THK5351
Names
[ CAS No. ]:
1707147-26-9
[ Name ]:
THK5351
[Synonym ]:
(2S)-1-Fluoro-3-({2-[6-(methylamino)-3-pyridinyl]-6-quinolinyl}oxy)-2-propanol
2-Propanol, 1-fluoro-3-[[2-[6-(methylamino)-3-pyridinyl]-6-quinolinyl]oxy]-, (2S)-
Biological Activity
[Description]:
THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.
[Related Catalog]:
[In Vitro]
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[1].
[In Vivo]
THK5351 exhibits favorable pharmacokinetics and no defluorination in mice. 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]. 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[2].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Density]:
1.3±0.1 g/cm3
[ Boiling Point ]:
561.5±50.0 °C at 760 mmHg
[ Molecular Formula ]:
C18H18FN3O2
[ Molecular Weight ]:
327.353
[ Flash Point ]:
293.4±30.1 °C
[ Exact Mass ]:
327.138306
[ LogP ]:
2.65
[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C
[ Index of Refraction ]:
1.642
[ Storage condition ]:
-20℃