How Melanotan 2 darkens the skin through the action of MC1R?

Apr 06, 2026 Leave a message

Melanotan causes white people to turn black due to its mechanism as a tanning agent. It works as a melanocortin receptor agonist, specifically targeting the melanocortin 1 receptor (MC1R), which plays a key role in skin pigmentation. Here's an explanation:

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Melanotan is a peptide hormone that acts as a melanocortin 1 receptor (MC1R) agonist. MC1R is a G-protein-coupled receptor (GPCR) with seven transmembrane alpha helices, an extracellular domain at the amino-terminus, and an intracellular tail at the carboxyl-terminus. The interaction with Gsα, an activated alpha subunit of the G-protein, triggers signaling processes.

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When MC1R is not bound by a ligand, Gsα binds GDP, and the Gα protein associates with the Gβγ dimer, preventing signal transduction. When MC1R binds to its agonist, its conformation changes, allowing GTP to replace GDP on Gα, which then dissociates from Gβγ and activates signal transduction.

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The agonists for MC1R include melanocyte-stimulating hormone (MSH) and adrenocorticotropic hormone (ACTH), as well as synthetic agents like Melanotan and BMS-470539. These agonists increase melanogenesis (the production of melanin) by activating MC1R.

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Melanocytes do not directly sense UV light; instead, epidermal keratinocytes detect UV exposure. UV exposure activates p53 in keratinocytes, which then upregulates the expression of Pro-opiomelanocortin (POMC), a precursor of MSH. POMC is cleaved by proteases to produce MSH, which then binds to MC1R on melanocytes.

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This binding triggers subsequent signal transduction, including the activation of adenylate cyclase, production of cAMP, and activation of PKA (protein kinase A). PKA phosphorylates CREB (cAMP response element-binding protein) and MITF (Microphthalmia-associated transcription factor), both of which enter the nucleus and upregulate the expression of tyrosinase (TYR) and dopachrome tautomerase (DCT). This results in increased melanin synthesis, darkening the skin and hair.

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Additionally, MC1R signaling is involved in pain perception, red blood cell formation, cartilage development, inflammation, antioxidant activity, DNA repair, and the recovery from membranous glomerulonephritis.

 

If you want to buy Melanotan 2 and would like to learn more, please feel free to contact Xi'an Ruichi. We look forward to hearing from you.

Email: Jenny@ruichibio.com

Reference: https://www.ruichibio.com/lyophilized-peptide/mt2-melanotan-2.html

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