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Tat-NR2B9c

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Chemical Structure| 500992-11-0 同义名 : NA-1;Tat-NR2Bct
CAS号 : 500992-11-0
货号 : A318271
分子式 : C105H188N42O30
纯度 : 98+%
分子量 : 2518.88
MDL号 : MFCD09842404
存储条件：

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

H2O: 100 mg/mL(39.7 mM)，配合低频超声助溶
动物实验配方：
生物活性
描述 Postsynaptic density protein-95 (PSD-95)/Discs-large/ZO-1 (PDZ) domains play an essential role in the regulation of intracellular signaling involved in neuronal disease and cancer. Tat-NR2B9c is a 20-mer peptide consisting of nine C-terminal amino acids of the NMDA NR2B subunit. It inhibits PSD-95 domain 1 and PSD-95 domain 2 with EC50 values of 670 nM and 6.7 nM, respectively. The IC50 values for Tat-NR2B9c inhibiting the interactions between NMDAR2A, NMDAR2B, NMDAR2C and PSD-95 are 0.5, 8, and 0.75μm, respectively. Tat-NR2B9c also inhibits the interaction between neuronal nitric oxide synthase and PSD-95 with an IC50 value of 0.2μm[3]. In NMDA-treated neuronal cultures, Tat-NR2B9c at 0.5µM suppressed NMDA-induced superoxide production by 75%. The NMDA-type glutamate receptor-triggered NOX2 activation and DNA damage were also prevented by Tat-NR2B9c at 0.5µM[4]. In mice subjected to temporary middle cerebral artery occlusion (tMCAO) for 30 and 60 min, treatment with 10nmol/g Tat-NR2B9c significantly decreased infarct volumes by 24.5% and 26.0%, respectively[5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

0.40mL

0.08mL

0.04mL

1.99mL

0.40mL

0.20mL

3.97mL

0.79mL

0.40mL
参考文献

[1]Teves LM, Cui H, 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.

[2]Chen Y, Brennan-Minnella AM, et al. Tat-NR2B9c prevents excitotoxic neuronal superoxide production. J Cereb Blood Flow Metab. 2015 May;35(5):739-42.

[3]Cui H, Hayashi A, Sun HS, Belmares MP, Cobey C, Phan T, Schweizer J, Salter MW, Wang YT, Tasker RA, Garman D, Rabinowitz J, Lu PS, Tymianski M. 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. PMID: 17855605; PMCID: PMC6672641.

[4]Chen Y, Brennan-Minnella AM, Sheth S, El-Benna J, Swanson RA. Tat-NR2B9c prevents excitotoxic neuronal superoxide production. J Cereb Blood Flow Metab. 2015 May;35(5):739-42. doi: 10.1038/jcbfm.2015.16. Epub 2015 Feb 11. PMID: 25669908; PMCID: PMC4420863.

[5]Teves LM, Cui H, Tymianski M. 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. Epub 2015 Oct 19. PMID: 26661213; PMCID: PMC4794097.