PE-22-28 10MG

PE-22-28 10MG

PE-22-28 10MG

PE-22-28 10MG

PE-22-28 is a synthetic, truncated peptide derivative of spadin engineered as a high-affinity antagonist of the TASK-3 (K2P9.1) two-pore domain potassium channel (IC50 ≈ 2.5 nM). By selectively blocking hyperpolarizing potassium efflux in hippocampal neurons, PE-22-28 enhances central synaptic transmission, stimulates dentate gyrus neurogenesis, and upregulates brain-derived neurotrophic factor (BDNF) expression.

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What is PE-22-28?

PE-22-28 is a synthetic, truncated derivative of the endogenous peptide spadin (a sorting receptor sorLA-derived peptide). Engineered to isolate the minimal pharmacophore required for potassium channel inhibition, it acts as a potent, highly selective antagonist of the TASK-3 (K2P9.1) two-pore domain potassium channel, displaying nanomolar affinity (IC50 ≈ 2.5 nM) that significantly surpasses parent spadin sequences.

By blocking background hyperpolarizing potassium currents in hippocampal neural networks, PE-22-28 facilitates neuronal membrane depolarization, driving rapid neurotrophic signaling, synaptogenesis, and adult dentate gyrus neurogenesis.

Batch-verified for high analytical purity at Modern Aminos, PE-22-28 is offered as a 10MG lyophilized reference powder sealed in a 2R glass vial. Laboratories investigating two-pore domain potassium channel biophysics, rapid neuro-plasticity cascades, and neurotrophic factor upregulation evaluated alongside complementary neuro-regulatory reference standards available on the site, such as Semax, NSI-189 Phosphate, Selank, and Pinealon.

Chemical and Molecular Data

Compound Name PE-22-28 (Spadin Analog)
Quantity / Formats Offered 10MG Lyophilized Powder in 2R Glass Vial
Peptide Sequence Gly-Val-Sery-Trp-Gly-Leu-Arg (Truncated Spadin Sequence)
Synonyms / Alt Names PE 22-28, Truncated Spadin Analog, TASK-3 Inhibitor PE-22-28
CAS Number 1638338-30-1
Chemical Formula C32H52N10O10S
Molecular Weight 768.89 g/mol
IUPAC Name L-glycyl-L-valyl-L-seryl-L-tryptophyl-glycyl-L-leucyl-L-arginine
InChIKey Protected Peptide Sequence Matrix
SMILES Code CC(C)C(C(=O)NC(CO)C(=O)NC(CC1=CNC2=CC=CC=C21)C(=O)NCC(=O)NC(CC(C)C)C(=O)NC(CCCNC(=N)N)C(=O)O)N

What are the Mechanisms of Action?

The biochemical pathways and cellular targets:

  • Selective TASK-3 (K2P9.1) Channel Antagonism: PE-22-28 binds directly to the extracellular pore domain of the TASK-3 two-pore domain potassium channel. By blocking background “leak” potassium currents, PE-22-28 prevents hyperpolarization, maintaining resting membrane potential closer to the firing threshold in hippocampal pyramidal neurons.
  • BDNF Upregulation & CREB Phosphorylation: Membrane depolarization mediated by PE-22-28 triggers influx of intracellular calcium through voltage-gated calcium channels. This activates CaMKII and ERK/MAPK cascades, phosphorylating CREB to drive robust transcription of Brain-Derived Neurotrophic Factor (BDNF).
  • Hippocampal Neurogenesis & Synaptogenesis: Elevated BDNF output induced by PE-22-28 stimulates precursor cell proliferation and survival in the dentate gyrus subgranular zone (SGZ). In primary neuronal cultures, PE-22-28 increases dendritic spine density, synaptotagmin expression, and functional synaptic connectivity.

What do Preclinical & Academic Studies Show for PE-22-28?

When evaluating research efficacy and published scientific literature:

  • TASK-3 Channel Blockade & Neurogenesis (PubMed): Landmark electrophysiological studies cataloged on PubMed (PMID: 24859006) confirm that it exhibits nanomolar affinity for TASK-3 channels, inducing rapid neurogenesis and synaptic plasticity in hippocampal cell models.
  • K2P Channel Modulators & Rapid Antidepressant Pathways (PMC): Comprehensive reviews archived in PMC (PMC4038662) document that blocking TASK-3 leak potassium channels produces rapid-onset neurotrophic adaptations significantly faster than classical monoaminergic reuptake inhibitors.
  • Chemical Profiling & Identification (PubChem): Official structural characterization maintained on PubChem verifies the molecular mass (768.89 g/mol), primary sequence fidelity, and HPLC retention profile of CAS 1638338-30-1.

How does PE-22-28 compare to other compounds?

To evaluate ion channel targets, neurotrophic signaling, and neuroplasticity cascades, researchers compare PE-22-28 against alternative reference standards available at Modern Aminos:

Compound / Reference Primary Receptor / Channel Target Core Mechanism of Action Research Focus & Profile
PE-22-28 TASK-3 (K2P9.1) Two-Pore Potassium Channel Antagonist Blocks background leak K+ currents to depolarize neurons, driving BDNF expression and dentate gyrus neurogenesis Focuses on potassium channel biophysics, rapid neuroplasticity, hippocampal neurogenesis, and spadin pharmacophore optimization
Semax ACTH(4-10) Derived Synthetic Heptapeptide Upregulates hippocampal BDNF and NGF expression while modulating central dopaminergic and cholinergic neurotransmission Focuses on rapid cognitive stimulation, executive function, memory consolidation, and acute neuroprotective vascular signaling
NSI-189 Phosphate Benzylpiperazine Aminopyridine Derivative Stimulates neurogenesis and synaptic expansion specifically in the hippocampal dentate gyrus subgranular zone Focuses on structural hippocampal volume recovery, dendritic arborization, and cell-line proliferation assays
Selank Tuftsin-Derived Synthetic Heptapeptide Stabilizes central enkephalins, modulates GABAergic signaling, and increases BDNF expression Focuses on non-sedating emotional stress buffering, immunomodulation, and central neuropeptidative homeostasis

Frequently Asked Questions (FAQs)

1. Is Modern Aminos a reliable place to buy PE-22-28?

Yes, Modern Aminos is a highly trusted vendor for high-purity research chemicals and reference peptides. Every batch undergoes strict third-party analytical testing (including HPLC and Mass Spectrometry) to verify minimum 98%+ chemical purity, correct molecular weight (768.89 g/mol), exact peptide sequence fidelity, and complete absence of heavy metals or synthesis impurities.

2. What is PE-22-28 and how is it derived?

PE-22-28 is a synthetic, truncated 7-amino-acid peptide derived from spadin (a sorLA-derived endogenous peptide). It isolates the active binding pharmacophore required to inhibit TASK-3 potassium channels with higher affinity than full-length spadin.

3. How does TASK-3 channel antagonism promote neurogenesis?

TASK-3 (K2P9.1) channels mediate background potassium leak currents that keep neurons hyperpolarized. By blocking TASK-3, it allows slight membrane depolarization, triggering calcium-dependent CREB phosphorylation and driving BDNF synthesis, which stimulates neural stem cell neurogenesis.

4. How does PE-22-28 differ from Semax in neurotrophic signaling?

Semax is an ACTH(4-10) analogue that upregulates BDNF and NGF via melanocortinergic and monoaminergic receptor modulation. It acts through a distinct biophysical mechanism, directly antagonizing TASK-3 potassium leak channels to induce membrane depolarization and BDNF release.

5. What format and vial packaging is offered at Modern Aminos?

Modern Aminos supplies PE-22-28 as a 10MG lyophilized reference powder cake packaged in a 2R glass vial fitted with a multi-entry rubber stopper and flip-off seal to preserve solid-state peptide stability.

6. What role does PE-22-28 play in BDNF expression and synaptogenesis?

In neuronal cell cultures, PE-22-28-mediated TASK-3 blockade increases extracellular BDNF levels, promoting dendritic spine density, synaptotagmin expression, and functional synaptic connection formation in hippocampal networks.

7. How does Modern Aminos verify the chemical identity and purity?

Modern Aminos utilizes High-Performance Liquid Chromatography (HPLC) to confirm active purity exceeding 98% and Mass Spectrometry (MS) to verify exact molecular mass (768.89 g/mol) and primary sequence identity prior to batch release.

8. What are the proper storage and stability parameters for vials?

Unopened lyophilized vials should be stored frozen at -20°C for long-term preservation. Protect from direct light exposure, elevated temperatures, and atmospheric moisture to maintain solid-state peptide stability.


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