TA-7552 is a potent cholesterol-lowering agent. When TA-7552 is mixed with unsupplemented CLEA CE-2 powder in a concentration of 0.05% and administered to rats for 7 days, TA-7552 does not reduce the normal level of serum cholesterol. The hypocholesterolemic effect of TA-7552 is apparent at the lowest concentration (0.01%) of the drug in the diet, corresponding to a daily dose of ~10 mg/kg body weight, and maximal at the highest concentration of 0.2% TA-7552, lowering serum total cholesterol by 72% while elevating serum HDL cholesterol by 88%. TA-7552 also dose dependently suppresses this rise of hepatic cholesterol, and its lowering rate at the maximal dose is 90%.