| 产品描述： | Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis |
| 靶点： |
cathepsin K:22 nM (IC50);cathepsin L:48 nM (IC50);Cathepsin B:61 nM (IC50);cathepsin S:2900 nM (IC50);CysteineProtease |
| 体内研究： |
Balicatib (0, 3, 10, 50 mg/kg; Oral gavage; twice daily for 18 months) partially prevented ovariectomyinduced changes in bone mass, inhibited bone turnover at most sites, and had an stimulatory effect on periosteal bone formation in cynomolgus monkeys |
| 参考文献： |
1. Jerome C, et al. Balicatib, a cathepsin K inhibitor, stimulates periosteal bone formation in monkeys. Osteoporos Int. 2012 Jan;23(1):339-49. 2. Gauthier JY, et al. The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K. Bioorg Med Chem Lett. 2008 Feb 1;18(3):923-8. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
2-8℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.43 ml |
12.149 ml |
24.299 ml |
| 5 mM |
0.486 ml |
2.43 ml |
4.86 ml |
| 10 mM |
0.243 ml |
1.215 ml |
2.43 ml |
| 50 mM |
0.049 ml |
0.243 ml |
0.486 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京