Tat-NR2B9c

Tat-NR2B9c (Tat-NR2Bct; NA-1) is a postsynaptic density-95 (PSD-95) inhibitor, with EC50 values of 6.7 nM and 670 nM for PSD-95d2 (PSD-95 PDZ domain 2) and PSD-95d1, respectively. Tat-NR2B9c disrupts the PSD-95/NMDAR interaction, inhibiting NR2A and NR2B binding to PSD-95 with IC50 values of 0.5 μM and 8 μM, respectively. Tat-NR2B9c also inhibits neuronal nitric oxide synthase (nNOS) /PSD-95 interaction, and possesses neuroprotective efficacy[1][2][5].

Product Specifications

CAS Number

[500992-11-0]

Product Name Alternative

Tat-NR2Bct; NA-1

UNSPSC

12352209

Target

IGluR; NO Synthase

Type

Peptides

Related Pathways

Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Tat-NR2B9c.html

Purity

99.77

Solubility

H2O : 100 mg/mL (ultrasonic)

Smiles

OC(C=C1)=CC=C1C[C@H](N)C(NCC(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CCCCN)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCC(N)=O)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CC(C)C)C(N[C@@H](CO)C(N[C@@H](CO)C(N[C@@H]([C@@H](C)CC)C(N[C@@H](CCC(O)=O)C(N[C@@H](CO)C(N[C@@H](CC(O)=O)C(N[C@H](C(O)=O)C(C)C)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O)=O

Molecular Formula

C105H188N42O30

Molecular Weight

2518.88

References & Citations

[1]Cui H, et al. PDZ protein interactions underlying NMDA receptor-mediated excitotoxicity and neuroprotection by PSD-95 inhibitors. J Neurosci. 2007 Sep 12;27 (37) :9901-15.|[2]Fan J, et al. P38 MAPK is involved in enhanced NMDA receptor-dependent excitotoxicity in YAC transgenic mouse model of Huntington disease. Neurobiol Dis. 2012 Mar;45 (3) :999-1009.|[3]Teves LM, et al. Efficacy of the PSD95 inhibitor Tat-NR2B9c in mice requires dose translation between species. J Cereb Blood Flow Metab. 2016 Mar;36 (3) :555-61.|[4]Jing Fan, et al. N-methyl-D-aspartate Receptor Subunit- And Neuronal-Type Dependence of Excitotoxic Signaling Through Post-Synaptic Density 9. J Neurochem. 2010 Nov;115 (4) :1045-56.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture)

Scientific Category

Peptides

Clinical Information

Phase 3

Isoform

NMDA Receptor; nNOS

Citation 01

Biochem Biophys Res Commun. 2024 May 8:720:150076.|J Cereb Blood Flow Metab. 2019 Aug;39 (8) :1588-1601. |J Neuropathol Exp Neurol. 2020 Jul 1;79 (7) :800-808.|Neuropharmacology. 2024 Jun 15:251:109905.|Neuroreport. 2021 Sep 8;32 (13) :1122-1127.|PLoS One. 2020 Mar 3;15 (3) :e0229499. |Sci Rep. 2018 May 18;8 (1) :7848. |Behav Brain Res. 2022 Jan 7:416:113537.