Name | THK5351 |
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Synonyms |
(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)- |
Description | THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain. |
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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 |
Density | 1.3±0.1 g/cm3 |
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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℃ |