产品
编 号：F205101
分子式：C18H18FN3O2
分子量：327.35
分子式：C18H18FN3O2
分子量：327.35
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
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1mg
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5mg
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10mg
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结构图
CAS No: 1707147-26-9
产品详情
生物活性：
THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.
体内研究：
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.
体外研究：
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 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.
体内研究：
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.
体外研究：
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.
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