BCX-1470 methanesulfonate is a potent serine protease inhibitor that inhibits the esterolytic activity of factor D (IC50=96 nM) and C1s (IC50=1.6 nM).
BCX-1470 methanesulfonate displays 3.4-fold and 200-fold bette than that of trypsin, respectively.
BCX-1470 methanesulfonate inhibits esterolytic activity translates into potent inhibition of the proteolytic activity of C1s, factor D, and consequently of the classical and alternative pathway-mediated hemolysis of target RBC (IC50=46 nM and 330 nM, respectively).
BCX-1470 methanesulfonate blocks the reverse passive Arthus (RPA) reaction in rats.
