THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of brain tau pathology.

Aggregated tau protein is a major neuropathological substrate central to the pathophysiology of neurodegenerative diseases such as Alzheimer's disease (AD). 18F-THK5351 binds to Alzheimer disease hippocampal homogenates with high affinity (Kd=2.9 nM; maximum number of binding sites=368.3 pmol/g tissue). It has fast dissociation from white-matter tissue. In tissue, The THK5351 binding amount correlates with the amount of tau deposits [1].

In mice,THK5351 exhibits favorable pharmacokinetics and no defluorination . 18F-THK5351 enters the brain immediately after intravenous injection and shows a fast washout from the brain. At 0.1 and 1 mg/kg, no animals died and no treatment-related changes in any animal are noted in clinical observations, body weight measurement, and pathologic examination[1]. [3H]THK-5351 binding to tau deposits with a high selectivity. in the temporal cortex, Although patients with PSP exhibits no remarkable [18F]THK-5351 retention, significantly higher tracer retention is observed in the globus pallidus and midbrain[2].

1707147-26-9

C18H18FN3O2

327.35

DMSO:50 mg/mL (152.74 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years