BF-158

BF-158 (1 mM; 60 min) reduces [¹⁸F]T808 binding in NFT-enriched regions by 93% in human AD visual cortex slices, suggesting that it recognizes tau aggregation regions similar to those identified by T808^[1].
BF-158 (4 h) shows weak binding to synthetic Aβ_1-42 fibrils, with a K_i >5000 nM in the [¹²⁵I]BF-180 competitive binding assay^[2].
BF-158 (100 μM; 10 min) clearly stains NFTs and neuropil threads in AD hippocampal brain sections and predominantly labels PHF-type neurites consistent with tau immunostaining, whereas it shows only weak staining for amyloid plaques^[2].
BF-158 (100 μM; 10 min) no longer shows NFT staining in AD brain sections pretreated with 90% formic acid for 5 min, supporting that it recognizes the β-sheet structure of NFTs rather than monomeric tau^[2].
BF-158 (100 μM; 10 min) does not detect Pick bodies in Pick's disease brain sections^[2].
BF-158 (100 μM; 10 min) shows no detectable globose tangles and glial pathology in PSP brain sections^[2].

In fluorescence assays, BF-158 (0.01-10 μM) exhibits EC₅₀ values of 399 nM and 659 nM for tau fibrils and Aβ_1-42 fibrils, respectively, demonstrating a relatively higher binding preference for tau fibrils^[2].