Date published: 2025-11-21

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MC1-R Inhibitors

MC1-R inhibitors are a diverse group of molecules that modulate the activity of melanocortin 1 receptor (MC1-R), a G protein-coupled receptor involved in skin pigmentation. These inhibitors function by either competing with natural ligands for receptor binding or by interfering with the receptor's ability to activate downstream signaling pathways. The primary role of MC1-R in melanogenesis makes these inhibitors crucial for understanding and modulating pigmentation processes. Synthetic antagonists like SHU 9119, ML00253764, ML00253765, BMS-470539, and LY2112688 are designed to mimic the action of natural antagonists. These compounds bind to MC1-R and block its activation by natural ligands. By inhibiting MC1-R, these molecules reduce the signaling through pathways that lead to increased melanin synthesis.

Overall, MC1-R inhibitors, whether natural or synthetic, play a crucial role in regulating skin pigmentation. Their ability to modulate MC1-R activity presents avenues for addressing pigmentation-related disorders. These inhibitors function primarily by competing with natural ligands for receptor binding or by interfering with the receptor's signaling mechanisms. The diverse nature of these compounds, ranging from proteins and peptides to small molecules, underscores the complex regulatory mechanisms governing MC1-R activity and its pivotal role in melanogenesis. The study of these inhibitors not only enhances our understanding of pigmentation processes and opens up possibilities for further research in pigmentation disorders.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

BMS 470539 dihydrochloride

457893-92-4sc-362716
sc-362716A
sc-362716B
10 mg
50 mg
100 mg
$428.00
$1714.00
$3264.00
4
(0)

BMS-470539 is a selective antagonist of MC1-R. It inhibits MC1-R by binding to the receptor and preventing its activation by natural agonists, thus affecting the signaling pathways that lead to melanin production.