COMT-IN-1
COMT-IN-1 (compound C12), a nitrophenolic analogue, is an orally active dopamine metabolic enzyme catechol-O-methyltransferase (COMT) inhibitor with IC50s of 0.37 μM, 95.58 μM and 58.82 μM for COMT, MAO-A and MAO-B, respectively. COMT-IN-1 exhibits chelation with a variety of metal ions. COMT-IN-1 exhibits good BBB permeability. COMT-IN-1 improves dopamine levels and ameliorates MPTP (HY-15608)-induced Parkinson's disease (PD) symptoms in mice.
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- CAS. Nr.: 2987884-27-3
- Formel: C24H18FN3O6
- Molecular Weight:463.41
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
COMT 0.37 μM (IC50) |
MAO-A 95.58 μM (IC50) |
MAO-B 58.82 μM (IC50) |
Chemical Information
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CAS. Nr. 2987884-27-3
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Molecular Weight 463.41
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Formel C24H18FN3O6
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SMILES
OC1=C([N+]([O-])=O)C=C(/C=C(C(NCC2=CC=C(OCC3=CC=CC(F)=C3)C=C2)=O)\C#N)C=C1O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Human pluripotent stem cell midbrain dopaminergic neuron differentiation
Human pluripotent stem cells are directed toward midbrain dopaminergic neurons by first inducing a neural floor-plate-like progenitor state, then patterning cells with ventralizing SHH signaling and midbrain/WNT-FGF cues, and finally maturing progenitors into neurons expressing dopaminergic markers such as TH, NURR1/NR4A2, PITX3, DAT/SLC6A3, VMAT2/SLC18A2, GIRK2/KCNJ6, FOXA2, LMX1A, and EN1. The main readouts are loss of pluripotency, acquisition of FOXA2+/LMX1A+ midbrain floor-plate progenitors, emergence of βIII-tubulin+/MAP2+ neurons, and production of TH+ dopaminergic neurons with molecular, dopamine-release, and electrophysiological features of midbrain dopaminergic identity.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)