THK5351

Research use only, not for human use.

THK5351 is a tracer involved in PET imaging for electron emission tomography imaging of Alzheimer's disease and cognitive impairment.

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

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. The THK5351 binding amount correlates with the amount of tau deposits in tissue.

THK5351 exhibits favorable pharmacokinetics and no defluorination in mice. 18F-THK5351 enters the brain immediately after intravenous injection and showsa 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. Autoradiography in the brain sections of patients with PSP demonstrates [3H]THK-5351 binding to tau deposits with a high selectivity. Although patients with PSP exhibits no remarkable [18F]THK-5351 retention in the temporal cortex, significantly higher tracer retention is observed in the globus pallidus and midbrain.

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Others

Other Targets

Others

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1707147-26-9

327.35

C18H18FN3O2

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (152.74 mM; Ultrasonic )

CNc1ccc(cn1)-c1ccc2cc(OC[C@H](O)CF)ccc2n1

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(-20℃)

With Ice Pack

≥ 2 years