CP-283097
CP-283097 is an orally active and conformationally restricted and NR2B subtype-selective NMDA antagonist. CP-283097 efficiently competitively inhibits the binding of [³H]CP-101,606 to the rat meninges, with an IC50 value of 18 nM. CP-283097 exhibits nearly complete inhibition of the current mediated by the NR2B receptor (IC50 = 206 nM), while the inhibitory effect on the NR2A or NR2C receptors is very weak. CP-283097 demonstrates excellent central nervous system permeability and in vivo efficacy in animal models. CP-283097 can be used for neurological diseases related to excessive activation of NMDA receptors.
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- CAS. Nr.: 138047-56-0
- Formel: C21H25NO4
- Molecular Weight:355.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
CP-283097 exhibits an IC50 of 4 nM for inhibiting the toxicity of glutamate-induced hippocampal neurons[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
CP-283097 (1-15 mg/kg, i.v., single dose) inhibits the expression of c-Fos induced by NMDA with and ED50 of 4 mg/kg in mice[1].
CP-283097 (0.2-2 mg/kg, i.v., single dose) exhibits efficacy in inhibiting electrically induced cortical spreading depression (CSD) in the rat[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Cortical spreading depression model established in rats[1]
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Dosage:0.2, 0.6 and 2 mg/kg bolus + 0.2, 0.6 and 2 mg/kg infusion
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Administration:Intravenous injection (i.v.), single dose
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Result:Dose-dependently inhibited CSD propagation.
Chemical Information
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CAS. Nr. 138047-56-0
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Molecular Weight 355.43
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Formel C21H25NO4
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SMILES
O[C@@H]1[C@H](N2CCC(O)(CC2)CC3=CC=CC=C3)COC4=CC(O)=CC=C41
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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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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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)