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Catalog/PE 22-28
PE 22-28
#1043
Lyophilized Peptide

PE 22-28 10mg

PE 22-28 is a synthetic heptapeptide (Gly-Val-Ser-Trp-Gly-Leu-Arg) corresponding to residues 22-28 of the 44-amino-acid propeptide released during furin maturation of sortilin, also known as neurotensin receptor-3 (gene SORT1). It is the shortened active core of spadin (PE 12-28), a 17-residue fragment of the same propeptide, and was designed from the study of spadin's blood degradation products. The stated 773.89 Da is the free base; peptides of this class are commonly supplied as an acetate salt, for which the theoretical mono-acetate mass is 833.9 Da and the actual acetate content is lot-dependent. Supplied strictly for in-vitro research and laboratory use only. Not for human or animal use.

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Mechanism of Action

PE 22-28 is a selective blocker of TREK-1 (KCNK2), a two-pore-domain potassium channel whose inhibition is associated with antidepressant-like activity in rodent models. Reported in-vitro potency at human TREK-1 is sub-nanomolar - approximately 0.1 nM by whole-cell patch clamp on arachidonic-acid-activated channels, against 40-60 nM for spadin - with no comparable inhibition of TREK-2, TRAAK, TRESK, TASK-1 or the cardiac hERG channel at the concentrations tested. Duration of action for PE 22-28 itself is NOT established: the widely quoted figure of roughly 23 hours is a behavioural half-effect time measured in the forced swim test for chemically modified analogs (G/A-PE 22-28 and its biotinylated form), not a pharmacokinetic half-life and not a measurement of this peptide. Downstream endpoints studied in preclinical models include MAPK and PI3K pathway activation, hippocampal neurogenesis and synaptogenesis markers (PSD-95, synapsin), and BDNF expression. Some work reports a biphasic concentration-response at TREK-1, so dose selection is itself a research variable.

Properties

Molecular Formula

C₃₅H₅₅N₁₁O₉

Molecular Weight

773.89 Da

Sequence

Gly-Val-Ser-Trp-Gly-Leu-Arg

Half-Life

Not established - no published pharmacokinetic study

Storage

Store lyophilized at -20°C. Reconstituted at 2-8°C, use within 14 days.

Shipping & Delivery

  • Same-day dispatch on orders placed before 2 PM MST (Arizona — no daylight saving).
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Quality & Testing

  • No third-party certificate has been published for this compound yet.
  • USA-based; dispatched from Phoenix, Arizona.
  • Supplied strictly for in-vitro laboratory research — not for human use.

Certificates are published for each lot we have tested — see the 14 published so far.

Research Applications

1TREK-1 (KCNK2) channel pharmacology and electrophysiology
2Two-pore-domain potassium channel selectivity profiling
3Antidepressant-mechanism models (forced swim, novelty-suppressed feeding)
4Hippocampal neurogenesis and synaptogenesis marker studies
5Comparative potency and stability vs. spadin (PE 12-28)

References & Citations

(3)
1

Shortened Spadin Analogs Display Better TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity

Djillani A, Pietri M, Moreno S, et al.

Front Pharmacol (2017)PMID: 28955242 DOI
2

Propeptide cleavage conditions sortilin/neurotensin receptor-3 for ligand binding

Munck Petersen C, Nielsen MS, Jacobsen C, et al.

EMBO J (1999)PMID: 9927419 DOI
3

Role of TREK-1 in Health and Disease, Focus on the Central Nervous System

Djillani A, Mazella J, Heurteaux C, Borsotto M.

Front Pharmacol (2019)PMID: 31031627 DOI

Research Use Only

This product is intended strictly for in-vitro research, educational, and laboratory use. Not for human consumption. The information provided is based on published research and does not constitute medical advice.

Research reference

A published identity, mechanism, and bibliography record corresponds to this catalog entry.

Research reference: PE 22-28

More references from the Research Library (1)

Further papers cited in the Library's PE 22-28 record, each checked against PubMed. They describe the compound in research settings and are not statements about this product. See the full record for its identity, structure and complete bibliography.

  1. Spadin, a sortilin-derived peptide, targeting rodent TREK-1 channels: a new concept in the antidepressant drug design.

    Mazella J, Pétrault O, Lucas G, et al.

    PLoS biology (2010)In vitro · AnimalPMID 20405001