| 产品描述： | δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research |
| 靶点： |
Caspase-3:31.86 ± 1. μM (IC50);Caspase-8:86.71 ± 10 μM (IC50) |
| 体外研究： |
δ-Secretase inhibitor 11 (化合物 11) (0-1 μM，10 分钟) 以浓度和时间依赖性方式抑制 δ-分泌酶。 δ-Secretase inhibitor 11 (0-1 μM) 通过 δ-分泌酶选择性地阻断 tau 和 APP (淀粉样前体蛋白) 片段化 |
| 体内研究： |
δ-Secretase inhibitor 11 (化合物 11) (10 mg/kg，口服，每天一次，持续 3 个月) 减轻 OGD (氧糖剥夺) 诱导的神经元损伤，并特别发挥神经保护作用。 δ-Secretase inhibitor 11 (0-10 mg/kg，口服，每天一次，持续 1.5 个月和 3 个月) 抑制 δ-分泌酶活性，减轻 5XFAD 小鼠模型中的 Aβ 沉积和认知缺陷。 Animal Model: Tau P301S transgenic mice (n=4 mice per group) Dosage: 10 mg/kg Administration: Orally, once daily for 3 months Result: Significantly inhibited the activity of δ-secretase in both wild-type and tau P301S mice brain, increased PP2A activity, and attenuated the truncation and phosphorylation of tau in tau P301S mice. Ameliorated synaptic loss and restored synaptic dysfunction in tau P301S mice. Animal Model: 5XFAD mice Dosage: 2, 5 or 10 mg kg Administration: Orally, once daily for 1.5 and 3 months Result: Attenuated the β-secretase-mediated processing of APP, significantly decreased the concentrations of Aβ 1-40 and Aβ 1-42 in the brain lysates, and attenuated Aβ deposition in a time- and dose-dependent manner. |
| 参考文献： |
1. Zhang Z, et al. Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease. Nat Commun. 2017 Mar 27;8:14740. |
| 溶解性： |
Soluble 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 |
4.541 ml |
22.704 ml |
45.407 ml |
| 5 mM |
0.908 ml |
4.541 ml |
9.081 ml |
| 10 mM |
0.454 ml |
2.27 ml |
4.541 ml |
| 50 mM |
0.091 ml |
0.454 ml |
0.908 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