Spadin (trifluoroacetate salt) (Synonyms: YAPLPRWSGPIGVSWGLR) |
Catalog No.GC52449 |
An inhibitor of K2P2.1/TREK1
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Sample solution is provided at 25 µL, 10mM.
Spadin is an inhibitor of the two-pore domain potassium channel K2P2.1/TREK1 (Ki = 10 nM in homogenates from COS-7 cells expressing K2P2.1/TREK1) that corresponds to amino acids 12-28 of human sortilin, also known as the neurotensin-3 receptor (NTS3).1 It also binds to sortilin in C13NJ microglial cells (Ki = 8 nM). Spadin inhibits currents induced by arachidonic acid in COS-7 cells expressing K2P2.1/TREK1 (IC50 = 70.7 nM). It decreases immobility time in the forced swim test in mice.
1.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 designPLoS Biol.8(4)e1000355(2010)
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