PE-22-28
TREK-1 channel modulator · spadin analogue
Identifier graph
Cross-references to canonical chemistry knowledge graphs. Each binding is the same identity used in PubMed-indexed literature.
- ChEMBL
- CHEMBL2109265
- Molecular weight
- ~2700 g/mol
What is PE-22-28?
PE-22-28 is a synthetic peptide analogue of the spadin peptide — a 17-residue fragment of the propeptide sortilin/neurotensin receptor 3 that selectively blocks the two-pore-domain potassium channel TREK-1. The compound has been characterised by Mazella, Lazdunski and colleagues as a research probe for TREK-1 function.
Approximate molecular weight 2700 Da. ChEMBL ID CHEMBL2109265.
Mechanism of action
TREK-1 is a two-pore-domain potassium channel that contributes to neuronal resting membrane potential, and its inhibition produces a slight depolarisation that increases neuronal excitability in specific circuits. PE-22-28 selectively blocks TREK-1, mimicking the activity of the endogenous spadin peptide.
TREK-1 inhibition has been investigated as a potential antidepressant mechanism — TREK-1-knockout mice show a depression-resistant phenotype, suggesting that selective TREK-1 antagonism could produce antidepressant effects.
Research context
Investigated in preclinical models of depression-related behaviour, neuronal excitability, and TREK-1-channel pharmacology. The compound is a research tool for studying TREK-1 function rather than a therapeutic candidate at this stage.
Analytical specifications
Every batch of PE-22-28 supplied by NMChem is characterised by reversed-phase HPLC for purity determination and by mass spectrometry for identity confirmation. Certificate of Analysis (COA) documents are issued per batch and made available on request.
Identity is confirmed by electrospray-ionisation mass spectrometry (ESI-MS); the observed mass falls within ±2 Da of the theoretical monoisotopic mass calculated from the residue sequence. Purity is determined by reversed-phase HPLC on a C18 column with a trifluoroacetic-acid-modified water/acetonitrile gradient and reported as the area-under-curve percentage of the main peak at 214 nm. NMChem specification is ≥99% main peak. Material ships as lyophilised powder and must be reconstituted in sterile water or bacteriostatic water immediately before use.
UK regulatory status
Supplied as a research-grade reference standard for laboratory use only. Not a licensed medicinal product in the United Kingdom and not approved by the MHRA for human or veterinary administration. Sale is restricted to researchers, institutions and laboratory professionals; the compound must be retained within research premises. End-user compliance with the Human Medicines Regulations 2012, the Misuse of Drugs Act 1971 (where applicable) and local institutional biosafety policy is the responsibility of the buyer.
Research literature
Selected peer-reviewed publications from PubMed referencing this compound.
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Shortened Spadin Analogs Display Better TREK-1 Inhibition,
Djillani A et al. · Frontiers in pharmacology · 2017
PubMed PMID 28955242
Related compounds
Other research compounds in adjacent mechanism classes or commonly used alongside PE-22-28.
Frequently asked questions about PE-22-28
What is spadin and how does PE-22-28 relate to it?
Get research-grade PE-22-28 from NMChem
UK supplier · HPLC and MS verified · Per-batch Certificate of Analysis · Tracked Royal Mail dispatch.