1374109-02-0

Basic information

• Product Name: THK-951
• Synonyms: THK-951
• CAS NO: 1374109-02-0
• Molecular Weight: 250.3
• Mol File: 1374109-02-0.mol

Chemical Properties

• CAS DataBase Reference: THK-951(CAS DataBase Reference)
• NIST Chemistry Reference: THK-951(1374109-02-0)
• EPA Substance Registry System: THK-951(1374109-02-0)

Safety Data

• Hazardous Substances Data: 1374109-02-0(Hazardous Substances Data)

Upstream product

• 1563178-42-6 C₂₂H₂₄N₂O₃ 
• 86045-69-4 4-methoxy-2-(trimethylacetamido)benzaldehyde 
• 1374109-01-9 C₂₅H₃₀N₂O₄ 
• 1374108-60-7 C₁₃H₁₄ClNO₂ 
• 375358-19-3 2-chloroquinoline-7-ol 
• 70500-72-0 quinoline-2,7-diol 

Downstream Products

• 1374107-49-9 2-(4-ethylmethylaminophenyl)-7-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy]quinoline 
• 1374107-51-3 2-(4-methylaminophenyl)-7-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy]quinoline 
• 1374107-52-4 2-(4-dimethylaminophenyl)-7-[[2-(tetrahydro-2H-pyran-2-yloxy)-3-tosyloxy]propoxy]quinoline 
• 1374109-04-2 C₃₄H₄₄N₂O₅SSi 
• 1374109-05-3 C₂₈H₃₀N₂O₅S 
• 1374109-07-5 C₃₄H₃₉F₃N₂O₆SSi 
• 1374109-08-6 C₂₈H₂₅F₃N₂O₆S 
• 1374109-09-7 C₃₃H₃₃F₃N₂O₇S 
• 1374109-06-4 C₁₈H₁₃F₃N₂O₂ 
• 1374109-03-1 C₁₈H₁₈N₂O 

Relevant articles and documents

Synthesis and preliminary evaluation of 2-arylhydroxyquinoline derivatives for tau imaging

Alzheimer's disease (AD) is the most common cause of dementia. Senile plaques, consisting of β-amyloid, and neurofibrillary tangles (NFTs), composed of tau protein, are representative pathological hallmarks of AD. It is believed that the accumulation of NFTs precedes the onset of clinical symptoms of AD and correlates with the progression of memory dysfunction. Thus, the use of noninvasive detection techniques including radiolabeled probes and positron emission tomography (PET) will facilitate early diagnosis or staging of AD. In this study, we synthesized and evaluated novel hydroxylated 2-arylquinoline derivatives as tau imaging PET probes. The binding affinities of compounds for tau were evaluated by fluorescent staining of the AD hippocampal section and a competitive binding assay using [18F]THK-523. THK-951 showed high binding affinity for tau pathology in an AD brain section and K18Δ280K fibrils (Ki = 20.7 nM); thus, we radiosynthesized a 11C-labeled THK-951 and further studied its potential as a tau PET probe. The [11C]THK-951 demonstrated excellent kinetics in a normal mouse brain (3.23% ID/g at 2 min postinjection and 0.15% ID/g at 30 min postinjection) and showed the labeling of NFTs in an AD brain section by autoradiography assay. These findings indicate the availability of [ 11C]THK-951 for in vivo PET imaging of tau pathology in AD. Copyright

TAU IMAGING PROBE

An object of the present invention is to provide a probe for imaging a β-sheet structure protein which can be used for the diagnosis of conformational diseases, particularly disease (tauopathy) having a cardinal symptom such as intracerebral accumulation of tau protein, for example, Alzheimer's disease. Another object of the present invention is to provide a compound which is highly specific to tau and can image tau with satisfactory sensitivity, and also has high brain transition, low or non-recognized bone-seeking properties and low or non-recognized toxicity. According to the present invention, the above problems are solved by providing a compound of a formula I (wherein A, R1, R2, R3, R4, R5, R6, Ra and Rb are as defined in the present description) or a pharmaceutically acceptable salt or solvate thereof.