Carbenoxolone is a synthetic derivative of glycyrrhizin that exhibits anti-ulcerative, anti-inflammatory, neuromodulatory, neuroprotective, anti-hyperlipidemic, hepatoprotective, and immunosuppressive activities. Carbenoxolone is clinically used to treat ulcers and inflammation; it inhibits 11β-hydroxysteroid dehydrogenase as well as connexins, limiting gap junction communication. In animal models of cerebral ischemia/reperfusion, carbenoxolone decreases infarct volume and neuronal damage. Carbenoxolone also increases NO levels in other animal models, preventing gastric injury. In animal models of experimental autoimmune encephalitis (EAE), carbenoxolone delays disease onset and suppresses production of IL-23 and Th17 cells. In other animal models, this compound decreases levels of triglycerides, free fatty acids, SREBP-1c, LXR, and fatty acid synthase and suppresses hepatocyte apoptosis and inflammatory cytokine expression.