CCX771

CCX771 is a **highly selective small molecule antagonist** of the human chemokine receptor **CXCR7 (also known as ACKR3)**, with an IC50 of approximately 4.1 nM in binding assays[1][3][5][6]. It was developed and patented by ChemoCentryx for research purposes, and has not reached commercial availability or clinical approval[1]. CCX771 binds and functionally blocks CXCR7, limiting receptor internalization of its endogenous ligands such as CXCL12 and CXCL11, which in turn affects CXCR4 and CXCR3 signaling pathways[3][6]. In preclinical models, CCX771 has demonstrated the ability to inhibit tumor angiogenesis and metastasis, reduce inflammation, improve disease severity in autoimmune encephalitis models, and promote remyelination in models of CNS injury[1][2][3][5][6]. The exact mechanism—agonist versus antagonist properties—remains debated in literature, but functional studies support a primary antagonist effect, particularly impacting CXCL12–CXCR4 biological activity[1][3][6].

Brand names

CCX771CCX-771CCX 771

Other names

CCX771CCX-771CCX 771