T807
Based on 2 publication(s) in Google Scholar
T807 a novel tau positron emission tomography (PET) tracer.
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- Pureté: 99.21%
- CAS No.: 1415379-56-4
- Formule: C16H10FN3
- Masse moléculaire:263.27
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
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Publications Citing Use of MedChemExpress (MCE) T807
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Activité biologique
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1415379-56-4
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Appearance Solid
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Masse moléculaire 263.27
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Formule C16H10FN3
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Color Off-white to yellow
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SMILES
FC1=CC=C(C2=CC3=C(C=C2)C(C=NC=C4)=C4N3)C=N1
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Synonyms
AV-1451
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Mol Psychiatry
Thy1-ApoE4/C/EBPβ double transgenic mice act as a sporadic model with Alzheimer's disease. [Abstract]2024 Oct;29(10):3040-3055. PMID: 38658772 -
Elife
Targeted degradation of aberrant tau in frontotemporal dementia patient-derived neuronal cell models. [Abstract]2019 Mar 25:8:e45457. PMID: 30907729
Solvant et solubilité
DMSO : ≥ 16.6 mg/mL (63.05 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1.25 mg/mL (4.75 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (277 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.7984 mL | 18.9919 mL | 37.9838 mL | 94.9596 mL |
| 5 mM | 0.7597 mL | 3.7984 mL | 7.5968 mL | 18.9919 mL | |
| 10 mM | 0.3798 mL | 1.8992 mL | 3.7984 mL | 9.4960 mL | |
| 15 mM | 0.2532 mL | 1.2661 mL | 2.5323 mL | 6.3306 mL | |
| 20 mM | 0.1899 mL | 0.9496 mL | 1.8992 mL | 4.7480 mL | |
| 25 mM | 0.1519 mL | 0.7597 mL | 1.5194 mL | 3.7984 mL | |
| 30 mM | 0.1266 mL | 0.6331 mL | 1.2661 mL | 3.1653 mL | |
| 40 mM | 0.0950 mL | 0.4748 mL | 0.9496 mL | 2.3740 mL | |
| 50 mM | 0.0760 mL | 0.3798 mL | 0.7597 mL | 1.8992 mL | |
| 60 mM | 0.0633 mL | 0.3165 mL | 0.6331 mL | 1.5827 mL |
T807 Related Classifications
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