Dipeptide-58 D-Phenylalanyl Arginyl D-Tryptophyl Tetrapeptide-90 Amide is a synthetic biomimetic nonapeptide that acts as an antagonist of α‑MSH (melanin‑stimulating hormone). It is optimized for its ability to block MC1‑R receptors on melanocytes. It has a sequence Phe-Val-D-Phe-Arg-D-Trp-Phe-Lys-Pro-Val is known under the trade name Brightening Intide™.
Dipeptide-58 D-Phenylalanyl Arginyl D-Tryptophyl Tetrapeptide-90 Amide repeats key motifs (Phe-Arg-Trp and Lys-Pro-Val) of the α‑MSH. Thanks to the replacement of Phenylalanine3 and Tryptophan5 with their D-forms, it still occupies the MC1-R receptor and prevents its activation, reducing melanin production. Mechanistically, it suppresses cAMP signaling and downstream tyrosinase activity, the enzyme central to melanin production. Moreover, D-form amino acids and many aromatic rings within the molecule enhance its stability against proteolytic enzymes.
According to the manufacturer, Dipeptide-58 D-Phenylalanyl Arginyl D-Tryptophyl Tetrapeptide-90 Amide acts as a skin‑brightening agent without cytotoxicity or disruption of normal melanocyte physiology. It does not completely block melanogenesis, but instead counteracts the hyper‑production of pigment that leads to uneven tone and dark spots.
Incorporated into skin care applications, Dipeptide-58 D-Phenylalanyl Arginyl D-Tryptophyl Tetrapeptide-90 Amide relieves melasma, solar lentigo, freckles, and post‑inflammatory hyperpigmentation. Delivery systems such as liposomes and penetration enhancers ensure effective transport into the skin.