Tat-NR2B9c
- Product Name
- Tat-NR2B9c
- CAS No.
- 500992-11-0
- Chemical Name
- Tat-NR2B9c
- Synonyms
- Tat-NR2B9c;Tat-NR2B9c/NA-1;Tat-NR2B9c, >98%;Tat-NR2Bct|||NA-1;tat-nr2b9c ,P1220;500992-11-0/1834571-04-8;Tat-NR2B9c trifluoroacetate;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-;(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
- CBNumber
- CB33146625
- Molecular Formula
- C105H188N42O30
- Formula Weight
- 2518.88
- MOL File
- 500992-11-0.mol
Tat-NR2B9c Property
- 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)
Safety
- HS Code
- 2934999090
N-Bromosuccinimide Price
- Product number
- CS-5808
- Product name
- Tat-NR2B9c
- Packaging
- 1mg
- Price
- $84
- Updated
- 2021/12/16
- Product number
- CS-5808
- Product name
- Tat-NR2B9c
- Packaging
- 5mg
- Price
- $216
- Updated
- 2021/12/16
- Product number
- CS-5808
- Product name
- Tat-NR2B9c
- Packaging
- 10mg
- Price
- $336
- Updated
- 2021/12/16
- Product number
- orb611422
- Product name
- Tat-NR2B9c
- Packaging
- 5mg
- Price
- $382.5
- Updated
- 2021/12/16
- Product number
- orb611422
- Product name
- Tat-NR2B9c
- Packaging
- 10mg
- Price
- $460.7
- Updated
- 2021/12/16
Tat-NR2B9c Chemical Properties,Usage,Production
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 inhibits?neuronal nitric oxide synthase (nNOS)/PSD-95?interaction, 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 (10?nmol/g, i.v.) reduces infarction volume of male C57BL/6 mice, but has no effect at 3?nM/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
Raw materials
Preparation Products
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