Leuphasyl¶
Identification¶
| Property | Value |
|---|---|
| CAS Number | — (Pentapeptide-18) |
| Molecular Formula | C₃₃H₄₅N₅O₈ |
| Molecular Weight | ~623.7 Da |
| Sequence | Tyr-D-Ala-Gly-Phe-Leu-OH |
| Amino Acid Count | 5 (D-Ala² substitution) |
| Appearance | White to off-white lyophilized powder |
| Purity Standard | ≥99% by HPLC |
| Solubility | Soluble in sterile water; cosmetic formulation-compatible |
| Storage | 2–8°C, desiccated, protect from light |
Category: Cosmetic & Skin
Catalog SKU: PSH-LEUPH-10MG
Research Background¶
Leuphasyl (Pentapeptide-18) is a synthetic enkephalin analogue pentapeptide featuring a D-Ala² substitution that confers resistance to enzymatic degradation. Unlike Snap-8 and Argireline — which target SNARE-mediated vesicle docking — Leuphasyl operates through a fundamentally different mechanism: δ-opioid receptor (DOR) agonism leading to modulation of voltage-gated calcium channels. This reduces neuronal calcium influx, which in turn decreases acetylcholine release at the neuromuscular junction.
Key Mechanisms¶
| Mechanism | Details |
|---|---|
| δ-Opioid Receptor Agonism | Enkephalin analogue → δ-opioid receptor (DOR) activation → reduced neuronal excitability |
| Ca²⁺ Channel Modulation | DOR-mediated inhibition of voltage-gated calcium channels → reduced calcium influx |
| ACh Release Reduction | Decreased intracellular Ca²⁺ → reduced vesicular acetylcholine release at NMJ |
Research Focus Areas¶
Fine Lines¶
Periorbital and perioral fine line reduction in topical models
Muscle Tone Modulation¶
Calcium channel-mediated smooth muscle relaxation
Expression Modulation¶
Enkephalin receptor-mediated neuromuscular signaling
Cosmetic Formulations¶
Topical delivery of enkephalin analogue peptides
Available Configurations¶
| Configuration | Content | Best For |
|---|---|---|
| Standard Kit | 10 mg × 10 vials | Fine line models; evaluation |
| Bulk Kit | 50 mg × 10 vials | Product development; pilot batches |
| Custom | Custom mg × custom vials | OEM; private-label cosmetics |
Tiered Wholesale Pricing¶
| Volume | Discount | For |
|---|---|---|
| 1 kit | List price | Evaluation; competitive analysis |
| 5+ kits | 10% off | Initial portfolio expansion |
| 20+ kits | 20% off | Mid-size distributors |
| 50+ kits | 30% off | Regional distributors |
Quality Specifications¶
| Parameter | Method | Criterion |
|---|---|---|
| Purity | HPLC at 214 nm, C18 column | ≥99.0% peak area |
| Identity (MW) | ESI-MS | ~623.7 ± 1.0 Da |
| Appearance | Visual inspection | White to off-white powder |
| Peptide Content | Amino acid analysis | ≥80% net peptide |
| Residual Moisture | Karl Fischer | ≤3% |
Frequently Asked Questions¶
Q1: What is Leuphasyl and how does it work?¶
Leuphasyl (Pentapeptide-18) is a synthetic enkephalin analogue pentapeptide with a D-Ala² substitution. It activates δ-opioid receptors, which modulate voltage-gated calcium channels — reducing calcium influx and consequently decreasing ACh release at the NMJ.
Q2: How does Leuphasyl differ from Snap-8 and Argireline?¶
Mechanistically: Leuphasyl targets opioid receptors → calcium channel modulation. Snap-8 and Argireline target SNARE complex → vesicle docking inhibition. Leuphasyl is preferred for fine line models; Snap-8/Argireline for deeper expression lines.
Q3: What does the D-Ala² substitution do?¶
The D-Ala² substitution replaces natural L-Ala with D-Ala, conferring resistance to aminopeptidase degradation. This significantly extends half-life compared to natural enkephalins, making it viable for topical formulation research.
Q4: Is Leuphasyl stable in topical formulations?¶
Yes. As a short pentapeptide (~623.7 Da), Leuphasyl shows good stability at pH 5.0–7.0. Small size facilitates stratum corneum penetration in topical models.
Q5: What is the standard purity specification?¶
≥99% by HPLC with ESI-MS identity. The D-Ala² substitution is verified by chiral amino acid analysis. Batch-specific COA included.
Key Research References¶
| Reference | PMID | Key Finding |
|---|---|---|
| Gorouhi F & Maibach HI. "Role of topical peptides in preventing or treating aged skin." Int J Cosmet Sci. 2009;31(5):327–345. | 19570099 | Review of cosmetic peptides including Leuphasyl (Pentapeptide-18); enkephalin-derived δ-opioid mechanism for anti-wrinkle research |
| Lupo MP & Cole AL. "Cosmeceutical peptides." Dermatol Ther. 2007;20(5):343–349. | 18045359 | Comprehensive review of cosmetic peptides including Leuphasyl as δ-opioid receptor agonist; mechanism distinct from SNARE-targeting peptides |
Stability & Storage¶
| Condition | Degradation Profile |
|---|---|
| Lyophilized Storage | Standard peptide stability; 24 months at 2–8°C in desiccated environment, protect from light |
| D-Ala² Stability | D-Ala² substitution confers resistance to aminopeptidase degradation; significantly extended half-life vs natural enkephalins |
| Neutral pH (5.0–7.0) | Stable; compatible with cosmetic formulation conditions. Small pentapeptide (~624 Da) with good stratum corneum penetration |
| Reconstituted Solution | 24 h at 2–8°C; aliquot and freeze at −20°C for extended use. Avoid repeated freeze-thaw |
Source & Purchase¶
For research-grade LEUPHASYL and related compounds in this category, visit the PeptideSourceHub category page for bulk pricing and available specifications.
Browse LEUPHASYL & Related Products →
Related Products¶
| Product | Link |
|---|---|
| Argireline (Acetyl Hexapeptide-8) | argireline.md — SNARE complex inhibitor |
| Snap-8 (Acetyl Octapeptide-3) | snap-8.md — SNAP-25 competition peptide |
| Matrixyl (Palmitoyl Pentapeptide-4) | matrixyl.md — Matrikine signaling for collagen synthesis |
| GHK-Cu (Copper Tripeptide) | ghk-cu.md — Copper peptide for wound healing |