PE-22-28

Synthetic heptapeptide inhibitor of the neuronal TREK-1 potassium channel, studied in preclinical neuroscience research.

Molecular Profile

Type
Synthetic heptapeptide (spadin-derived fragment)
Molecular formula
C₃₅H₅₅N₁₁O₉
Molecular weight
773.89 Da
CAS number
1801959-12-5
Amino acids
7
Sequence
Gly-Val-Ser-Trp-Gly-Leu-Arg
Modification
None (linear peptide)

Mechanism & Target Class

PE-22-28 is a selective inhibitor of the TREK-1 (KCNK2) two-pore-domain potassium channel. TREK-1 is a background K⁺ channel that contributes to stabilizing neuronal resting membrane potential; blocking it reduces this stabilization and alters cell excitability. Patch-clamp recordings in human TREK-1–expressing cell lines show that PE-22-28 inhibits TREK-1 current; comparative assays of the parent spadin peptide in the same system indicate lower inhibitory activity, motivating the truncation strategy that produced this fragment. PE-22-28's compact structure—7 residues with a hydrophobic tryptophan and a basic arginine—is structurally consistent with binding near the extracellular pore of TREK-1. In selectivity panels, PE-22-28 did not produce significant current inhibition at the closely related K2P channels TREK-2 or TRAAK. PE-22-28 is therefore characterized as a selective peptide antagonist of a neuronal two-pore K⁺ channel.

Storage & Handling

Lyophilized
–20 °C; store dry and protected from moisture.
Handling
No long-term stability data are published for this peptide; general small-peptide handling practices (sealed, dry, minimize freeze–thaw) apply.

Primary Database

PubChem CID 165437303 ↗

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