产品描述: | T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes |
靶点: |
IC50: 6.75 pM (MMP-13);MMP |
体外研究: |
T-26c significantly inhibits the breakdown of collagen (87.4% inhibition at 0.1 μM) in IL-1β and oncostatin M stimulated cartilage. |
体内研究: |
T-26c is well absorbed in all species at the oral dose of 10–20 mg/kg. Oral administration of the disodium salt formulations of T-26c to guinea pigs results in significant increases in AUC (8357 ng h/mL) and Cmax (1445 ng/ mL) compared with those of the free acid T-26c (AUC = 6478 ng h/ mL and Cmax= 911 ng/mL). |
参考文献: |
1. Nara H, et al. Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site. Bioorg Med Chem. 2014 Oct 1;22(19):5487-505. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20°C |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
2.085 ml |
10.427 ml |
20.855 ml |
5 mM |
0.417 ml |
2.085 ml |
4.171 ml |
10 mM |
0.209 ml |
1.043 ml |
2.085 ml |
50 mM |
0.042 ml |
0.209 ml |
0.417 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。 |