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.
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- 分子式: C29H28N4O2
- 分子量:464.56
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
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.
化学情報
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分子量 464.56
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
NFI23 関連分類
HY-182068 関連分類
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