What is PE-22-28?
PE-22-28 is a seven-amino-acid peptide, GVSWGLR, cut down from spadin, a fragment of the sortilin propeptide that blocks the potassium channel TREK-1. A 2017 study designed it to be more potent and longer-lasting than spadin in cell and mouse experiments. Here is where it comes from, what that work measured and what is still unknown.
PE-22-28 in one table.
| Sequence | Gly-Val-Ser-Trp-Gly-Leu-Arg (GVSWGLR), unmodified ends |
|---|---|
| Length | 7 amino acids, a heptapeptide |
| Formula | C35H55N11O9 |
| Molecular weight | 773.9 g/mol (monoisotopic 773.4184) |
| PubChem CID | 165437303 |
| Source | Positions 22 to 28 of the sortilin propeptide, identical in human and mouse |
| Target | TREK-1 potassium channel |
| Status | Research compound; no registered human trials |
Formula and masses from Helion's peptide molecular weight calculator, matching PubChem.
A piece of a receptor's propeptide.
Sortilin, also called neurotensin receptor 3, is made with a 44-residue propeptide that is cut away as the receptor matures. In 2010 Jean Mazella's group in France showed that a 17-residue piece of that propeptide, PE 12-28, which they named spadin, binds the TREK-1 potassium channel with nanomolar affinity and blocks its current, and proposed it as a new concept in antidepressant drug design, based on rodent studies.
Shorter, stronger in the assays.
In a 2017 study the same group built shorter analogs from the pieces spadin breaks into in blood. The seven-residue PE 22-28 blocked human TREK-1 in cells with a half-maximal concentration of about 0.12 nM, against 40 to 60 nM for spadin, and its effect in mice lasted up to 23 hours, against about 7 hours for spadin. A 2018 paper from the group calls it mini-spadin. Results in cells and mice describe those systems only.
No human trials.
PE-22-28 has been studied only in cells and animals; ClinicalTrials.gov lists no trials of it or of spadin, and it is not an approved drug. Helion supplies compounds for laboratory research use only.
Not supplied.
Helion does not supply PE-22-28. The research library covers the compounds it does supply, and Selank vs Semax compares two other short peptides studied in rodent behavior models.
Specs and storage by compound.
Questions (7)
What is PE-22-28?
A seven-amino-acid peptide, GVSWGLR, derived from spadin, a fragment of the sortilin propeptide that blocks the TREK-1 potassium channel.
What is the PE-22-28 sequence?
Gly-Val-Ser-Trp-Gly-Leu-Arg, with unmodified ends.
What is spadin?
PE 12-28, a 17-residue fragment of the sortilin propeptide reported in 2010 to bind and block the TREK-1 channel.
How is PE-22-28 different from spadin?
It is the last seven residues of spadin. In the 2017 study it blocked TREK-1 at far lower concentrations and its effect in mice lasted longer.
What is the molecular weight of PE-22-28?
773.9 g/mol (C35H55N11O9).
Has PE-22-28 been tested in humans?
No. ClinicalTrials.gov lists no trials of PE-22-28 or spadin.
Does Helion sell PE-22-28?
No.
Published studies (4)
- Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design
- Shortened Spadin Analogs Display Better TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity
- The Involvement of Sortilin/NTSR3 in Depression as the Progenitor of Spadin and Its Role in the Membrane Expression of TREK-1
- Fighting against depression with TREK-1 blockers: Past and future. A focus on spadin
Citations from PubMed for reference. They describe the compound in the literature, not any Helion lot, and nothing here is guidance on use.