巴利卡替 /Balicatib
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货号：A254787
同义名：
AAE581
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.
Balicatib 化学结构
Balicatib 3D分子结构
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价格
会员价
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Balicatib 纯度/质量文件 产品仅供科研
货号：A254787
标准纯度：
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产品说明书
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Balicatib 质控信息
Z-FA-FMK
✔
99%+
Leupeptin hemisulfate
✔
97%
PMSF
✔
95%
PD 151746
+
μ-Calpain, IC50: 260 nM
m-calpain, IC50: 5.33 μM
98%
Odanacatib
++++
Cathepsin K (rabbit), IC50: 1 nM
Cathepsin K (human), IC50: 0.2 nM
99%+
E-64
+++
Cysteine protease, IC50: 9 nM
99%+
E 64c
✔
95%
E-64d
✔
99%+
MG-101
✔
98%+
Calpeptin
++
Calpain II (porcine kidney), ID50: 40 nM
Calpain I (porcine erythrocytes), ID50: 52 nM
98%+
Cathepsin inhibitor 1
+++
Cathepsin L2, pIC50: 5.5
Cathepsin L, pIC50: 7.9
98%
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Balicatib 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] [4]
作用机制
Balicatib targets to lysosomes by conjugating with poly(ethylene glycol) polymers.
Balicatib 动物研究
Dose
Cynomolgus monkey: 3 mg/kg - 50 mg/kg[3] [2]
Administration
p.o.
Balicatib 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.
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Balicatib 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
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
Balicatib 技术信息
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