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Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor, acting on ACAT1 (IC50: 4.9 μM) and ACAT2 (IC50: 3.0 μM). Pactimibe sulfate inhibited oleoyl-CoA non-competitively (Ki: 5.6 μM) and significantly inhibited cholesterol ester formation (IC50: 6.7 μM). Pactimibe sulfate reduces plasma cholesterol activity and has anti-atherogenic potential.