7-(6-Fluoropyridin-3-yl)-5H-pyrido[4,3-b]indole

Description

T807 is a tau-binding agent.1 It selectively binds to recombinant tau (Kd = 0.2 and 16.8 nM for high- and low-affinity tau binding sites) over 83 receptors, transporters, enzymes, and ion channels in a panel at 10 µM but does bind to monoamine oxidase A (MAO-A) and MAO-B (Kds = 1.6 and 21 nM, respectively). T807 binds to native tau fibrils from patients with Alzheimer’s disease or progressive supranuclear palsy (PSP; Kds = 0.3 nM for both for high-affinity tau binding sites; Kds = 30 and 70 nM, respectively, for low-affinity tau binding sites) but also binds to brain homogenates from patients without a tau-related disease (Kds = 0.6 and 52.5 nM for high- and low-affinity tau binding sites, respectively) due to its off-target binding to MAO-A and MAO-B. A radiolabeled form of T807, 18F-T807, has been used in the imaging of tau in animal models of tau pathology in vivo and in postmortem human brain tissue from patients with Alzheimer’s disease.2 WARNING This product is not for human or veterinary use.