PE-22-28: Molecular Structure
Chemical properties, amino acid sequence, and structural analysis
📌TL;DR
- •Molecular formula: C35H55N11O9
- •Molecular weight: 773.89 Da
- •Half-life: ~23 hours (duration of action in mice)
Amino Acid Sequence
7 amino acids
Formula
C35H55N11O9
Molecular Weight
773.89 Da
Half-Life
~23 hours (duration of action in mice)
Molecular Structure#
PE-22-28 is a linear heptapeptide with the sequence Gly-Val-Ser-Trp-Gly-Leu-Arg (GVSWGLR). It was derived from the C-terminal portion of spadin (a 17-amino acid peptide corresponding to positions 12-28 of the sortilin propeptide) through systematic truncation studies designed to identify the minimal active fragment.
Amino Acid Sequence#
| Property | Value |
|---|---|
| Sequence | GVSWGLR (Gly-Val-Ser-Trp-Gly-Leu-Arg) |
| Length | 7 amino acids |
| Molecular weight | ~773.89 Da |
| Molecular formula | C35H55N11O9 |
| CAS number | 1801959-12-5 |
| Parent compound | Spadin (17-mer from sortilin propeptide) |
| Target | TREK-1 (KCNK2) potassium channel |
Structure-Activity Relationship#
The tryptophan residue (Trp, position 4 of PE-22-28) is believed to be critical for TREK-1 channel interaction. The compact 7-amino acid structure provides several advantages over the parent 17-mer spadin:
- 300-500x improved affinity: IC50 of 0.12 nM vs 40-60 nM for spadin
- Extended duration: 23 hours vs 7 hours for spadin
- Improved metabolic stability: Resistance to blood proteases
- Maintained selectivity: Specific for TREK-1 over other potassium channels
Pharmacokinetic Properties#
| Parameter | Details |
|---|---|
| Duration of action | ~23 hours (mouse, IP) |
| Route | Intraperitoneal (research) |
| IC50 at TREK-1 | 0.12 nM |
| Selectivity | Specific for TREK-1 vs other K2P channels |
| Metabolism | Resistant to rapid blood degradation (unlike spadin) |
PE-22-28 was specifically designed from analysis of spadin's metabolic fate in blood, identifying the stable active core fragment that retains potent TREK-1 blocking activity while resisting proteolytic degradation.
Stability Characteristics#
PE-22-28 demonstrates improved metabolic stability compared to spadin, with resistance to the blood proteases that rapidly degrade the parent compound. Research-grade material is typically lyophilized and stored at -20 degrees C.
Molecular Context#
PE-22-28 belongs to the Neuropeptide category of research peptides. The molecular properties of PE-22-28 determine its pharmacological behavior, including receptor binding, distribution, metabolism, and elimination. Understanding these properties is fundamental to interpreting clinical data and designing research protocols.
Structural Overview#
PE-22-28 is characterized as: PE-22-28 is a synthetic heptapeptide (Gly-Val-Ser-Trp-Gly-Leu-Arg) corresponding to positions 22-28 of the sortilin propeptide. It was designed from analysis of spadin blood degradation products as the minimal active fragment retaining TREK-1 channel blocking activity with improved potency (IC50 0.12 nM)..
Amino Acid Sequence Details#
The amino acid sequence of PE-22-28 is: GVSWGLR. This sequence determines the peptide's three-dimensional structure, receptor binding properties, and biological activity.
Pharmacokinetic Profile#
Half-Life: ~23 hours (duration of action in mice)
The half-life of a peptide influences dosing frequency, duration of effect, and the clinical utility of the compound. Researchers should consider the half-life when designing experimental protocols.
Related Reading#
Frequently Asked Questions About PE-22-28
What type of peptide is PE-22-28?
PE-22-28 is a synthetic 7-amino acid peptide derived from spadin that potently blocks TREK-1 two-pore domain potassium channels (IC50 0.12 nM). It demonstrates antidepressant-like effects in rodent models including the forced swimming test and novelty suppressed feeding test, and promotes hippocampal neurogenesis after only 4 days of treatment. PE-22-28 has improved stability and duration of action compared to parent spadin.
What is the half-life of PE-22-28?
The reported half-life of PE-22-28 is ~23 hours (duration of action in mice). Half-life can vary depending on the route of administration, formulation, and individual factors. This information is based on available preclinical or pharmacokinetic data.
What is the amino acid sequence of PE-22-28?
The amino acid sequence of PE-22-28 is GVSWGLR. PE-22-28 is a synthetic heptapeptide (Gly-Val-Ser-Trp-Gly-Leu-Arg) corresponding to positions 22-28 of the sortilin propeptide. It was designed from analysis of spadin blood degradation products as the minimal active fragment retaining TREK-1 channel blocking activity with improved potency (IC50 0.12 nM).. This sequence determines its biological activity and binding properties.
How stable is PE-22-28 in storage?
PE-22-28 is typically supplied as a lyophilized powder for maximum stability. PE-22-28 is a synthetic heptapeptide (Gly-Val-Ser-Trp-Gly-Leu-Arg) corresponding to positions 22-28 of the sortilin propeptide. It was designed from analysis of spadin blood degradation products as the minimal active fragment retaining TREK-1 channel blocking activity with improved potency (IC50 0.12 nM).. When reconstituted, it should be stored refrigerated at 2-8 degrees C and protected from light. Lyophilized powder should be stored at -20 degrees C.
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