Spadin |
カタログ番号GC13353
One-Click Copy Product Info
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血中に放出されるプロペプチドに由来する天然ペプチドである Spadin は、10 nM の IC50 値を持つ強力な TREK-1 チャネル遮断薬です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1270083-24-3
Sample solution is provided at 25 µL, 10mM.
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Spadin is a potent TREK-1 channel inhibitor with IC50 of 71nM. It is a secreted peptide derived from the propeptide generated by the maturation of NTSR3/Sortilin. [1]
TREK-1, aka KCNK2, is a two-pore domain ion channel that involved in the passive transmembrane K+ transport. It is related to the ischemia, anesthesia and electrogenesis in the neurons. It also plays an important role in the pathophysiological process of depression and in the response to antidepressant. [1]
In TREK-1 transfected COS-7 cells, 100nM of spadin inhibited 63% of the TREK-1 current stimulated by arachidnice acid. Spadin also blocked the TREK-1 channels activity in CA3 hippocampal neurons on brain slices of wild-type mice. [1]
In behavioral tests that predicting an antidepressant response, spadin-treated mice displayed a resistance to depression. Mice treated with spadin for 4 days also exhibited a significant antidepressant effect as well as elevated hippocampal phosphorylation of CREB protein and neurogenesis. [2]
References:
1. Borsotto M, Veyssiere J, Moha Ou Maati H 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.
2. Mazella J, Pétrault O, Lucas G, 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.
| Cas No. | 1270083-24-3 | SDF | |
| Chemical Name | (1Z,3S,4Z,7Z,9S,10Z,12S,13Z,15S,16Z,19Z,21S,22Z,24S)-15-((1H-indol-3-yl)methyl)-1-((S)-1-((6S,7Z,9S,10Z,12S,13Z)-9-((1H-indol-3-yl)methyl)-1-amino-6-((Z)-(((S)-1-((S)-2-((Z)-(((S)-1-((S)-2-((Z)-((S)-2-amino-1-hydroxy-3-(4-hydroxyphenyl)propylidene)amino)p | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@]1([H])CCCN1C(C/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@]2([H])CCCN2C([C@](/N=C(O)/[C@]3([H])CCCN3C([C@](/N=C(O)/[C@](N)([H])CC4=CC=C(O)C=C4)([H])C)=O)([H])CC(C)C)=O)([H])CCCNC(N)=N)([H])CC5=CNC6=CC=CC=C56)([H])CO)=O)([H]) | ||
| Formula | C96H142N26O22 | M.Wt | 2012.32 |
| 溶解度 | Soluble to 2 mg/ml in Water | 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 | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 496.9 μL | 2.4847 mL | 4.9694 mL |
| 5 mM | 99.4 μL | 496.9 μL | 993.9 μL |
| 10 mM | 49.7 μL | 248.5 μL | 496.9 μL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
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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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 14 reference(s) in Google Scholar.)