Razuprotafib sodium

Razuprotafib (AKB-9778) sodium is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC₅₀of 17 pM. Razuprotafib sodium promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib sodium inhibits the structurally related phosphatase PTP1B with an IC₅₀ of 780 nM. Razuprotafib sodium shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC₅₀=36 pM) and HPTPγ (100 pM).

• Data Sheet (273 KB)