CV122 is a potent inhibitor of heparanase (heparanase), exhibiting an IC50 of 2.97 µM. This compound inhibits pro-inflammatory cytokines and can be utilized in sepsis research.

CV122 (50 µM) significantly reduces heparanase levels in macrophages stimulated by LPS. Additionally, CV122 (50 µM) effectively inhibits heparanase activity in human umbilical vein endothelial cells (HUVEC), preserves the structure of the cell surface glycocalyx, and decreases the expression of adhesion molecules.

Administered subcutaneously in doses of 20-40 mg/kg, CV122 significantly reduces systemic pro-inflammatory cytokine levels, thus preventing organ damage and enhancing vitality, thereby protecting mice from sepsis-induced mortality. Mechanistically, CV122 inhibits heparanase activity, decreases its expression in the lungs, and preserves the structural integrity of lung glycocalyx. Additionally, a dosage of 20 mg/kg of CV122 effectively shields mice from both organ damage and death caused by Crimean-Congo Hemorrhagic Fever Virus (CCHFV) infections. In an animal model involving C57BL/6J male mice aged 6-8 weeks and weighing 20-25 g, those injected with 40 mg/kg of LPS showed that CV122 could significantly improve survival in a dose-dependent manner when administered at doses of 20, 30, and 40 mg/kg.