TAT-CN21
Based on 1 Customer Validation
TAT-CN21 is a potent CaMKII inhibitor with an IC50 of 77.2 nM. TAT-CN21 inhibits both calcium/calmodulin-dependent and autonomously activated CaMKII, blocks glutamate-induced translocation of CaMK IIα, and reverses the enhanced phosphorylation of CaMKII at Thr286 following excitotoxic injury. TAT-CN21 shows application potential in studies related to ischemic stroke by reducing neuronal excitotoxicity and exacerbating pre-existing long-term neuronal death prior to injury. TAT-CN21 improves definitive behaviors in rats with residual nerve injury without altering indicators such as mechanical/thermal hyperalgesia or spatial memory. TAT-CN21 can also be used in studies related to neuropathic pain.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.38%
- Fòrmula: C169H303N69O43
- Peso molecular:3989.65
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Almacenamiento:
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
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CaMK IIα 77.2 nM (IC50) |
In Vitro
Tat-CN21 (0.1-50 μM; 24 h) dose-dependently protects 7-8 DIV primary rat cortical neurons against glutamate/glycine-induced excitotoxic injury when administered 20 minutes prior to injury, with the optimal efficacy observed at 2-10 μM[1].
Tat-CN21 (10 μM; 1 h-2 h) protects primary rat cortical neurons at 7-8 DIV against glutamate/glycine-induced excitotoxic injury[1].
Tat-CN21 (10 μM; 8-24 h) exacerbates submaximal dose glutamate/glycine-induced excitotoxicity in 7-8 DIV primary rat cortical neurons, and post-injury overnight treatment with Tat-CN21 also increases neuronal death[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:7-8 DIV primary rat cortical neurons
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Concentration:10 μM
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Incubation Time:1 h pre-insult or post-insult up to 2 h
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Result:Protected 7-8 DIV primary rat cortical neurons from glutamate/glycine-induced excitotoxicity when applied up to 2 h post-insult onset, with protection lost by 3 h post-insult.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (male, 200-250 g, spared nerve injury-induced neuropathic pain)[2]
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Dosage:5 μM
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Administration:bilateral stereotaxic microinjection into rACC; once daily; 7 consecutive days
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Result:Did not significantly alter mechanical withdrawal threshold (2.85 ± 0.44 g on day 30; 2.87 ± 0.53 g on day 35) or thermal withdrawal latency compared to controls.
Did not significantly change spatial memory performance, including percentage of correct choices, working memory errors, or reference memory errors, compared to controls.
Reduced time spent in the light area to 32.84 ± 6.57% during the final 5 minutes in the place escape/avoidance paradigm, partially reversing pain-related aversion compared to controls.
Significantly reduced the relative expression of phosphorylated CaMKII-Thr286 to 1.12 ± 0.11 compared to controls (1.63 ± 1.18) in contralateral rACC tissue, with no significant effects on GluN2B protein or mRNA expression, or CaMKIIα protein, mRNA, or immunoreactivity levels.
Chemical Information
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Appearance Solid
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Peso molecular 3989.65
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Fòrmula C169H303N69O43
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Color White to off-white
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Sequence
Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Lys-Arg-Pro-Pro-Lys-Leu-Gly-Gln-Ile-Gly-Arg-Ser-Lys-Arg-Val-Val-Ile-Glu-Asp-Asp-Arg
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Sequence Shortening
YGRKKRRQRRRKRPPKLGQIGRSKRVVIEDDR
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Solvente y solubilidad
In Vitro:
H2O : ≥ 50 mg/mL (12.53 mM)
* "≥" means soluble, but saturation unknown.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (299 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Ashpole NM, et al. Excitotoxic neuroprotection and vulnerability with CaMKII inhibition. Mol Cell Neurosci. 2011;46(4):720-730. [Content Brief]
[2]. Gao X, et al. Activation of the N-methyl-D-aspartate receptor and calcium/calmodulin-dependent protein kinase IIα signal in the rostral anterior cingulate cortex is involved in pain-related aversion in rats with peripheral nerve injury. Behav Brain Res. 2023;452:114560. [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 |
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| H2O | 1 mM | 0.2506 mL | 1.2532 mL | 2.5065 mL | 6.2662 mL |
| 5 mM | 0.0501 mL | 0.2506 mL | 0.5013 mL | 1.2532 mL | |
| 10 mM | 0.0251 mL | 0.1253 mL | 0.2506 mL | 0.6266 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-CN21 Related Classifications
HY-P10638 Related Classifications
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