Identification | Back Directory | [Name]
THK5351 | [CAS]
1707147-26-9 | [Synonyms]
THK5351 THK5351?, >98%,>98%ee 2-Propanol, 1-fluoro-3-[[2-[6-(methylamino)-3-pyridinyl]-6-quinolinyl]oxy]-, (2S)- | [Molecular Formula]
C18H18FN3O2 | [MOL File]
1707147-26-9.mol | [Molecular Weight]
327.35 |
Chemical Properties | Back Directory | [Boiling point ]
561.5±50.0 °C(Predicted) | [density ]
1.283±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
12.82±0.20(Predicted) | [color ]
Light yellow to yellow |
Hazard Information | Back Directory | [Uses]
THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain. | [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]
[1] Harada R, et al. 18F-THK5351: A Novel PET Radiotracer for Imaging Neurofibrillary Pathology in Alzheimer Disease. J Nucl Med. 2016 Feb;57(2):208-14. DOI:10.2967/jnumed.115.164848 [2] Ishiki A, et al. Tau imaging with [18 F]THK-5351 in progressive supranuclear palsy. Eur J Neurol. 2017 Jan;24(1):130-136. DOI:10.1111/ene.13164 |
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BOC Sciences
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https://www.bocsci.com |
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