NFI23
NFI23 is a blood-brain barrier-penetrant GluN2B-NMDAR inhibitor, with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 reduces NMDA-induced Ca2+ influx and ROS production, maintains mitochondrial membrane potential, inhibits neuronal apoptosis, and restores the expression of p-ERK1/2. NFI23 exerts neuroprotective effects against NMDA-induced cytotoxicity and in the rat middle cerebral artery occlusion (MCAO) model. NFI23 can be used for the research of ischemic stroke.
For research use only. We do not sell to patients.
- Formula: C29H28N4O2
- Molecular Weight:464.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
NFI23 (0.05-5 μM; 6 h pretreatment) potently protects PC12 cells from NMDA-induced cytotoxicity, with cell viability reaching 81.2% at 0.05 μM, 86.1% at 0.5 μM, and 90.2% at 5 μM[1].
NFI23 (5 μM; 6 h pretreatment) inhibits NMDA-induced excessive calcium influx in PC12 cells[1].
NFI23 can inhibit NMDA-induced excessive production of reactive oxygen species (ROS) in PC12 cells; maintain mitochondrial membrane potential and antagonize NMDA-induced mitochondrial dysfunction in PC12 cells; and significantly inhibit NMDA-induced apoptosis in PC12 cells[1].
NFI23 (0.05-5 μM; 6 h pretreatment) restores p-ERK1/2 expression in a concentration-dependent manner in NMDA-treated PC12 cells[1].
NFI23 has high binding affinity for GluN2B-NMDAR, with a Ki of 5.98 nM[1].
NFI23 is highly selective for GluN2B-NMDAR over σ1 (≥1600-fold selectivity) and σ2 (~40-fold selectivity) receptors[1].
NFI23 (0.1-30 μM; 10-15 s per concentration) potently inhibits GluN1/GluN2B receptor-mediated currents with an IC50 of 1.31 μM, and shows high selectivity over GluN1/GluN2A, GluN1/GluN2C, and GluN1/GluN2D receptors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:PC12 cells
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Concentration:0.05, 0.5, 5 μM
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Incubation Time:6 h (pretreatment)
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Result:Increased PC12 cell viability to 81.2% at 0.05 μM.
Increased PC12 cell viability to 86.1% at 0.5 μM.
Increased PC12 cell viability to 90.2% at 5 μM.
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Cell Line:PC12 cells
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Concentration:0.05, 0.5, 5 μM
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Incubation Time:6 h (pretreatment)
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Result:Induced a concentration-dependent increase in p-ERK1/2 expression.
Showed no significant difference in p-ERK1/2 expression from the NMDA model at 0.05 μM.
Significantly increased p-ERK1/2 expression at 0.5 μM.
Significantly increased p-ERK1/2 expression at 5 μM.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUC0-t | AUC0-∞ | Vz | CL | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 2 mg/kg | i.v. | 2.54 h | 0.0833 h | 176 ng/mL | 163 ng·h/mL | 169 ng·h/mL | 42.66 L/kg | 12.05 L/h/kg | 0.97 h | 1.29 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (SD) rats (weighing 200-220 g; middle cerebral artery occlusion model)[1]
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Dosage:2 mg/kg; 5 mg/kg; 10 mg/kg
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Administration:i.v.; single dose at reperfusion
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Result:Failed to reduce cerebral ischemic area percentage significantly relative to the model group at 2 mg/kg.
Reduced cerebral ischemic area percentage and improved neurological scores significantly relative to the model group at 5 mg/kg.
Reduced cerebral ischemic area percentage to a greater degree than 10 mg/kg Ifenprodil and improved neurological scores significantly relative to the model group at 10 mg/kg, showing a dose-dependent therapeutic effect.
Chemical Information
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Molecular Weight 464.56
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Formula C29H28N4O2
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SMILES
O=C(NCCC1=CC=C(O)C=C1)CC2=CN(C3=CC=CC(CN4C=CN=C4C)=C3)C5=C2C=CC=C5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NFI23 Related Classifications
HY-182068 Related Classifications
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