Cayman Spla2 Dtnb; Size- 1 Ea

BMS 470539 is an agonist of melanocortin receptor 1 (MC1R). It induces cAMP accumulation in B16/F10 murine melanoma cells and in CHO cells overexpressing human MC1R (EC₅₀s = 11.6 and 16.8 nM, respectively). It inhibits TNF-α-induced NF-κB activation in vitro in a concentration-dependent manner. In vivo, BMS 470539 inhibits LPS-induced TNF-α production in mice (ED₅₀ = 10 μmol/kg, s.c.). It reduces LPS-induced leukocyte infiltration and paw swelling in mouse models of lung inflammation and delayed-type hypersensitivity, respectively. BMS 470539 decreases retinal damage in a mouse model of streptozotocin-induced diabetic retinopathy. It also increases striatal dopamine levels and decreases the number of striatal α-synuclein aggregates in a mouse model of Parkinson’s disease when administered at a dose of 20 mg/kg.

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