RS504393

RS504393 is a highly selective small molecule antagonist of the chemokine receptor CCR2 (C-C chemokine receptor type 2). It was identified from a chemical library screen for its potent inhibition of CCR2 with high specificity, exhibiting an IC₅₀ of 98 nM for human recombinant CCR2b and >100 μM for the related CCR1 receptor[1][8]. RS504393 effectively blocks chemotaxis mediated by monocyte chemoattractant protein-1 (MCP-1 or CCL2) and has been widely used in preclinical research to assess the pharmacological effects of CCR2 inhibition in various inflammatory and immune-mediated diseases. Its primary mechanism is to inhibit the recruitment and infiltration of CCR2-positive monocytes/macrophages and reduce inflammatory signaling in target tissues[1][2][4][5]. RS504393 has shown efficacy in animal models of mitral valve disease with Marfan syndrome, rheumatic heart disease, neuroinflammation following subarachnoid hemorrhage, and immunoregulatory effects in cancer settings, including reduce macrophage and myeloid-derived suppressor cell infiltration[1][2][4][5]. RS504393 is not a marketed pharmaceutical product and has no current clinical development status, but serves as a research tool for the study of CCR2-related pathways[7][8].

Other names

6-methyl-1'-[2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl]-1,2-dihydrospiro[3,1-benzoxazine-4,4'-piperidine]-2-one6-methyl-1'-(2-(5-methyl-2-phenyl-1,3-oxazol-4-yl)ethyl)-1,2-dihydrospiro(3,1-benzoxazine-4,4'-piperidine)-2-one6-Methyl-1'-(2-(5-methyl-2-phenyloxazol-4-yl)ethyl)spiro[benzo[d][1,3]oxazine-4,4'-piperidin]-2(1H)-one6-Methyl-1'-[2-(5-methyl-2-phenyl-4-oxazolyl)ethyl]spiro[4H-3,1-benzoxazine-4,4'-piperidin]-2(1H)-one[7]