| 产品描述: | TM-25659是 具有PDZ结合基序的转录共激活子 (TAZ) 的调制剂。抗骨质疏松和抗肥胖活性。 |
| 靶点: |
TAZ |
| 体外研究: |
TM-25659 (2, 10, 20, 100 μM) enhances nuclear TAZ localization in a dose-dependent manner and attenuates PPARγ-mediated adipocyte differentiation by facilitating PPARγ suppression activity of TAZ . TM-25659 (2, 10, 50 μM) enhances osteogenic gene expression and thereby increases osteoblast differentiation . |
| 体内研究: |
TM-25659 (50 mg/kg, i.p., every other day for 2 weeks) suppresses bone loss in vivo and decreases weight gain in an obesity model.
TM-25659 has a favourable pharmacokinetic profile in rats. The plasma concentration of TM-25659 declines with an approximate t1/2 of 7 or 10 h following i.v or p.o. administration respectively. The systemic clearance (CL) is 0.21 L×h-1×kg-1 and the volume of distribution at steady-state (1.91 L×h-1×kg-1) is larger than the volume of total body fluids. |
| 参考文献: |
1.Jang EJ, et al. TM-25659 enhances osteogenic differentiation and suppresses adipogenic differentiation by modulating the transcriptional co-activator TAZ. Br J Pharmacol. 2012 Mar;165(5):1584-94. |
| 溶解性: |
Souble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.998 ml |
9.988 ml |
19.976 ml |
| 5 mM |
0.4 ml |
1.998 ml |
3.995 ml |
| 10 mM |
0.2 ml |
0.999 ml |
1.998 ml |
| 50 mM |
0.04 ml |
0.2 ml |
0.4 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。 |