| Hazard Information | Back Directory | [Description]
Tat-NR2B9c (TFA) is a 20-aa peptide, which acts as a postsynaptic density-95 (PSD-95) inhibitor, with an EC50 of 6.7 nM for PSD-95d2 (PSD-95 PDZ domain 2), and 670 nM for PSD-95d1[1]. Tat-NR2B9c also reduces NMDA-induced p38 activation, and possesses neuroprotective efficacy[2].
EC50: 6.7 nM (PSD-95d2), 670 nM (PSD-95d1)[1]p38[2] | [Uses]
Tat-NR2B9c TFA (Tat-NR2Bct TFA) 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 TFA 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 TFA also inhibits neuronal nitric oxide synthase (nNOS)/PSD-95 interaction, and possesses neuroprotective efficacy[1]. | [in vivo]
Tat-NR2B9c (10?nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3?nmol/g[3]. | [IC 50]
NMDA Receptor; nNOS | [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. |
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