Tat-NR2B9c
Based on 8 publication(s) in Google Scholar
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.89%
- CAS 番号: 500992-11-0
- 分子式: C105H188N42O30
- 分子量:2518.88
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
MedChemExpress（MCE）の使用を引用している文献 Tat-NR2B9c
More- Sci Rep. 2018 May 18;8(1):7848. [Abstract]
- Neuropharmacology. 2024 Jun 15:251:109905. [Abstract]
- J Cereb Blood Flow Metab. 2019 Aug;39(8):1588-1601. [Abstract]
- J Neuropathol Exp Neurol. 2020 Jul 1;79(7):800-808. [Abstract]
- Behav Brain Res. 2022 Jan 7:416:113537. [Abstract]
- PLoS One. 2020 Mar 3;15(3):e0229499. [Abstract]
- Biochem Biophys Res Commun. 2024 Aug 6:720:150076. [Abstract]
- Neuroreport. 2021 Sep 8;32(13):1122-1127. [Abstract]
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生物活性
製品説明
IC50 & Target
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NMDA Receptor |
nNOS |
体外実験
Tat-NR2B9c is a PSD-95 inhibitor, with an EC50 of 6.7 nM for PSD-95d2, representing a >100-fold higher affinity for this domain than for PSD-95d1 (EC50, 0.67 μM). Tat-NR2B9c inhibits NMDAR2A, NMDAR2B, and NMDAR2C binding to PSD-95, with IC50s of 0.5 μM, ∼8 μM, and 0.75 μM, respectively.Tat-NR2B9c also blocks the interaction between PSD-95 and nNOS with an IC50 of ∼0.2 μM[1]. Tat-NR2B9c reduces association of PSD-95 with GluN2B by ∼50% in the YAC128 striatum, decreases NMDA-induced p38 activation in YAC128 striatal tissue, but shows no effect on the NMDA-induced JNK activation[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 500992-11-0
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性状 Solid
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分子量 2518.88
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分子式 C105H188N42O30
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Color White to off-white
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別名
Tat-NR2Bct; NA-1
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シーケンスの短縮
YGRKKRRQRRRKLSSIESDV
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (8)
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Journal Impact Factor
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Most Recent
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Sci Rep
N-methyl D-aspartate receptor subtype 2B antagonist, Ro 25-6981, attenuates neuropathic pain by inhibiting postsynaptic density 95 expression. [Abstract]2018 May 18;8(1):7848. PMID: 29777135 -
Neuropharmacology
Tat-NR2B9c attenuates oxidative stress via inhibition of PSD95-NR2B-nNOS complex after subarachnoid hemorrhage in rats. [Abstract]2024 Jun 15:251:109905. PMID: 38521229 -
J Cereb Blood Flow Metab
Treatment of secondary brain injury by perturbing postsynaptic density protein-95-NMDA receptor interaction after intracerebral hemorrhage in rats. [Abstract]2019 Aug;39(8):1588-1601. PMID: 29513122
Tat-NR2B9c purchased from MedChemExpress. Usage Cited in: J Cereb Blood Flow Metab. 2019 Aug;39(8):1588-1601. [Abstract]
Tat-NR2B9c affects PSD95-NR2B-nNOS complex and PSD95-neurexin-neuroligin complex formation after ICH. Western blots of IP with PSD95 antibody show the interactions between nNOS, NR2B, neurexin-1 or neuroligin-1, and PSD95.
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J Neuropathol Exp Neurol
Activation of CaMKII and GluR1 by the PSD-95-GluN2B Coupling-Dependent Phosphorylation of GluN2B in the Spinal Cord in a Rat Model of Type-2 Diabetic Neuropathic Pain. [Abstract]2020 Jul 1;79(7):800-808. PMID: 32386416 -
Behav Brain Res
Intravenous administration of Tat-NR2B9c peptide, a PSD95 inhibitor, attenuates reinstatement of cocaine-seeking behavior in rats. [Abstract]2022 Jan 7:416:113537. PMID: 34416299 -
PLoS One
Hypothermia but not NMDA receptor antagonism protects against stroke induced by distal middle cerebral arterial occlusion in mice. [Abstract]2020 Mar 3;15(3):e0229499. PMID: 32126102 -
Biochem Biophys Res Commun
Formation of chronic morphine withdrawal memories requires C1QL3-mediated regulation of PSD95 in the mouse basolateral amygdala. [Abstract]2024 Aug 6:720:150076. PMID: 38772224 -
Neuroreport
Stroke injury induced by distal middle cerebral artery occlusion is resistant to N-methyl-d-aspartate receptor antagonism in FVB/NJ mice. [Abstract]2021 Sep 8;32(13):1122-1127. PMID: 34284452
溶剤 & 溶解度
体外:
H2O : 100 mg/mL (39.70 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
プロトコル
Cell Assay[2]
Postnatal mono-cultured WT and YAC128 striatal neurons (DIV 9, due to the viability of these mono-cultured MSNs) are pretreated for 1 h with 200 nM Tat-NR2B9c, and/or SB-239063 (p38 inhibitor), and/or SP-600125 (JNK inhibitor), then incubated with or without 500 μM NMDA for 10 min. After NMDA treatment, striatal neurons are washed once with warm plating medium (PM) and then incubated in conditioned PM (without Tat peptides or p38, JNK inhibitors) for 24 h. Then cells are washed with PBS once and fixed with 4% paraformaldehyde (PFA) for 30 min[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration[3]
Mice[3]
In each study mice are randomly allocated to three treatment groups (0.0, 3.0, 10.0 nMole/g Tat-NR2B9c) or to sham treatment. The individual performing the experimental procedures, administering treatments and performing the analyses is blinded to the treatment assignments. Tat-NR2B9c is prepared at the indicated doses and administered intravenously via the tail vein using a pump in a volume of 1 µL/g over 5 min beginning at reperfusion[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (278 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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取扱説明書 (2659 KB)
参考文献
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
[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. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.3970 mL | 1.9850 mL | 3.9700 mL | 9.9250 mL |
| 5 mM | 0.0794 mL | 0.3970 mL | 0.7940 mL | 1.9850 mL | |
| 10 mM | 0.0397 mL | 0.1985 mL | 0.3970 mL | 0.9925 mL | |
| 15 mM | 0.0265 mL | 0.1323 mL | 0.2647 mL | 0.6617 mL | |
| 20 mM | 0.0199 mL | 0.0993 mL | 0.1985 mL | 0.4963 mL | |
| 25 mM | 0.0159 mL | 0.0794 mL | 0.1588 mL | 0.3970 mL | |
| 30 mM | 0.0132 mL | 0.0662 mL | 0.1323 mL | 0.3308 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Tat-NR2B9c 関連分類
HY-P0117 関連分類
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