CAS NO: | 1707147-26-9 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
生物活性 | THK5351 can be radiolabeled and used as a radiotracer forin vivoimaging oftaupathology in the brain. | ||||||||||||||||
体外研究 (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]. | ||||||||||||||||
体内研究 (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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 327.35 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C18H18FN3O2 | ||||||||||||||||
CAS 号 | 1707147-26-9 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 50 mg/mL(152.74 mM;Need ultrasonic) 配制储备液
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以下溶剂前显示的百
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