CCX140 (Ilacirnon, CCX140B) is a potent, selective, orally bioavailable CCR2 antagonist with Kd of 2.3 nM for hCCR2.
CCX140 (CCX140B) displays little to no activity against 142 various biologically important receptor, no effect on plasma levels of the CCR2 ligand CCL2 or on the numbers of blood monocytes.
CCX140 (CCX140B) potently inhibits CCL2-induced chemotaxis of purified human blood monocytes with IC50 of 8 nM, also inhibits CCL2-induced Ca2+ mobilization in monocytes with IC50 of 3 nM.
CCX140 (CCX140B) decreases levels of fasting blood glucose and improves insulin sensitivity in mice.
