| 靶点: |
Ki: 170 μM (Human GGT) |
| 体内研究: |
GGsTop (1 mg/kg) lowers levels of ALT, AST, γ-GT at 12, 24, and 48 h after ischemia-reperfusion in rats. GGsTop also reduces 4-HNE and TNF-α production, and decreases hepatic necrosis in rats. |
| 参考文献: |
1. Han L, et al. Design, synthesis, and evaluation of gamma-phosphono diester analogues of glutamate as highly potent inhibitors and active site probes of gamma-glutamyl transpeptidase. Biochemistry. 2007 Feb 6;46(5):1432-47. 2. Kamiyama A, et al. Phosphonate-based irreversible inhibitors of human γ-glutamyl transpeptidase (GGT). GGsTop is a non-toxic and highly selective inhibitor with critical electrostatic interaction with an active-site residue Lys562 for enhanced inhibitory activity. Bioorg Med Chem. 2016 Nov 1;24(21):5340-5352. 3. Tamura K, et al. GGsTop, a novel and specific γ-glutamyl transpeptidase inhibitor, protects hepatic ischemia-reperfusion injury in rats. Am J Physiol Gastrointest Liver Physiol. 2016 Aug 1;311(2):G305-12. |
| 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 |
3.019 ml |
15.094 ml |
30.188 ml |
| 5 mM |
0.604 ml |
3.019 ml |
6.038 ml |
| 10 mM |
0.302 ml |
1.509 ml |
3.019 ml |
| 50 mM |
0.06 ml |
0.302 ml |
0.604 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。 |