2-(4-Aminophenyl)quinoline

BF-170 is a selective tau fibril binding agent with an EC50 of 221 nM. It exhibits good blood-brain barrier permeability, and after intravenous injection in mice, the concentration in brain tissue reaches 9.1% ID/g within 2 minutes (with a brain clearance rate of 0.25% ID/g after 30 minutes). BF-170 can be used as a probe for tau protein pathology imaging in Alzheimer's disease (AD). It plays an important role in early-stage AD research and holds potential for imaging studies of tau-related neurodegenerative diseases[1].

BF-170 is a new probe for neurofibrillary tangles (tau fibrils). It exhibits greater binding affinity to tau than to Aβ fibrils, EC50 = 221 nM vs. EC50 = 786 nM (Ki for Aβ > 5,000 nM). BF-170 demonstrates fast clearance from the brain; clearly visualizes neurofibrillary tangles, neuropil threads, and paired helical filament-type neuritis. BF-70 may become one of the candidate compounds for in vivo imaging of tau pathology associated with Alzheimerμs disease and is a useful tool in distinguishing among tau and Aβ fibrils specifically in AD.

[1] Okamura N, et al. Quinoline and benzimidazole derivatives: candidate probes for in vivo imaging of tau pathology in Alzheimer's disease. J Neurosci. 2005 Nov 23;25(47):10857-62. DOI:10.1523/JNEUROSCI.1738-05.2005