2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. iGluR
  4. NFI23

NFI23 is a GluN2B-NMDAR inhibitor with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 can cross the blood-brain barrier. NFI23 binds to the ifenprodil binding site of GluN2B-NMDAR, reduces NMDA-induced Ca2+ influx and reactive oxygen species (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.

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NFI23

NFI23 Chemical Structure

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Description

NFI23 is a GluN2B-NMDAR inhibitor with an IC50 of 1.31 μM and a Ki of 5.98 nM against GluN2B-NMDAR. NFI23 can cross the blood-brain barrier. NFI23 binds to the ifenprodil binding site of GluN2B-NMDAR, reduces NMDA-induced Ca2+ influx and reactive oxygen species (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[1].

In Vitro

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 inhibits NMDA-induced excessive ROS generation in PC12 cells[1].
NFI23 preserves mitochondrial membrane potential and protects against NMDA-induced mitochondrial dysfunction in PC12 cells[1].
NFI23 significantly inhibits 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, with significant effects at 0.5 μM and 5 μM[1].
NFI23 (0.3-30 μM) exhibits negligible hERG channel inhibition, with an IC50 exceeding 30 μM[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].
NFI23 (1 μM; 0-120 min at 37°C) has favorable plasma stability with a half-life of 57.8 h[1].
NFI23 (up to 10 μM) has a low risk of clinically relevant drug-drug interactions, with IC50 values for CYP450 isoforms all above 10 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

NFI23 Related Antibodies

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 0.05-5 μM
Incubation Time: 6 h (pretreatment)
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.

Western Blot Analysis[1]

Cell Line: PC12 cells
Concentration: 0.05-5 μM
Incubation Time: 6 h (pretreatment)
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.
Parmacokinetics
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
In Vivo

NFI23 (2-10 mg/kg; i.v.; single dose at reperfusion) exerts dose-dependent neuroprotective effects in MCAO rats, with 10 mg/kg NFI23 providing a more pronounced reduction in cerebral infarct volume than 10 mg/kg Ifenprodil[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague-Dawley (SD) rats (weighing 200−220 g; middle cerebral artery occlusion model)[1]
Dosage: 2 mg/kg; 5 mg/kg; 10 mg/kg
Administration: i.v.; single dose at reperfusion
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.
Molecular Weight

464.56

Formula

C29H28N4O2
SMILES

O=C(NCCC1=CC=C(O)C=C1)CC2=CN(C3=CC=CC(CN4C=CN=C4C)=C3)C5=C2C=CC=C5
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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NFI23 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NFI23NFI 23NFI-23iGluRIonotropic glutamate receptorshERG channelGluN2B-NMDARCa2+ifenprodil siteblood-brain barriermitochondrial membrane potentialp-ERK1/2PC12 cellsROSneuronal apoptosisInhibitorinhibitorinhibit

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