产品描述:
Muvalaplin is a trivalent binder of apolipoprotein A (ApoA).{68808} It selectively binds to ApoA kringle domain IV type 8 (KIV8) over KIV2 (IC50s = 22 and 3,900 nM, respectively). Muvalaplin also binds to rat plasminogen (Kd = 50 = 0.09 nM). Muvalaplin decreases plasma levels of lipoprotein A in mice expressing both human ApoA and human ApoB (LPA x ApoB100; ED50 = 3 mg/kg). It reduces plasma levels of lipoprotein A in cynomolgus monkeys when administered at a dose of 100 mg/kg per day. Muvalaplin (31.6 mg/kg for four days) decreases ex vivo plasmin activity and plasminogen levels after administration in rats.