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

NFI23 是一种 GluN2B-NMDAR 抑制剂，其对 GluN2B-NMDAR 的 IC50 为 1.31 μM、Ki 为 5.98 nM，可透过血脑屏障。NFI23 结合于 GluN2B-NMDAR 的 ifenprodil 结合位点，可减少 NMDA 诱导的 Ca2+ 内流与活性氧 (ROS) 生成，维持线粒体膜电位，抑制神经元凋亡，并恢复 p-ERK1/2 的表达。NFI23 对 NMDA 诱导的细胞毒性及大鼠大脑中动脉闭塞 (MCAO) 模型具有神经保护作用。NFI23 可用于缺血性脑卒中的研究。

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NFI23

NFI23 Chemical Structure

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NFI23 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

NFI23 (0.05-5 μM; 6 h pretreatment) 可强效保护 PC12 细胞免受 NMDA 诱导的细胞毒性，在 0.05 μM、0.5 μM 和 5 μM 浓度下细胞存活率分别达到 81.2%、86.1%和 90.2[1]。
NFI23 (5 μM; 6 h pretreatment) 可抑制 NMDA 诱导的 PC12 细胞内钙超载[1]。
NFI23 可抑制 PC12 细胞中 NMDA 诱导的活性氧 (ROS) 过度生成[1]。
NFI23 可维持线粒体膜电位，并在 PC12 细胞中拮抗 NMDA 诱导的线粒体功能障碍[1]。
NFI23 可显著抑制 NMDA 诱导的 PC12 细胞凋亡[1]。
NFI23 (0.05-5 μM; 6 h pretreatment) 以浓度依赖的方式恢复经 NMDA 处理的 PC12 细胞中 p-ERK1/2 的表达，在 0.5 μM 和 5 μM 时效果显著[1]。
NFI23 (0.3-30 μM) 对 hERG 通道的抑制作用可忽略不计，其 IC50 超过 30 μM[1]。
NFI23 对 GluN2B-NMDAR 具有高结合亲和力，其 Ki 值为 5.98 nM[1]。
NFI23 对 GluN2B-NMDAR 的选择性远高于 σ1 (选择性≥1600 倍) 和 σ2 (选择性约 40 倍) 受体[1]。
NFI23 (0.1-30 μM; 10-15 s per concentration) 可强效抑制 GluN1/GluN2B 受体介导的电流，其 IC50 为 1.31 μM，且对 GluN1/GluN2A、GluN1/GluN2C 和 GluN1/GluN2D 受体具有高选择性[1]。
NFI23 (1 μM; 0-120 min at 37°C) 具有良好的血浆稳定性，半衰期为 57.8 h[1]。
NFI23 (up to 10 μM) 具有较低的临床相关药物-药物相互作用风险，其针对 CYP450 同工酶的 IC50 值均高于 10 μM[1]。

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

NFI23 相关抗体:

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.
药代动力学
(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
体内研究
(In Vivo)

NFI23 (静脉注射，再灌注时单次给药，剂量 2-10 mg/kg) 在大脑中动脉闭塞 (MCAO) 大鼠中发挥剂量依赖性神经保护作用，其中 10 mg/kg NFI23 对脑梗死体积的减小作用比 10 mg/kg Ifenprodil 更显著[1]。

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.
分子量

464.56

Formula

C29H28N4O2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

NFI23 相关分类

  • 摩尔计算器

  • 稀释计算器

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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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