Pactimibe sulfate is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2) with IC50 values of 4.9 μM and 3.0 μM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells, demonstrating IC50s of 2.0 μM, 2.7 μM, and 4.7 μM, respectively. Pactimibe sulfate also noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM and significantly inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Additionally, it exhibits anti-atherosclerotic properties by reducing plasma cholesterol levels, making it valuable for research in lipid metabolism and cardiovascular disease.
Pactimibe sulfate is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2) with IC50 values of 4.9 μM and 3.0 μM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells, demonstrating IC50s of 2.0 μM, 2.7 μM, and 4.7 μM, respectively. Pactimibe sulfate also noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM and significantly inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Additionally, it exhibits anti-atherosclerotic properties by reducing plasma cholesterol levels, making it valuable for research in lipid metabolism and cardiovascular disease.
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