产品描述: | FPS-ZM1 is a high-affinity RAGE inhibitor with a Ki of 25 nM. |
靶点: |
Ki: 25 nM (RAGE) |
体内研究: |
FPS-ZM1 is nontoxic to mice and readily crossed the blood-brain barrier. In aged APPsw/0 mice overexpressing human Aβ-precursor protein, a transgenic mouse model of AD with established Aβ pathology, FPS-ZM1 inhibits RAGE-mediated influx of circulating Aβ40 and Aβ42 into the brain. In brain, FPS-ZM1 binds exclusively to RAGE, which inhibits β-secretase activity and Aβ production and suppresses microglia activation and the neuro-inflammatory response. FPS-ZM1 treatment reduces the level of Aβ1-40 and Aβ1-42 in AGEs Rats. It Inhibits AGEs-mediated increase of Aβ-metabolism-related proteins and downregulates AGEs-mediated increase of pro-inflammatory cytokines in the hippocampus. FPS-ZM1 up-Regulates anti-oxidant defense system and attenuated AGEs induced memory impairment in AGEs rats |
参考文献: |
1. Deane R, et al. A multimodal RAGE-specific inhibitor reduces amyloid β-mediated brain disorder in a mouse model of Alzheimer disease. J Clin Invest. 2012 Apr;122(4):1377-92. 2. Hong Y, et al. Effects of RAGE-Specific Inhibitor FPS-ZM1 on Amyloid-β Metabolism and AGEs-Induced Inflammation and Oxidative Stress in Rat Hippocampus. Neurochem Res. 2016 May;41(5):1192-9. 3. Lian YJ, et al. Ds-HMGB1 and fr-HMGB induce depressive behavior through neuroinflammation in contrast to nonoxid-HMGB1. Brain Behav Immun. 2017 Jan;59:322-332. |
溶解性: |
DMSO : 100 mg/mL (305.02 mM; Need ultrasonic) H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble) |
保存条件: |
2-8℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.05 ml |
15.251 ml |
30.502 ml |
5 mM |
0.61 ml |
3.05 ml |
6.1 ml |
10 mM |
0.305 ml |
1.525 ml |
3.05 ml |
50 mM |
0.061 ml |
0.305 ml |
0.61 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。 |