Potent somatostatin receptor 1 (sst1) agonist; displays selectivity for sst1 (IC50 values are 30.9 nM, 345 nM, > 1 μM, > 10 μM and > 10μM for human sst1, sst3, sst4, sst2 and sst5 respectively). Attenuates somatostatin release in the rat nucleus accumbens
tau Protein α-synuclein-IN-2 (Compound 14T) 是一种可以穿透血脑屏障的tau和α-syn抑制剂。tau Protein α-synuclein-IN-2 通过硫脲连接子结构以剂量依赖方式减少α-syn的寡聚。该化合物在生物传感器细胞中阻止tau聚集的种子效应,并在M17D神经母细胞瘤模型中显示出抗包涵体效应。此外,tau Protein α-synuclein-IN-2 能够抑制Aβ斑块的形成,展示了其在阿尔茨海默病和帕金森病研究中的潜力。
Amylin (AMY3) antagonist (IC50 = 0.3 μM). Protects neuronal cells from Aβ(1-42)-induced cytotoxicity in vitro. Brain penetrant. Improves spatial memory and reduces Aβ plaque number and total area in a mouse Alzheimer's disease model.