ZED3197

ZED3197 (ZED-3197) is a novel peptidomimetic direct-acting, potent and selective inhibitor of human FXIIIa, inhibits human plasma derived FXIII‐A2B2 and the recombinant cellular form (FXIII‐A2) with IC50 of 10 and 14 nM, respectively.ZED3197 strongly blocks FXIII‐A2 from mouse, rat, rabbit, dog, and cynomolgus monkey (IC50 8-30 nM), is a significantly weaker inhibitor of FXIII‐A2 from pig (IC50=220 nM).ZED3197 displays 20‐fold to 3000‐fold selectivity against human transglutaminases TG1, TG2, TG3, and TG7.ZED3197 prolonged clot formation, reduced clot firmness, and facilitated clot lysis in whole human blood without affecting the clotting time, indicating minimal impact on hemostasis.ZED3197 effectively decreased the weight of clots and facilitated flow restoration without prolongation of the bleeding time in vivo.