Tat-NR2B9c (Synonyms: Tat-NR2Bct; NA-1) |
| Catalog No.GC30774 |
Tat-NR2B9c is designed to prevent nitric oxide (NO) production by preventing postsynaptic density protein 95 (PSD-95) binding to N-methyl-D-aspartate (NMDA) receptors and neuronal nitric oxide synthase.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 500992-11-0
Sample solution is provided at 25 µL, 10mM.
Tat-NR2B9c is designed to prevent nitric oxide (NO) production by preventing postsynaptic density protein 95 (PSD-95) binding to N-methyl-D-aspartate (NMDA) receptors and neuronal nitric oxide synthase. Tat-NR2B9c dissociates NMDA glutamate receptors from downstream excitotoxic signaling pathways without affecting normal glutamate receptor function. Neuroprotective effects of Tat-NR2B9c have been demonstrated in a diverse range of stroke models in several species including rodents, primates, and humans. Moreover, Tat-NR2B9c peptide has shown clinical efficacy as a neuroprotective agent in acute stroke.[1][2]
In vitro study indicated that Tat-NR2B9c have no measurable effect on the rate or magnitude of NMDA-induced calcium influx. However, Tat-NR2B9c prevented NMDA-induced DNA breaks, and the neuronal death could be significantly reduced by Tat-NR2B9c. Tat-NR2B9c also prevented NMDA-induced superoxide p47phox formation by blocking phosphorylation, and neuroprotective effect of Tat-NR2B9c may be partly or wholly attributable to its suppression of NOX2 activation. In addition, Tat-NR2B9c, which targets the PDZ domain of PSD-95, disrupts the functional coupling between NR2B and NOX2.[2]
In vivo experiments demonstrated that Tat-NR2B9c would be effective in treating or preventing perinatal and neonatal hypoxic-ischemic brain injury, as well as its related brain disorders. Results indicated that Tat-NR2B9c reduced brain damage caused by hypoxic-ischemic injury when administered either before or after ischemia and improved post-HI neurobehavioral outcomes when delivered before or after ischemia. Moreover, Tat-NR2B9c might exert neuroprotective effects through the promotion of pro-survival signaling and inhibition of pro-apoptotic signaling.[1]
References:
[1]. Xu B, et al. Neuroprotective Effects of a PSD-95 Inhibitor in Neonatal Hypoxic-Ischemic Brain Injury. Mol Neurobiol. 2016 Nov;53(9):5962-5970.
[2]. Chen Y, et al. Tat-NR2B9c prevents excitotoxic neuronal superoxide production. J Cereb Blood Flow Metab. 2015 May;35(5):739-42.
| Cell experiment [1]: | |
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Cell lines |
Neuronal cells |
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Preparation Method |
Studies were initiated in cultures at days 10 to 12 in vitro by exchanging the culture medium with a low-magnesium balanced salt solution.10 Peptides and drugs were added from concentrated stocks 15 minutes before the addition of NMDA. |
|
Reaction Conditions |
Treated neuronal cell cultures with 100 μmol/L NMDA for 30 minutes together with Tat-NR2B9c over a range of concentrations: 0, 0.05, 0.1, 0.5 μmol/L. |
|
Applications |
Tat-NR2B9c showed neuroprotectant efficacy in patients with acute stroke. Tat-NR2B9c is designed to uncouple NO production from NMDAr activation by blocking PSD-95 binding to NMDAr and nNOS. Tat-NR2B9c also prevents NMDA-induced superoxide p47phox formation by blocking phosphorylation. |
| Animal experiment [2]: | |
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Animal models |
Timed pregnant CD1 mice (7-day-old (P7) pups of either sex) |
|
Preparation Method |
Tat-NR2B9c was administered intraperitoneally at a single dose of 15 μg/g body weight in 100–120 μl of saline. |
|
Dosage form |
15 μg/g |
|
Applications |
Tat-NR2B9c has a neuroprotective effect in the neonatal mouse hypoxic-ischemic brain injury model of stroke. In addition, Tat-NR2B9c reduced brain damage caused by hypoxic-ischemic injury and showed the potential to promote long-term recovery. Tat-NR2B9c would be effective in treating or preventing perinatal and neonatal hypoxic-ischemic brain injury, as well as its related brain disorders. |
|
References: [1]. Chen Y, et al. Tat-NR2B9c prevents excitotoxic neuronal superoxide production. J Cereb Blood Flow Metab. 2015 May;35(5):739-42. [2]. Xu B, et al. Neuroprotective Effects of a PSD-95 Inhibitor in Neonatal Hypoxic-Ischemic Brain Injury. Mol Neurobiol. 2016 Nov;53(9):5962-5970. |
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| Cas No. | 500992-11-0 | SDF | |
| Synonyms | Tat-NR2Bct; NA-1 | ||
| Canonical SMILES | Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Leu-Ser-Ser-Ile-Glu-Ser-Asp-Val | ||
| Formula | C105H188N42O30 | M.Wt | 2518.88 |
| Solubility | Water : ≥ 50 mg/mL (19.85 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.397 mL | 1.985 mL | 3.97 mL |
| 5 mM | 0.0794 mL | 0.397 mL | 0.794 mL |
| 10 mM | 0.0397 mL | 0.1985 mL | 0.397 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 28 reference(s) in Google Scholar.)
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