Description

PE-22-28

Synthetic shortened spadin derivative for in vitro research on selective TREK-1 potassium channel inhibition, hippocampal neurogenesis, synaptic plasticity, and neurocognitive pathways

Overview & Mechanism of Action (In Vitro)

PE-22-28 is a synthetic heptapeptide consisting of seven amino acids with the sequence (Gly-Val-Ser-Trp-Gly-Leu-Arg), engineered from the active functional domain of native spadin (a sortilin-derived propeptide). It represents a high-affinity, enzymatically stabilized miniaturized peptide antagonist of two-pore domain potassium channels TREK-1 (K2P2.1). In cellular neurobiology, patch-clamp electrophysiology, and neuropsychopharmacology, it serves as a primary reference model for studying neuronal excitability modulation and rapid neurogenic signaling:

• Selective & High-Affinity TREK-1 Channel Blockade: Potent and selective inhibition of TREK-1 potassium currents (IC50≈0.12 nM) with enhanced stability and receptor affinity compared to full-length spadin, without cross-inhibition of related K2P channels (e.g., TREK-2, TRAAK).
• Induction of Adult Hippocampal Neurogenesis: Significant stimulation of proliferation, survival, and neuronal differentiation of progenitor cells in the subgranular zone of the dentate gyrus in vitro.
• Activation of BDNF / TrkB Signaling & Synaptogenesis: Upregulation of brain-derived neurotrophic factor (BDNF) release, induction of TrkB receptor phosphorylation, and enhancement of long-term potentiation (LTP) in hippocampal neuronal networks.
• Cellular Bioenergetic Support & Excitotoxicity Attenuation: Reduced neuronal vulnerability to glutamate-induced excitotoxic stress and mitochondrial depolarization in cell culture models.

Technical & Chemical Specifications

• Classification: Research Peptide / Selective TREK-1 Channel Antagonist (Stabilized Spadin Analogue)
• Amino Acid Sequence: Gly-Val-Ser-Trp-Gly-Leu-Arg (GVSWGLR)
• Form: Sterile lyophilized white powder (cake)
• Component Identification: Verified via Mass Spectrometry (MS) and analytical HPLC
• Recommended Reconstitution Solvent: Sterile bacteriostatic water or sterile phosphate-buffered saline (PBS)
• Storage Conditions: Store long-term at -20 °C in a dry, dark environment. Following reconstitution, keep refrigerated at 2–8 °C in accordance with standard laboratory protocols.

Scientific References & Literature

• Djillani, A., et al. Shortened spadin analogs with enhanced TREK-1 channel inhibition and neurogenic properties in vitro and in vivo. Neuropharmacology, 2017.
• Mazella, J., et al. Spadin, a sortilin-derived peptide, targeting TREK-1 channels: A new concept for rapid antidepressant signaling. PLoS Biology, 2010.
• Veyssiere, J., et al. PE-22-28, a new TREK-1 blocker with potent neurotrophic and neuroprotective effects in hippocampal neuronal cultures. Biochemical Pharmacology, 2018.
• Heurteaux, C., et al. TREK-1, a two-pore-domain potassium channel, as a molecular target for neuroprotection and affective regulation. Current Drug Targets, 2016.

Legal Disclaimer & Terms of Purchase

This product is classified and supplied strictly for laboratory, scientific, and in vitro research purposes only (Research Use Only – RUO). This compound is not a drug, medicine, dietary supplement, cosmetic product, or substance intended for human or veterinary consumption, direct administration, injection, or diagnostic procedures.

By placing an order, the purchaser explicitly confirms that they are at least 18 years of age, possess the requisite professional qualifications and laboratory equipment to safely handle research materials, and are fully conversant with all relevant safety protocols for managing research substances. The seller assumes no liability for any use contrary to these terms.