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We report herein the synthesis and application of a novel tetradentate ruthenium(II) complex 1 containing a tris(2-pyridylmethyl)amine (tpa) ligand as an inhibitor of β-amyloid fibrillogenesis. [Ru(tpa)(bt)]ClO4 1 (bt =2-acetylbenzo[b]thiophene-3-olate) showed significant inhibition of Aβ(1-40) peptide aggregation in vitro, which was confirmed by a Thioflavin T assay and transmission electron microscopy imaging.