VC108

VC108 is a selective small molecule antagonist of the G protein-coupled receptor 39 (GPR39), currently in preclinical development for the treatment of cardiovascular and cerebrovascular diseases. GPR39 is expressed in vascular smooth muscle cells, pericytes, and cardiomyocytes, where its activation by the endogenous agonist 15-hydroxyeicosatetraenoic acid (15-HETE) triggers vasoconstriction and reduces perfusion. VC108 acts by blocking this receptor, thereby increasing coronary blood flow and inducing maximal coronary hyperemia. Beyond its vasodilatory properties, VC108 has demonstrated the ability to significantly reduce infarct size in animal models of stroke (middle cerebral artery occlusion) and myocardial infarction, suggesting a direct cytoprotective effect on tissues that may involve the inhibition of cell death pathways such as ferroptosis, apoptosis, or necrosis.