F-1394

F-1394 is a potent, selective, and competitive small molecule inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT). It inhibits the esterification of cholesterol, reducing the formation of foam cells and the development as well as progression of atherosclerotic lesions without affecting circulating serum cholesterol levels. F-1394 exerts its anti-atherogenic effect by acting directly on the arterial wall, and it demonstrates strong efficacy in both prevention and regression models of experimental atherosclerosis. Developed by Fujirebio, it has shown high selectivity and potency with an IC50 of 71 nM in human intestinal cells, and has advanced to early-phase clinical trials for atherosclerosis. It is orally bioavailable and has not been associated with systemic toxicity in preclinical studies[1][2][3][4][5][6][7][8].

Other names

(1S,2S)-2-[3-(2,2-dimethylpropyl)-3-nonylureido]cyclohexane-1-yl 3-[(4R)-N-(2,2,5,5-tetramethyl-1,3-dioxane-4-carbonyl)amino]propionateFujirebio compound F1394