| 產(chǎn)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 |
| 靶點(diǎn)： |
IC50: 6.75 pM (MMP-13);MMP |
| 體外研究： |
T-26c significantly inhibits the breakdown of collagen (87.4% inhibition at 0.1 μM) in IL-1β and oncostatin M stimulated cartilage. |
| 體內(nèi)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). |
| 參考文獻(xiàn)： |
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 |
| 保存條件： |
-20°C |
| 配置溶液濃度參考： |
|
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(quán)威性，僅供客戶參考交流研究之用。 |
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