An MC1R agonist
BMS 470539 is an agonist of melanocortin receptor 1 (MC1R) with EC50 values of 16.8 and 11.6 nM for human and murine MC1R, respectively, in a cAMP accumulation assay. [1] It inhibits TNF-α-induced NF-κB activation in vitro in a dose-dependent manner. In vivo, subcutaneous administration of BMS 470539 inhibits LPS-induced TNF-α production in wild-type mice (ED50 = 10 μmol/kg). It reduces LPS-induced leukocyte infiltration and paw swelling in mouse models of lung inflammation and delayed-type hypersensitivity, respectively. BMS 470539 administration also decreases retinal damage in a mouse model of streptozotocin-induced diabetic retinopathy. [2]
Reference:
[1]. Kang, L., McIntyre, K.W., Gillooly, K.M., et al. A selective small molecule agonist of the melanocortin-1 receptor inhibits lipopolysaccharide-induced cytokine accumulation and leukocyte infiltration in mice. J. Leukoc. Biol. 80(4), 897-904 (2006).
[2]. Rossi, S., Maisto, R., Gesualdo, C., et al. Activation of melanocortin receptors MC1 and MC5 attenuates retinal damage in experimental diabetic retinopathy. Mediators Inflamm.
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