Bindarit is an inhibitor of monocyte chemoattractant protein (MCP) production that is selective for MCP-1/CCL2, MPC-3/CCL7, and MCP-2/CCL8 over other chemokines.
1 It inhibits LPS- or
C. albicans-induced production of MCP-1/CCL2 in isolated human monocytes (IC
50s = 172 and 403 μM, respectively).
2 Bindarit downregulates NF-κB signaling and prevents p65 and p65/p50-mediated MCP-1/CCL2 promoter activation in RAW264.7 cells.
3 It delays the onset of proteinuria and prolongs survival in a mouse model of experimental lupus nephritis when administered at a dose of 50 mg/kg.
4 It prevents LPS-induced increases in MCP-1/CCL2 expression in mouse brain and spinal cord when administered at a dose of 200 mg/kg and reduces the incidence and severity of experimental autoimmune encephalomyelitis (EAE) in mice.
5 Bindarit is also a noncompetitive inhibitor of monocarboxylate transporter 4 (MCT4; K
i = 30.2 μM for the human transporter) that is selective for MCT4 over MCT1.
6 
