bace1in1

BACE1-IN-1 is a high brain penetrant BACE1 inhibitor (IC50s: 32 and 47 nM for human BACE1 and BACE2).

AChE BChE BACE-1-IN-1 (Compound 4k) is an orally active inhibitor that targets acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and β-site amyloid precursor protein cleaving enzyme 1 (BACE-1). It displays IC50 values of 0.058 μM, 0.082 μM, and 0.115 μM against hAChE, hBChE, and hBACE-1, respectively. AChE BChE BACE-1-IN-1 exhibits significant binding affinity with PAS-AChE, excellent ability to cross the blood-brain barrier, potential disassembly of amyloid-beta (Aβ) aggregates, and neuroprotective properties against Aβ-induced stress. Moreover, AChE BChE BACE-1-IN-1 demonstrates remarkable antioxidant capabilities [1].

BACE1-IN-12 是能够透过血脑屏障的、有效的 BACE1 抑制剂 (IC50: 8.9 μM)。BACE1-IN-12 能够选择性的抑制 BuChE(丁基胆碱酯酶) 的活性 (IC50: 3.2 μM)。BACE1-IN-12 表现出较好的抗氧化活性，对 DPPH 的 IC50 值为 10.2 μM。BACE1-IN-12 具有潜力进行抗阿尔茨海默病的研究。

BACE1-IN-10为高效的BACE1抑制剂，对重组BACE1（rBACE1）显示出亚微摩尔级别的抑制活性。

BACE1-IN-13 (Compound 36)为一种BACE1抑制剂，展现出口服活性，IC50为2.9 nM。该化合物在hAβ42细胞中显示出强效 (IC50=1.3 nM)，证实了其心血管安全性，并在小鼠与狗的动物模型中有效降低Aβ42水平。