| 产品描述： | E 2012 is a potent gamma (γ) secretase modulator without affecting Notch processing. E 2012 inhibits 3β-hydroxysterol Δ24-reductase (DHCR24) at the final step in the cholesterol biosynthesis. E 2012 aims at Alzheimer's disease by reduction of amyloid β-42, and induces cataract following repeated doses in the rat |
| 靶点： |
γ-secretase;Gamma-secretase |
| 体内研究： |
In vivo lenticular concentration of E 2012 after 13-week repeated dose with cataract was well above those where inhibition is observed in vitro. E 2012 induces cataract in the rat by inhibiting DHCR24 at the final step of cholesterol synthesis with associated elevation in desmosterol within the lens, preceded by desmosterol changes that would serve as a predictive safety biomarker for lenticular opacity |
| 参考文献： |
1. Nakano-Ito K, et al. E2012-induced cataract and its predictive biomarkers. Toxicol Sci. 2014 Jan;137(1):249-58. 2. Portelius E, Van Broeck B, Andreasson U, Gustavsson MK, Mercken M, Zetterberg H, Borghys H, Blennow K.Acute effect on the Aβ isoform pattern in CSF in response to γ-secretase modulator and inhibitor treatment in dogs.J Alzheimers Dis. 2010;21(3):1005-12. |
| 溶解性： |
Soluble in DMSO |
| 保存条件： |
2-8℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.384 ml |
11.919 ml |
23.838 ml |
| 5 mM |
0.477 ml |
2.384 ml |
4.768 ml |
| 10 mM |
0.238 ml |
1.192 ml |
2.384 ml |
| 50 mM |
0.048 ml |
0.238 ml |
0.477 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京