INCB3284

INCB3284 is a potent, selective, and orally bioavailable small molecule antagonist of the chemokine receptor CCR2 (C-C motif chemokine receptor 2). It was developed by Incyte for the treatment of chronic inflammatory diseases such as rheumatoid arthritis and insulin resistance. The drug acts by inhibiting the binding of monocyte chemoattractant protein-1 (MCP-1/CCL2) to CCR2, thereby blocking downstream signaling pathways involved in inflammation and immune response. INCB3284 demonstrated high selectivity for CCR2 with an IC50 value of approximately 3.7 nM for antagonism of MCP-1 binding and showed acceptable oral bioavailability in preclinical species as well as humans. Clinical trials reached Phase II for rheumatoid arthritis and insulin resistance but were discontinued[1][3][5][6][7].

Other names

4-Aldoximino-2,2,5,5-tetramethyl-3-imidazoline3-oxide1-oxyl