Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
One important neuropathological substrate that plays a key role in the pathophysiology of neurodegenerative diseases like Alzheimer's disease (AD) is aggregated tau protein. 18F-THK5351 exhibits a high degree of affinity (Kd=2.9 nM; maximum number of binding sites = 368.3 pmol/g tissue) for Alzheimer's disease hippocampus homogenate. It quickly separates from the white matter tissue. The quantity of tau deposition in tissues is correlated with the amount of THK5351 bound [1].
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ln Vivo |
In mice, THK5351 shows no defluorination and good pharmacokinetics. 18F-THK5351 is injected intravenously, enters the brain right away, and leaves the brain quickly. No animals died at doses of 0.1 or 1 mg/kg, and clinical observation, body weight measurements, and pathological examinations did not reveal any treatment-related changes in any of the animals [1]. PSP patients' brain sections autoradiographically reveal that [3H]THK-5351 binds to tau deposits with extreme selectivity. PSP patients had significantly higher tracer retention in the globus pallidus and midbrain [2], despite not exhibiting significant [18F]THK-5351 retention in the temporal cortex.
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References |
[1]. Harada R, 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]. Ishiki A, et al. Tau imaging with [18 F]THK-5351 in progressive supranuclear palsy. Eur J Neurol. 2017 Jan;24(1):130-136. |
Molecular Formula |
C18H18FN3O2
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Molecular Weight |
327.352827548981
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CAS # |
1707147-26-9
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Related CAS # |
THK5351 (R enantiomer);2101218-44-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O[C@@H](COC1=CC=C2N=C(C3=CC=C(NC)N=C3)C=CC2=C1)CF
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : ~50 mg/mL (~152.74 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.64 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.0548 mL | 15.2742 mL | 30.5483 mL | |
5 mM | 0.6110 mL | 3.0548 mL | 6.1097 mL | |
10 mM | 0.3055 mL | 1.5274 mL | 3.0548 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.