Spadin
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.
| Storage | Store at -20°C |
| M.Wt | 2012.32 |
| Cas No. | 1270083-24-3 |
| Formula | C96H142N26O22 |
| Solubility | Soluble to 2 mg/ml in H2O |
| 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 |
| SDF | Download SDF |
| 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]) |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
Quality Control & MSDS
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Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
