| 產(chǎn)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 |
| 靶點： |
cathepsin K:22 nM (IC50);cathepsin L:48 nM (IC50);Cathepsin B:61 nM (IC50);cathepsin S:2900 nM (IC50);CysteineProtease |
| 體內研究： |
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 |
| 參考文獻： |
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 |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
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： |
部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經(jīng)營許可證（不帶存儲）
營業(yè)執(zhí)照(三證合一)
北京