5A-aPC

5A-aPC is a molecularly engineered variant of activated protein C (aPC) in which five basic residues (Lys191, Lys192, Lys193, Arg229, and Arg230) are substituted with alanine in two exposed surface loops that comprise part of the factor Va exosite on aPC[2][3]. This design results in a protein that retains full cytoprotective and anti-inflammatory signaling activities—such as PAR1-dependent suppression of LPS-induced TNFα and IL-6 in monocytes, protection against endothelial cell apoptosis, and reduced vascular permeability—but possesses minimal anticoagulant activity (<3% that of wild type aPC, in APTT and PT assays)[2][3][7]. 5A-aPC thus dissociates pharmacological anticoagulant effects from cellular cytoprotective effects, which may be therapeutically valuable for conditions like sepsis or inflammation, where anticoagulation is undesired[2][3].

Other names

5A-APC