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

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.

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PSD-95/nNOS PPI-IN-1

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

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Description

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].

In Vitro

PSD-95/nNOS PPI-IN-1 (Compound 32-2) (0.1-10 μM, 2 h pretreatment) significantly increases cell viability of HT22 cells injured by glutamate[1].
PSD-95/nNOS PPI-IN-1 (10-20 μM, 2 h pretreatment) significantly enhances cell viability of primary cortical neurons (cultured for 9 days) injured by glutamate[1].
PSD-95/nNOS PPI-IN-1 (10 μM, 2 h pretreatment) significantly reduces glutamate -induced intracellular ROS levels in HT22 cells[1].
PSD-95/nNOS PPI-IN-1 (10 μM, 2 h pretreatment) significantly upregulates Bcl-2 protein expression and downregulates Bax and cleaved-caspase 3 protein expressions in HT22 cells treated with glutamate[1].

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

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.
In Vivo

PSD-95/nNOS PPI-IN-1 (Compound 32-2) (8 mg/kg, i.v., once at 2 h post-reperfusion) significantly reduces cerebral infarct volume in male SD rats[1].

MedChemExpress (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.
Molecular Weight

655.76

Formula

C32H41N5O8S

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    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.

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Product Name:
PSD-95/nNOS PPI-IN-1
Cat. No.:
HY-175824
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