BMS-470539 is a synthetic agonist of the melanocortin-1 receptor (MC-1R), notable for its potent anti-inflammatory properties. With EC50 values of 16.8 nM and 11.6 nM for human and murine MC-1R activation respectively, it effectively inhibits TNF-alpha-induced NF-kB activation in human melanoma cells. In vivo studies demonstrate that subcutaneous administration of BMS-470539 in BALB/c mice significantly reduces LPS-induced TNF-alpha production, leukocyte infiltration in lung inflammation, and paw swelling in delayed-type hypersensitivity models, indicating its potential as a therapeutic agent targeting inflammation through MC-1R modulation.
BMS-470539 is a synthetic agonist of the melanocortin-1 receptor (MC-1R), notable for its potent anti-inflammatory properties. With EC50 values of 16.8 nM and 11.6 nM for human and murine MC-1R activation respectively, it effectively inhibits TNF-alpha-induced NF-kB activation in human melanoma cells. In vivo studies demonstrate that subcutaneous administration of BMS-470539 in BALB/c mice significantly reduces LPS-induced TNF-alpha production, leukocyte infiltration in lung inflammation, and paw swelling in delayed-type hypersensitivity models, indicating its potential as a therapeutic agent targeting inflammation through MC-1R modulation.
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