| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
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Purity: ≥98%
| Targets |
PET tracer for tau protein
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|---|---|
| ln Vitro |
One important neuropathological substrate in the pathogenesis of neurodegenerative disorders like Alzheimer's disease (AD) is aggregated tau protein. Results from in vitro radiation self-healing demonstrate that PHF-tau positive human brain slices bind to [18F] T807 with a strong force (Kd=14.6nM). It was observed that [18F]T807 binding colocalized with immunoreactive PHF-tau pathology but did not highlight Ab plaques on antagonist sections when autoradiographic and double immunohistochemical staining of PHF-tau and Ab were compared [1]. [18F] T807 binds tightly to tau lesions, which are mainly made up of pairs of helical filaments and are found in the brains of Alzheimer's patients. These lesions include dystrophic neurites and neuronal outer tangles. In Arduino, [18F] T807 binds off-target to cells that contain melanophore and neuromelanin, as well as to cerebral thrombotic effects [2].
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| ln Vivo |
In mouse models, [18F] T807 can cross the blood-brain barrier and vanish quickly. With activity values ranging from 4.43% ID/g at 5 minutes to 0.62% ID/g at 30 minutes, [18F] T807 is rapidly eliminated from the brain. Elimination: Elimination is a crucial clearance process that causes the maximal concentration of tracer in the interference to drop to 5.52% ID/g after 30 minutes from 14.99% ID/g at the 5-minute mark. During a PET scan, the amount of activity that builds up in the bones and anatomy is comparatively minimal [1].
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| Enzyme Assay |
To screen potential tau binders, human AD brain sections were used as a source of native paired helical filament (PHF)-tau and Aβ rather than synthetic tau aggregates or Aβ fibrils generated in vitro to measure the affinity and selectivity of [(18)F]T807 to tau and Aβ. In vitro autoradiography results show that [(18)F]T807 exhibits strong binding to PHF-tau-positive human brain sections. A dissociation constant (Kd) of [(18)F]T807 (14.6 nM) was measured using brain sections from the frontal lobe of AD patients. A comparison of autoradiography and double immunohistochemical staining of PHF-tau and Aβ on adjacent sections demonstrated that [(18)F]T807 binding colocalized with immunoreactive PHF-tau pathology, but did not highlight Aβ plaques[1].
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| Cell Assay |
We applied [F-18]-AV-1451 phosphor screen autoradiography, [F-18]-AV-1451 nuclear emulsion autoradiography, and [H-3]-AV-1451 in vitro binding assays to the study of postmortem samples from patients with a definite pathological diagnosis of Alzheimer disease, frontotemporal lobar degeneration-tau, frontotemporal lobar degeneration-transactive response DNA binding protein 43 (TDP-43), progressive supranuclear palsy, corticobasal degeneration, dementia with Lewy bodies, multiple system atrophy, cerebral amyloid angiopathy and elderly controls free of pathology[2].
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| Animal Protocol |
In vivo studies in mice demonstrated that [(18)F]T807 was able to cross the blood-brain barrier and washed out quickly.
Conclusions: [(18)F]T807 demonstrates high affinity and selectivity to PHF-tau as well as favorable in vivo properties, making this a promising candidate as an imaging agent for AD.[2]
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| References | |
| Additional Infomation |
Flortaucipir is under investigation in clinical trial NCT03507257 (Longitudinal Early-onset Alzheimer's Disease Study Protocol).
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| Molecular Formula |
C₁₆H₁₀FN₃
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|---|---|
| Molecular Weight |
263.2691
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| Exact Mass |
263.086
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| Elemental Analysis |
C, 72.99; H, 3.83; F, 7.22; N, 15.96
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| CAS # |
1415379-56-4
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| PubChem CID |
71059746
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| Appearance |
Typically exists as off-white to yellow solids at room temperature
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| LogP |
3.917
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
20
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| Complexity |
351
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C([H])=C([H])C(=C([H])N=1)C1C([H])=C([H])C2C3C([H])=NC([H])=C([H])C=3N([H])C=2C=1[H]
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| InChi Key |
GETAAWDSFUCLBS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10FN3/c17-16-4-2-11(8-19-16)10-1-3-12-13-9-18-6-5-14(13)20-15(12)7-10/h1-9,20H
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| Chemical Name |
5H-Pyrido(4,3-b)indole, 7-(6-fluoro-3-pyridinyl)-
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| Synonyms |
AV-1451; AV 1451; AV1451; Flortaucipir;T-807; T807; T 807
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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 : ≥ 16.6 mg/mL (~63.05 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (4.75 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: ≥ 1.25 mg/mL (4.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
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