产品描述: | K 01-162 (K162) inhibits the fibril formation of Aβ peptides and eliminates their neurotoxicity. K 01-162 binds with Aβ42 peptide with an EC50 value of 80 nM. K 01-162 binds directly to AβO with a KD value of 19 μM. K 01-162 is capable of penetrating the brain and can be used for the research of Alzheimer’s disease |
靶点: |
Amyloid-β |
体外研究: |
K 01-162 (1 μM; 24 h) reduces the level of intracellular AβO. K 01-162 (0.78-50 μM; 5 min) blocks the synaptic binding activity of AβO in mouse hippocampal neurons. Western Blot Analysis Cell Line: MC65 cell line Concentration: 1 μM Incubation Time: 24 hours Result: Reduced the levels of SDS-stable Aβ trimer and larger aggregates. |
体内研究: |
K 01-162 (100 μM; intracerebroventricular infusion 0.25 μL/h for 2 weeks) attenuates amyloid load in vivo. Animal Model: 5xFAD mice with cerebral Aβ amyloidosis Dosage: 100 μM Administration: Intracerebroventricular infusion; 100 μM 0.25 μL/h; for 2 weeks Result: Caused no apparent toxicity and significantly reduced the amyloid load in hippocampus to 50% of the mock-treated |
参考文献: |
1. Li J, et al. Alzheimer's disease drug candidates stabilize A-β protein native structure by interacting with the hydrophobic core. Biophys J. 2011 Feb 16;100(4):1076-82. 2. Hong HS, et al. Candidate anti-A beta fluorene compounds selected from analogs of amyloid imaging agents. Neurobiol Aging. 2010 Oct;31(10):1690-9. |
溶解性: |
Soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.47 ml |
17.35 ml |
34.7 ml |
5 mM |
0.694 ml |
3.47 ml |
6.94 ml |
10 mM |
0.347 ml |
1.735 ml |
3.47 ml |
50 mM |
0.069 ml |
0.347 ml |
0.694 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。 |