Product Data Sheet

BMS-470539

Catalog No. A61682

main product photo
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.
Chemical Information
Catalog NumA61682
M. Wt559.70
FormulaC32H41N5O4
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.457893-92-4
Synonyms
SMILESCCCC(C1(C2=CC=CC=C2)CCN(C([C@@H](CC3=CC=C(C=C3)OC)NC([C@H](CC4=CN=CN4C)N)=O)=O)CC1)=O
Biological Activity
DescriptionBMS-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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