ABT-639 is a novel, peripherally acting, selective T-type Ca2+ channel blocker. ABT-639 blocks recombinant human T-type (Cav3.2) Ca2+ channels in a voltage-dependent fashion (IC50 = 2 M) and attenuates LVA currents in rat DRG neurons (IC50 = 8 M).
ABT-639 is significantly less active at other Ca2+ channels (e.g. Cav1.2 and Cav2.2) (IC50 > 30 M). ABT-639 has high oral bioavailability (%F = 73), low protein binding (88.9%) and a low brain:plasma ratio (0.05:1) in rodents.