DermaPep™ W411 is a peptide-based complex that contains Methyl Undecenoyl Leucinate, a Melanocortin 1 Receptor (MC1R) antagonist, and Palmitoyl hexapeptide-36, Endothelin Receptor Type B (ETBR) antagonist, with a synergic suppressing effect on melanin production.
It is well known that skin pigmentation is mainly affected by three major signaling pathways: α-MSH/MC1R, ET-1/ETBR, and SCF/c-kit. Despite the identification of several pathways involved in human pigmentation, the Melanocortin-1 receptor (MC1R) has consistently been a representative determinant of pigmentation phenotype.
Another important pathway affecting human pigmentation besides α-MSH/MC1R is ET-1/ETBR. Endothelin has been identified as a potent stimulator of human melanocyte proliferation and differentiation. Endothelin is indeed secreted by keratinocytes and stimulated by UVB radiation to evoke a melanocyte response characterized by proliferation and melanogenesis. In addition, Endothelins have also been implicated in the development of melanocyte dendricity.
In vitro study results showed that both actives in DermaPep™ W411 effectively inhibit UV-induced expression and production of tyrosinase, tyrosinase activity, and finally melanin production.Methyl undecenoyl leucinate, an active ingredient of DermaPep™ UL, binds strongly to the MC-1 receptor, thereby antagonizing the α-MSH effects, and Palmitoyl hexapeptide-36, an active ingredient of DermaPep™ W650, binds to the ETB receptor, thereby antagonizing ET-1 effects. Both peptides act synergistically to inhibit MITF expression, downregulate melanogenic gene expression, and ultimately suppress melanin production.
