THK5351 |
Catalog No.GC30814
One-Click Copy Product Info
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THK5351, after being radiolabeled, is a positron emission tomography (PET) tau protein imaging tracer.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1707147-26-9
Sample solution is provided at 25 µL, 10mM.
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THK5351, after being radiolabeled, is a positron emission tomography (PET) tau protein imaging tracer. THK5351 visualizes tau protein pathology in the brain by binding to the β-sheet structure of tau protein in neurofibrillary tangles[1-4].
References:
[1] Brendel M, Wagner L, Levin J, et al. Perfusion-Phase [18F]THK5351 Tau-PET Imaging as a Surrogate Marker for Neurodegeneration. J Alzheimers Dis Rep. 2017 Sep 28;1(1):109-113.
[2] Kang JM, Lee SY, Seo S, et al. Tau positron emission tomography using [18F]THK5351 and cerebral glucose hypometabolism in Alzheimer's disease. Neurobiol Aging. 2017 Nov;59:210-219.
[3] Kikuchi A, Okamura N, Hasegawa T, et al. In vivo visualization of tau deposits in corticobasal syndrome by 18F-THK5351 PET. Neurology. 2016 Nov 29;87(22):2309-2316.
[4] Harada R, Ishiki A, Kai H, Sato N, et al. Correlations of 18F-THK5351 PET with Postmortem Burden of Tau and Astrogliosis in Alzheimer Disease. J Nucl Med. 2018 Apr;59(4):671-674.
Radiochemistry and Clinical PET Imaging Methods for 18F-THK5351[1-2]
This protocol is adapted from research data and provided for reference only. Adjustments may be necessary based on specific experimental requirements.
1. Radiochemical Synthesis of 18F-THK5351 from THK535:
(1) The target water containing fluorine-18 (18F-), produced by a cyclotron, is passed through a Sep-Pak Light Accell Plus QMA cartridge. The 18F- is captured on the cartridge. It is then eluted into a reaction vial using a Kryptofix solution. The eluate is mixed with acetonitrile, and water is removed by azeotropic distillation to obtain a dry 18F-/Kryptofix 222/K₂CO₃ complex.
(2) THK5352 (3mg, 5.3μmol) dissolved in 0.7mL of DMSO is added to the dry reaction vial. The mixture is stirred at 110°C for 10 minutes. Then, 0.2mL of 2mol/L aqueous HCl is added, and stirring continues at 110°C for another 3 minutes. Subsequently, 1mL of 0.8mol/L aqueous AcOK and 7mL of distilled water are added to quench the reaction.
(3) The product is eluted from a C18 cartridge using 60% ethanol. The ethanolic eluate is mixed with water and then purified by semi-preparative HPLC. Chromatographic conditions: Inertsil ODS-4 column, mobile phase: 20mmol/L NaH₂PO₄ / acetonitrile (75/25, v/v), flow rate: 5.0mL/min. The HPLC fraction corresponding to 18F-THK5351 is collected.
2. PET Imaging Procedure: Intravenously inject a dose of 185MBq of 18F-THK5351. Perform a dynamic PET scan using a PET scanner for 90 minutes. Reconstruct the PET images and calculate standardized uptake value (SUV) images. Co-register the individual's T1-weighted MRI image with the early (0-10 minutes post-injection) PET image. Spatially normalize the co-registered MR and PET images to a template in Talairach space. Manually or semi-automatically place regions of interest (ROIs) on the normalized images. Calculate the ratio of the SUV in each ROI to the SUV in the cerebellar cortex (SUVR) as an index of tracer retention.
Precautions:
(1) Operators must strictly adhere to radiation protection regulations, wear appropriate protective equipment, and perform the final sterile filtration and dispensing of the product under aseptic conditions.
References:
[1] Harada R, Okamura N, Furumoto S, et al. 18F-THK5351: A Novel PET Radiotracer for Imaging Neurofibrillary Pathology in Alzheimer Disease. J Nucl Med. 2016 Feb;57(2):208-14.
[2] Okamura N, Furumoto S, Harada R, et al. Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease. J Nucl Med. 2013 Aug;54(8):1420-7.
| Cas No. | 1707147-26-9 | SDF | |
| Canonical SMILES | O[C@@H](COC1=CC=C2N=C(C3=CC=C(NC)N=C3)C=CC2=C1)CF | ||
| Formula | C18H18FN3O2 | M.Wt | 327.35 |
| Solubility | DMSO : 50 mg/mL (152.74 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.0548 mL | 15.2742 mL | 30.5483 mL |
| 5 mM | 611 μL | 3.0548 mL | 6.1097 mL |
| 10 mM | 305.5 μL | 1.5274 mL | 3.0548 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)