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THK-523 

Cat. No. M28618
THK-523  Structure
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Biological Activity

THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer. 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease.

Chemical Information
Molecular Weight 282.31
Formula C17H15FN2O
CAS Number 1573029-17-0
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Karoline T Neumann, et al. J Labelled Comp Radiopharm. Synthesis and selective 2 H-, 13 C-, and 15 N-labeling of the Tau protein binder THK-523

[2] Lisheng Cai, et al. ACS Chem Neurosci. Candidate PET Radioligand Development for Neurofibrillary Tangles: Two Distinct Radioligand Binding Sites Identified in Postmortem Alzheimer's Disease Brain

[3] Tetsuro Tago, et al. J Labelled Comp Radiopharm. Synthesis and preliminary evaluation of 2-arylhydroxyquinoline derivatives for tau imaging

[4] Nobuyuki Okamura, et al. J Nucl Med. Novel 18F-labeled arylquinoline derivatives for noninvasive imaging of tau pathology in Alzheimer disease

[5] Ryuichi Harada, et al. Eur J Nucl Med Mol Imaging. Comparison of the binding characteristics of [18F]THK-523 and other amyloid imaging tracers to Alzheimer's disease pathology

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