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
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Disclaimer: For educational purposes only. Not medical advice. Read full disclaimer