TOP-N53 is a dual-acting nitric oxide (NO) donor and selective PDE5 inhibitor, potently inhibits PDE5 with IC50 of 1.6 nM.
TOP-N53 increased the levels of cGMP in a concentration-dependent and time-dependent manner and was significantly more potent than sildenafil in treated human platelets.
TOP-N53 had no toxic effects on primary mouse fibroblasts and KCs, human blood endothelial cells (BECs), and human HaCaT KCs.
TOP-N53 promotes different parameters of wound healing in healthy mice, does not promote scarring.
TOP-N53 (0.2 nmol per injection day) promotes wound re-epithelialization and angiogenesis in mice with diabetes, directly induces healing-promoting activities in KCs and fibroblasts.
TOP-N53 promotes endothelial cell migration and tube formation in primary human BEC.
