EST64454 maleate
EST64454 maleate is a highly soluble σ1 receptor antagonist, demonstrating potent antinociceptive properties for pain treatment. EST64454 maleate exhibits excellent metabolic stability across various species and possesses an adequate pharmacokinetic profile in rodents. EST64454 maleate has been identified as a promising clinical candidate due to its favorable aqueous solubility and high permeability in Caco-2 cells.
For research use only. We do not sell to patients.
- CAS No.: 2088272-67-5
- Formula: C22H26F2N4O6
- Molecular Weight:480.46
-
Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Sigma Receptor Isoforms
More
Biological Activity
Description
Chemical Information
-
CAS No. 2088272-67-5
-
Molecular Weight 480.46
-
Formula C22H26F2N4O6
-
SMILES
OC(/C=C\C(O)=O)=O.CC(N(CC1)CCN1CCOCC2=NN(C3=CC(F)=C(C=C3)F)C=C2)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
-
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)