THK5351

CAS No. 1707147-26-9

THK5351( —— )

Catalog No. M33147 CAS No. 1707147-26-9

THK5351 is a tracer involved in PET imaging for electron emission tomography imaging of Alzheimer's disease and cognitive impairment.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    THK5351
  • Note
    Research use only, not for human use.
  • Brief Description
    THK5351 is a tracer involved in PET imaging for electron emission tomography imaging of Alzheimer's disease and cognitive impairment.
  • Description
    THK5351 can be radiolabeled and used as a radiotracer for in vivo imaging of tau pathology in the brain.
  • In Vitro
    Aggregated tau protein is a major neuropathological substrate central to the pathophysiology of neurodegenerative diseases such as Alzheimer's disease (AD). 18F-THK5351 binds to Alzheimer disease hippocampal homogenates with high affinity (Kd=2.9 nM; maximum number of binding sites=368.3 pmol/g tissue). It has fast dissociation from white-matter tissue. The THK5351 binding amount correlates with the amount of tau deposits in tissue.
  • In Vivo
    THK5351 exhibits favorable pharmacokinetics and no defluorination in mice. 18F-THK5351 enters the brain immediately after intravenous injection and showsa fast washout from the brain. At 0.1 and 1 mg/kg, no animals died and no treatment-related changes in any animal are noted in clinical observations, body weight measurement, and pathologic examination. Autoradiography in the brain sections of patients with PSP demonstrates [3H]THK-5351 binding to tau deposits with a high selectivity. Although patients with PSP exhibits no remarkable [18F]THK-5351 retention in the temporal cortex, significantly higher tracer retention is observed in the globus pallidus and midbrain.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Others
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1707147-26-9
  • Formula Weight
    327.35
  • Molecular Formula
    C18H18FN3O2
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 50 mg/mL (152.74 mM; Ultrasonic )
  • SMILES
    CNc1ccc(cn1)-c1ccc2cc(OC[C@H](O)CF)ccc2n1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

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.?
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