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| Catalog Number | CI-BP-0023 |
| Product Name | Pentapeptide-18 |
| CAS | 64963-01-5 |
| Structure |  |
| Synonyms | Consisting of Ala, Gly, Leu, Phe and Tyr. |
| Molecular Weight | 569.28 g/mol |
| Boiling Point | Improve skin wrinkles, hydration, softness |
| Purity | 98% by HPLC |
| Appearance | Lyophilized powder |
| Application | Wrinkle smoothing and skin relaxing |
| Storage | Keep in dark and cool dry place -5~8°C |
Pentapeptide-18, also known as Leuphasyl®, functions as a modulator of calcium channels and offers an innovative approach to reducing expression wrinkles by mimicking the activity of natural enkephalins. These peptides, similar to endogenous opioids, interact with enkephalin receptors located outside neurons, which are linked to inhibitory G proteins. When Pentapeptide-18 binds to these receptors, it triggers a conformational change, leading to the release of G protein subunits (alpha, beta, gamma) within the cell. This intracellular cascade results in the closure of calcium channels and the opening of potassium channels, thereby preventing the entry of calcium into neurons. This action inhibits the fusion of vesicles and subsequent release of acetylcholine at the synapse, ultimately reducing muscle contraction and diminishing the appearance of expression wrinkles.
Park, Jisu, et al. Scientific reports, 2020, 10(1), 262.
The incorporation of D-tyrosine at the terminus of the commercially available anti-wrinkle peptide, pentapeptide-18, enhanced its capacity to decrease melanin levels and inhibit tyrosinase activity in human MNT-1 melanoma cells as well as primary melanocytes. Similarly, the D-tyrosine-modified pentapeptide-18 effectively suppressed melanogenesis triggered by α-MSH treatment or UV exposure in MNT-1 cells and diminished melanin production in the epidermal basal layer of a 3D human skin model.
Experimental methods and results
· Variations of pentapeptide-18 (Leuphasyl, YdAGFL) were synthesized by substituting L-tyrosine with D-tyrosine at the N-terminus or by adding L- or D-tyrosine at the C-terminus. Then human melanoma MNT-1 cells were treated with different doses of these peptides.
· As expected, a 500 μM dose of D-tyrosine lowered the melanin content in MNT-1 cells by approximately 50%. Importantly, both N-D (D-tyrosine at the N-terminus) and C-D (D-tyrosine at the C-terminus) pentapeptide-18 at 500 μM reduced melanin levels and tyrosinase activity in MNT-1 cells by 18% and 25%, respectively.
· Furthermore, both N-D and C-D treatments reduced the expression of tyrosinase and microphthalmia-associated transcription factor (MITF), which are key players in melanin production. L-DOPA staining confirmed that intracellular tyrosinase activity decreased in MNT-1 cells treated with 500 μM of N-D or C-D, with C-D showing reduced tyrosinase activity in vitro.
What is the chemical name of Pentapeptide-18?
The chemical name of Pentapeptide-18 is Leuphasyl.
How does Pentapeptide-18 modulate Ca2+ channels?
Pentapeptide-18 modulates Ca2+ channels by closing them and opening K+ channels.
What is the alternative mechanism of Pentapeptide-18 to Botulinum toxin-like molecules?
Pentapeptide-18 has an alternative mechanism to Botulinum toxin-like molecules in reducing expression wrinkles.
How do natural enkephalins work in inhibiting neuronal activity?
Natural enkephalins inhibit neuronal activity by docking onto receptors outside neurons, which results in the release of inhibiting G protein subunits within the cell. These subunits then close Ca2+ channels and open K+ channels.
How does Pentapeptide-18 act similar to natural enkephalins?
Pentapeptide-18 couples to the enkephalin receptor on the outside of nerve cells, leading to a conformational change and a cascade inside the neuron that decreases its excitability.
What is the result of Pentapeptide-18 modulating the release of acetylcholine?
Modulating the release of acetylcholine with Pentapeptide-18 relaxes muscle contraction, thereby diminishing expression wrinkles.
In which industries is Pentapeptide-18 widely utilized?
Pentapeptide-18 is widely utilized in skincare, cosmetics, and pharmaceutical industries.
What are some of the skin-enhancing benefits of Pentapeptide-18?
Pentapeptide-18 stimulates collagen production, reduces wrinkles, improves skin hydration, and fights free radicals.
What is the purity level of Premium Pentapeptide-18?
Premium Pentapeptide-18 has a purity level of 99%.
What are the common applications of Pentapeptide-18?
Pentapeptide-18 is commonly used in skincare products, cosmetics, and pharmaceuticals.
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