Product Description: 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].
Applications: Neuroscience-Neurodegeneration
Formula: C105H188N42O30
Citations: 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 Mar 21:109905./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. 7 January 2022, 113537.
References: [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.
CAS Number: 500992-11-0
Molecular Weight: 2518.88
Compound Purity: 99.97
Research Area: Neurological Disease
Solubility: H2O : 100 mg/mL (ultrasonic)
Target: iGluR;NO Synthase