PE154

PE154 is a fluorescent probe that binds to Aβ plaques, as well as a potent fluorescent inhibitor of AChE and BChE, with an IC₅₀ of 280 pM against hAChE and 16 nM against hBChE. PE154 is applicable for histochemical detection of Aβ plaques in mouse and human brain tissues. PE154 can be used in research related to Alzheimer's disease^[1][2][3]. In Vitro:PE154 reversibly binds to human acetylcholinesterase through active site cation-π stacking and interactions with the peripheral anionic site; its binding to human butyrylcholinesterase relies on active site cation-π stacking, with reduced effects on the peripheral site^[2][3].
PE154 binds to the β-sheet structure of Aβ plaques independently of cholinesterase binding, exhibits enhanced fluorescence upon binding to cholinesterase, and can target Aβ deposits in the hippocampus when delivered via nanoparticle carriers^[2][3].
PE154 (20 nM; 300 s) causes a significant increase in fluorescence intensity upon binding to purified recombinant human acetylcholinesterase and human butyrylcholinesterase, but this phenomenon is not observed when it binds to bovine serum albumin^[3]. In Vivo:PE154 (2 μL (0.1 mg/mL); stereotaxic injection into dorsal hippocampus; single dose) selectively targets hippocampal β-amyloid plaques in aged triple-transgenic Alzheimer's disease model mice in vivo, with approximately 80% of rostral hippocampal Aβ plaques labelled as early as 4 hours post-intrahippocampal injection and labelling persisting for up to 7 days^[2].