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Cat. No.: HY-182068

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NFI23

NFI23 is a blood-brain barrier-penetrant GluN2B-NMDAR inhibitor, with an IC₅₀ of 1.31 μM and a K_i 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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화학식: C₂₉H₂₈N₄O₂
분자량:464.56

보관:

Please store the product under the recommended conditions in the Certificate of Analysis.

NFI23 Chemical Structure

Amount: USD 0.00

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- 제품 설명
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
순도&문서
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

제품 설명

All iGluR Isoforms :

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 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 K_i 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.

Cell Viability Assay^[1]

Cell Line:

PC12 cells
Concentration:

0.05, 0.5, 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, 0.5, 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	T_1/2	T_max	C_max	AUC_0-t	AUC_0-∞	V_z	CL	MRT_0-t	MRT_0-∞
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 (HY-12882)^[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.

Chemical Information

분자량 464.56
화학식 C₂₉H₂₈N₄O₂
SMILES

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

Room temperature in continental US; may vary elsewhere.
보관

Please store the product under the recommended conditions in the Certificate of Analysis.

순도&문서

Handling Instructions (2659 KB)

References

[1]. Zhang Z, et al. Discovery and Evaluation of N-Arylindole-Based GluN2B-NMDAR Antagonists with Reduced Cardiotoxicity for the Treatment of Ischemic Stroke. J Med Chem. 2026;69(6):7290-7312. [Content Brief]

Calculators

몰농도 계산기

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

농도 희석 계산기

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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Other size

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Amount: USD 0.00

Biological Activity
- 제품 설명
- In Vitro
- In Vivo
Chemical Information
순도&문서
References

상품명:
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수량:
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NFI23

All iGluR Isoforms