| 靶点: |
IC50: 185 nM (rat Aβ42); 200 nM (human Aβ42); 3.9 μM (ZIKV NS2B-NS3 protease) |
| 体内研究: |
JNJ-40418677 (10-300 mg/kg; p.o.) decreases Aβ42 brain levels in a dose-dependent manner 4 h after treatment, while increasing Aβ38 level in non-transgenic mouse brain. JNJ-40418677 (30 mg/kg; p.o.; once) shows the mean brain and plasma levels 4 h after single dose are both 17 μM, indicating good brain penetration in non-transgenic mouse brain. JNJ-40418677 (20-120 mg/kg; p.o.; 7 months) has good biological tolerance with no adverse effects in a chronic treatment in Tg2576 mice. JNJ-40418677 (20-120 mg/kg; p.o.; 7 months) decreases the plaque number and the area occupied by plaques in Tg2576 mice dose-dependently. |
| 参考文献: |
1. Van Broeck B, et al. Chronic treatment with a novel γ-secretase modulator, JNJ-40418677, inhibits amyloid plaque formation in a mouse model of Alzheimer's disease. Br J Pharmacol. 2011 May;163(2):375-89. 2. Harrie J.M. Gijsen, et al. Chapter Five - Secretase Inhibitors and Modulators as a Disease-Modifying Approach Against Alzheimer's Disease. Annu Rep Med Chem. 2012. 47:55-69.3. Samrat SK, et al. Antiviral Agents against Flavivirus Protease: Prospect and Future Direction. Pathogens. 2022 Feb 25;11(3):293. |
| 溶解性: |
DMSO: soluble15mg/mL, clear |
| 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 |
2.081 ml |
10.407 ml |
20.814 ml |
| 5 mM |
0.416 ml |
2.081 ml |
4.163 ml |
| 10 mM |
0.208 ml |
1.041 ml |
2.081 ml |
| 50 mM |
0.042 ml |
0.208 ml |
0.416 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。 |