CXCR7 modulator 18 is a novel potent, selective CXCR7 modulator with Ki of 13 nM, β-arrestin EC50 of 11 nM.
CXCR7 modulator 18 demonstrates excellent selectivity profile adrenergic α1a Kb >10 ,000 nM, and adrenergic β2 Kb, CXCR4 Ki >1 uM.
Administration of CXCR7 modulator 18 in mice led to a statistically significant increase in circulating concentrations of plasma stromal-cell-derived factor 1α (SDF-1α) of approximately 2-fold.
Chronic dosing of compound 18 in a mouse model of isoproterenol-induced cardiac injury further resulted in a statistically significant reduction of cardiac fibrosis.
