T807 (AV-1451)
(Synonyms: AV-1451) 目录号 : GC30789
T807 (AV-1451) 一种新型 tau 正电子发射断层扫描 (PET) 示踪剂。
Cas No.:1415379-56-4
Sample solution is provided at 25 µL, 10mM.
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T807 a novel tau positron 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 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[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].
[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.
Kinase experiment: | 10 mg/mL frozen brain homogenate aliquots are thawed and diluted 10-fold in binding buffer to 1 mg/mL. 500 μL of appropriate concentrations of non-radioactive T807 to be tested are combined with 400 μL of [3H] T807 (29.7 Ci/mmol) in a volume of 900 μL of binding buffer. The assay begins by addition of 100 μL of the 1 mg/mL brain homogenate to achieve a final concentration of 0.10 mg tissue/mL for radioligands. The final concentration of [3H] T807 is typically 1-2 nM. After incubation at room temperature for 60 minutes, the binding mixture is filtered and rapidly washed 5 times with 3 mL binding buffer. The filters are counted[2]. |
Animal experiment: | Mice: Six male mice at each time point are administered 250 mCi [18F]T807 (in 200 mL saline) via tail vein injection. At 5, 15, and 30 minutes after administration, the mice are anesthetized and 500-mL whole blood samples and centrifuged. After euthanasia, the liver, kidneys, skeletal muscle (right quadriceps), brain, and bone (femur) are harvested and weighed. Each of the tissue samples are transferred to gamma counter tubes and counted[1]. |
References: [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. | |
| Cas No. | 1415379-56-4 | SDF | |
| 别名 | AV-1451 | ||
| Canonical SMILES | FC1=CC=C(C2=CC3=C(C=C2)C(C=NC=C4)=C4N3)C=N1 | ||
| 分子式 | C16H10FN3 | 分子量 | 263.27 |
| 溶解度 | DMSO : ≥ 16.6 mg/mL (63.05 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.7984 mL | 18.9919 mL | 37.9838 mL |
| 5 mM | 0.7597 mL | 3.7984 mL | 7.5968 mL |
| 10 mM | 0.3798 mL | 1.8992 mL | 3.7984 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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