T807

T807 is a tau-binding agent. It selectively binds to recombinant tau (Kd = 0. and 16. 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. and 21 nM, respectively). T807 binds to native tau fibrils from patients with Alzheimer's disease or progressive supranuclear palsy (PSP, Kds = 0. 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. and 52. 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.InChI: InChI=1S/C16H10FN3/c17-16-4-2-11(8-19-16)10-1-3-12-13-9-18-6-5-14(13)20-15(12)7-10/h1-9,20H InChIKey: GETAAWDSFUCLBS-UHFFFAOYSA-N SMILES: FC1=CC=C(C=N1)C2=CC=C3C(NC4=CC=NC=C43)=C2