Spadin TFA
Based on 1 publication(s) in Google Scholar
Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.73%
- Fòrmula: C92H143F3N26O24
- Peso molecular:2126.36
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Almacenamiento:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Spadin TFA
MoreVer todos los productos específicos de isoformas 5-HT Receptor
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Actividad biológica
Spadin TFA (100 nM; COS-7 cells) has inhibitory effect of spadin on the TREK-1 channel and blocks 63% of the TREK-1 current stimulated by arachidonic acid[1].
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Spadin TFA (100 nM) blocks the TREK-1 channels activity in CA3 hippocampal neurons on brain slices of wild-type mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? Spadin TFA (0.01-100 μM, 100 μL; ICV, i.p. and i.v.; daily, for 7 days; male C57Bl/6J and TREK-1 deficient mice) has anti-depressant behavior in mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57Bl/6J and TREK-1 deficient mice[2]
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Dosage:10 μM
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Administration:Intraperitoneal injection; for 30 min
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Result:Increased of the 5-HT neuron firing rate in the dorsal raphe nucleus (DRN).
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Animal Model:Male C57Bl/6J and TREK-1 deficient mice[2]
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Dosage:0.01-100 μM
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Administration:Intracerebroventrical injection (100 nM), intraperitoneal injection (1-100 μM) and intravenous injection (0.01-1 μM); daily, for 7 days
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Result:Had any effect on mouse locomotion analyzed in short- or long-time after the drug injection.
Chemical Information
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Appearance Solid
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Peso molecular 2126.36
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Fòrmula C92H143F3N26O24
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Color White to off-white
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Sequence Shortening
YAPLPRWSGPIGVSWGLR
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Publications (1)
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Journal Impact Factor
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Most Recent
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Biol Chem
Validation of TREK1 ion channel activators as an immunomodulatory and neuroprotective strategy in neuroinflammation. [Abstract]2023 Feb 14;404(4):355-375. PMID: 36774650
Solvente y solubilidad
DMSO : 100 mg/mL (47.03 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 25 mg/mL (11.76 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 and light). 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 and light). 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.18 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: PBS
Solubility: 50 mg/mL (23.51 mM); Clear solution; Need ultrasonic
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.
Pureza y Documentación
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Ficha de datos (272 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]. Borsotto M, et, al. Targeting two-pore domain K(+) channels TREK-1 and TASK-3 for the treatment of depression: a new therapeutic concept. Br J Pharmacol. 2015 Feb;172(3):771-84. [Content Brief]
[2]. Mazella J, et, al. Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design. PLoS Biol. 2010 Apr 13;8(4):e1000355. [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 and light). 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 / DMSO | 1 mM | 0.4703 mL | 2.3514 mL | 4.7029 mL | 11.7572 mL |
| 5 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | 2.3514 mL | |
| 10 mM | 0.0470 mL | 0.2351 mL | 0.4703 mL | 1.1757 mL | |
| DMSO | 15 mM | 0.0314 mL | 0.1568 mL | 0.3135 mL | 0.7838 mL |
| 20 mM | 0.0235 mL | 0.1176 mL | 0.2351 mL | 0.5879 mL | |
| 25 mM | 0.0188 mL | 0.0941 mL | 0.1881 mL | 0.4703 mL | |
| 30 mM | 0.0157 mL | 0.0784 mL | 0.1568 mL | 0.3919 mL | |
| 40 mM | 0.0118 mL | 0.0588 mL | 0.1176 mL | 0.2939 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.
Spadin TFA Related Classifications
HY-P1422A Related Classifications
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