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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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  • Certificates published per tested lot — see current coverage

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

CAS Number

1801959-12-5

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.

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  • Same-day dispatch on orders placed before 2 PM MST (Arizona — no daylight saving).
  • US shipping from $5. Free Priority on orders $100+ (before discounts).
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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

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

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

PLoS Biol (2010)PMID: 20405001 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