ACT-1004-1239 is a potent, selective, orally available CXCR7 antagonist with IC50 of 3.2 nM (hCXCR7).
ACT-1004-1239 also shows similar potency against rat, mouse and dog CXCR (IC50=2-3 nM), shows high selectivity in a panel of 87 enzymatic and radioligand binding assays (CXCR4, IC50>10 uM).
ACT-1004-1239 is a potent insurmountable CXCR7 antagonist against both CXCL11 and CXCL12, shows a dose-dependent increase of CXCL12 plasma concentration in mice.
