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MK-6240

a PET tracer for imaging neurofibrillary tangles; structure in first source

Also Known As:

6-(fluoro)-3-(1H-pyrrolo(2,3-c)pyridin-1-yl)isoquinolin-5-amine

Networked: 4 relevant articles (0 outcomes, 2 trials/studies)

Bio-Agent Context: Research Results

Heterocyclic Compounds: 198
- Fused-Ring Heterocyclic Compounds
  - 2-Ring Heterocyclic Compounds
    - Isoquinolines: 34
      - MK-6240: 4

Experts

1.	Bennacef, Idriss: 1 article (01/2020)
2.	Bormans, Guy: 1 article (01/2020)
3.	Briscoe, Richard J: 1 article (01/2020)
4.	Celen, Sofie: 1 article (01/2020)
5.	Declercq, Ruben: 1 article (01/2020)
6.	Ferry-Martin, Sandrine: 1 article (01/2020)
7.	Hostetler, Eric D: 1 article (01/2020)
8.	Koole, Michel: 1 article (01/2020)
9.	Laroque, Philippe: 1 article (01/2020)
10.	Lohith, Talakad G: 1 article (01/2020)

Related Diseases

1.	Melanoma (Melanoma, Malignant) 06/01/2019 - "In blocking studies with melanoma cells, compounds bearing multiple aromatic rings and an aminopyridine group, including tau ligands such as AV-1451, PBB3, and a lead compound of MK-6240, exhibited the inhibition of [18F]THK5351 binding comparable to self-blocking by THK5351 (> 70% at 10 µM). "
2.	Hemolysis 01/01/2020 - "MK-6240 was administered intravenously (IV) in a 7-day rat toxicity study at × 50, × 100, and × 1000 dose margins relative to projected highest clinical dose of 0.333 μg/kg. The IV formulation of MK-6240 for clinical use and the formulation used in the 7-day rat toxicity study was tested for hemolysis potential in human and Wistar rat whole blood. "
3.	Alzheimer Disease (Alzheimer's Disease) 11/01/2019 - "Our data indicate that MK-6240 strongly binds to neurofibrillary tangles in Alzheimer disease but does not seem to bind to a significant extent to tau aggregates in non-Alzheimer tauopathies, suggesting that it may have a limited utility for the in vivo detection of these pathologies. " 09/22/2023 - "Cryo-EM structure of Alzheimer's disease tau filaments with PET ligand MK-6240."
4.	Tauopathies 11/01/2019 - "Our data indicate that MK-6240 strongly binds to neurofibrillary tangles in Alzheimer disease but does not seem to bind to a significant extent to tau aggregates in non-Alzheimer tauopathies, suggesting that it may have a limited utility for the in vivo detection of these pathologies. "
5.	Hemorrhage 11/01/2019 - "In addition, we identified MK-6240 strong off-target binding to neuromelanin and melanin-containing cells, and some weaker binding to areas of hemorrhage. "

Related Drugs and Biologics

1.	Ligands
2.	Aminopyridines
3.	THK5351
4.	7- (6- fluoropyridin- 3- yl)- 5H- pyrido(4,3- b)indole
5.	Melanins (Melanin)
6.	neuromelanin