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Cat. No.: HY-175824

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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 (K_i = 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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Formule: C₃₂H₄₁N₅O₈S
Masse moléculaire:655.76

Stockage:

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

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

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Use of MCE Products

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

Activité biologique
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- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
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Activité biologique

Description

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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.

Chemical Information

Masse moléculaire 655.76
Formule C₃₂H₄₁N₅O₈S
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Wang J, et al. Development of cell-permeable and plasma-stable peptidomimetic inhibitors against PSD-95/nNOS interaction as potential anti-ischemic stroke agents. Eur J Med Chem. 2025 Dec 5;299:118062. [Content Brief]

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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.

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100 mg

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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PSD-95/nNOS PPI-IN-1

Voir tous les produits spécifiques à Isoform iGluR

Voir tous les produits spécifiques à Isoform NO Synthase