产品描述: | T807 a novel tau positron emission tomography (PET) tracer. |
靶点: |
Tau Protein;MicrotubuleAssociated |
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). In vitro autoradiography results show that [18F]T807 exhibits strong binding to PHF-tau positive human brain sections (Kd=14.6 nM). A comparison of autoradiography and double immunohistochemical staining of PHF-tau and Ab on adjacent sections demonstrates that [18F]T807 binding colocalizes with immunoreactive PHF-tau pathology, but does not highlight Ab plaques. [18F]T807 strongly binds to tau lesions primarily made of paired helical filaments in Alzheimer’s brains e.g. intra and extraneuronal tangles and dystrophic neurites. [18F]T807 off-target binding to neuromelanin- and melanin-containing cells and, to a lesser extent, to brain hemorrhagic lesions is identified |
体内研究: |
[18F]T807 is able to cross the blood–brain barrier and ished out quickly in mice model. [18F]T807 clears rapidly from the brain, with activity values decreasing from 4.43% ID/g at 5 minutes to 0.62% ID/g at 30 minutes. Kidney elimination is a significant clearance pathway, resulting in a maximum tracer concentration of 14.99% ID/g in the kidneys at 5 minutes, which decreases to 5.52% ID/g at 30 minutes. The accumulation of activity in muscle and bone remain relatively low throughout the PET scan |
参考文献: |
1. Xia CF, et al. [(18)F]T807, a novel tau positron emission tomography imaging agent for Alzheimer's disease. Alzheimers Dement. 2013 Nov;9(6):666-76. 2. Marquié M, et al. Validating novel tau positron emission tomography tracer [F-18]-AV-1451 (T807) on postmortem brain tissue. Ann Neurol. 2015 Nov;78(5):787-800. |
溶解性: |
soluble in DMSO |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
3.798 ml |
18.992 ml |
37.984 ml |
5 mM |
0.76 ml |
3.798 ml |
7.597 ml |
10 mM |
0.38 ml |
1.899 ml |
3.798 ml |
50 mM |
0.076 ml |
0.38 ml |
0.76 ml |
|
注意: |
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