0.4860 mL
- 2.4299 mL
- 4.8598 mL
- 10 mM
- 0.2430 mL
- 1.2149 mL
- 2.4299 mL

技术信息

CAS号

354813-19-7

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C23H33N5O2

运输

蓝冰

分子量

411.54

别名

AAE581;巴利卡替

溶解度

DMSO	82.0 mg/mL (199.3 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (7.3 mM)

动物实验配方

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