BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 µmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation[1].
Molekulargewicht:
559.70
CAS Nummer:
[457893-92-4]
Formel:
C32H41N5O4
Target-Kategorie:
Melanocortin Receptor
Anwendungsbeschreibung:
MCE Product type: Reference compound
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