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| | Tat-NR2B9c Basic information |
| Product Name: | Tat-NR2B9c | | Synonyms: | Tat-NR2B9c;Tat-NR2B9c, >98%;L-Valine, L-tyrosylglycyl-L-arginyl-L-lysyl-L-lysyl-L-arginyl-L-arginyl-L-glutaminyl-L-arginyl-L-arginyl-L-arginyl-L-lysyl-L-leucyl-L-seryl-L-seryl-L-isoleucyl-L-α-glutamyl-L-seryl-L-α-aspartyl-;Tat-NR2B9c/NA-1;500992-11-0/1834571-04-8;(2S,5S,8S,11S,14S,17S,20S,23S,26S,29S,32S,35S,38S,41S,44S,47S,50S,53S,59S)-59-Amino-38-(3-amino-3-oxopropyl)-26,47,50-tris(4-aminobutyl)-14-((S)-sec-butyl)-11-(2-carboxyethyl)-5-(carboxymethyl)-29,32,35,41,44,53-hexakis(3-guanidinopropyl)-8,17,20-tris(hydroxymethyl)-60-(4-hydroxyphenyl)-23-isobutyl-2-isopropyl-4,7,10,13,16,19,22,25,28,31,34,37,40,43,46,49,52,55,58-nonadecaoxo-3,6,9,12,15,18,21,24,27,30,33,36,39,42,45,48,51,54,57-nonadecaazahexacontanoic acid;Tat-NR2Bct|||NA-1;Tat-NR2B9c trifluoroacetate | | CAS: | 500992-11-0 | | MF: | C105H188N42O30 | | MW: | 2518.88 | | EINECS: | | | Product Categories: | | | Mol File: | 500992-11-0.mol |  |
| | Tat-NR2B9c Chemical Properties |
| density | 1.52±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | form | Solid | | color | White to off-white | | Water Solubility | Water : ≥ 50 mg/mL (19.85 mM) |
| WGK Germany | WGK 3 | | HS Code | 2934999090 | | Storage Class | 11 - Combustible Solids |
| | Tat-NR2B9c Usage And Synthesis |
| Uses | 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 inhibitsneuronal nitric oxide synthase (nNOS)/PSD-95interaction, and possesses neuroprotective efficacy[1][2][5]. | | Biological Activity | Tat-NR2B9c (NA-1) is a 20-mer peptide composed of a membrane-permeant HIV-1 T at protein transduction domain sequence (a.a. 47-57) N-terminal to the NMDA receptor (NMDAR) GluN2B carboxyl tail sequence KLSSIESDV th at blocks intracellular NMDAR-PSD-95 interaction-induced neurotoxic signaling without affecting NMDAR-mediated synaptic activity or calcium influx. NA-1 protects cultured cortical neurons from NMDA excitotoxicity (50 nM; 20/40/100 μM NMDA) and reduces focal ischemic brain damage in rats in vivo (3 μmol/kg iv. bolus 1 hr post MCAO onset). | | in vivo | Tat-NR2B9c (10nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3nM/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. DOI:10.1523/JNEUROSCI.1464-07.2007
[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. DOI:10.1016/j.nbd.2011.12.019
[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. DOI:10.1177/0271678X15612099
[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. DOI:10.1111/j.1471-4159.2010.06994.x |
| | Tat-NR2B9c Preparation Products And Raw materials |
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