T807 a noveltaupositron emission tomography (PET) tracer.

Aggregated tau protein is a major neuropathological substrate central to the pathophysiology of neurodegenerative diseases such as Alzheimer's disease (AD).In vitroautoradiography results show that [¹⁸F]T807 exhibits strong binding to PHF-tau positive human brain sections (K_d=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^[1]. [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^[2].

[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^[1].

263.27

Solid

C₁₆H₁₀FN₃

1415379-56-4

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 16.6 mg/mL(63.05 mM)

*"≥" means soluble, but saturation unknown.

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• 1.

  请依序添加每种溶剂： 10% DMSO    40%PEG300   5%Tween-80   45% saline

  Solubility: 1.25 mg/mL (4.75 mM); Suspended solution; Need ultrasonic

  此方案可获得 1.25 mg/mL (4.75 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

  以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 1.25 mg/mL (4.75 mM); Clear solution

  此方案可获得 ≥ 1.25 mg/mL (4.75 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。