2. Neuronal Signaling Membrane Transporter/Ion Channel Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. iGluR NO Synthase Apoptosis Reactive Oxygen Species (ROS)
  4. PSD-95/nNOS PPI-IN-1

PSD-95/nNOS PPI-IN-1 是一种靶向 PSD-95/nNOS 相互作用的抑制剂，具有潜在的血脑屏障通透性。PSD-95/nNOS PPI-IN-1 以高亲和力结合 PSD-95 PDZ2 结构域 (Ki = 19.45 μM)。PSD-95/nNOS PPI-IN-1 通过降低细胞内 ROS 水平并抑制凋亡 (apoptosis)，抑制谷氨酸诱导的兴奋性毒性。PSD-95/nNOS PPI-IN-1 在大鼠 tMCAO 模型中显著降低脑梗死体积。PSD-95/nNOS PPI-IN-1 可用于急性缺血性脑卒中的研究。

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PSD-95/nNOS PPI-IN-1

PSD-95/nNOS PPI-IN-1 Chemical Structure

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PSD-95/nNOS PPI-IN-1 相关抗体

Top Publications Citing Use of Products

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AMPA Receptor NMDA Receptor Kainate Receptor

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nNOS iNOS eNOS

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke[1].

体外研究
(In Vitro)

PSD-95/nNOS PPI-IN-1 (Compound 32-2) (0.1-10 μM, 预处理 2 小时) 在谷氨酸损伤的 HT22 细胞中显著提高细胞活力[1].
PSD-95/nNOS PPI-IN-1 (10-20 μM, 预处理 2 小时) 在谷氨酸损伤的原代皮层神经元（培养 9 天）中显著增强细胞活力[1].
PSD-95/nNOS PPI-IN-1 (10 μM, 预处理 2 小时) 在 HT22 细胞中显著降低谷氨酸诱导的细胞内 ROS 水平[1].
PSD-95/nNOS PPI-IN-1 (10 μM, 预处理 2 小时) 在谷氨酸处理的 HT22 细胞中显著上调 Bcl-2 蛋白表达，并下调 Bax 和 cleaved-caspase 3 蛋白表达[1].

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

PSD-95/nNOS PPI-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HT22 cells treated with glutamate
Concentration: 10 μM
Incubation Time: 2 h pretreatment
Result: Upregulated Bcl-2 protein expression and downregulated Bax and Cleaved-caspase 3 protein expressions.
体内研究
(In Vivo)

PSD-95/nNOS PPI-IN-1（Compound 32-2) (8 mg/kg，静脉注射，于再灌注后 2 小时给药一次) 可显著减少 SD 大鼠的脑梗死体积[1]。

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

Animal Model: Male SD rats (220-280 g) underwent transient middle cerebral artery occlusion (tMCAO) by inserting a 4/0 nylon monofilament via the external carotid artery to occlude the middle cerebral artery for 1.5 h, followed by reperfusion[1]
Dosage: 8 mg/kg
Administration: i.v., once at 2 h post-reperfusion
Result: Achieved a significant reduction in cerebral infarct volume from 32.64% (model group) to 25.28%.
Showed neuroprotective effect in reducing cerebral infarct volume.
分子量

655.76

Formula

C32H41N5O8S
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

PSD-95/nNOS PPI-IN-1 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

PSD-95/nNOS PPI-IN-1iGluRNO SynthaseApoptosisReactive Oxygen Species (ROS)Ionotropic glutamate receptorsNitric oxide synthasesNOSacute ischemic strokePSD-95/nNOSROSHT22 cellsprimary cortical neuronsInhibitorinhibitorinhibit

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