Pactimibe is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2), exhibiting IC50 values of 4.9 µM and 3.0 µM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells with IC50s of 2.0 µM, 2.7 µM, and 4.7 µM. Additionally, Pactimibe noncompetitively inhibits oleoyl-CoA with a Ki of 5.6 µM and reduces cholesteryl ester formation with an IC50 of 6.7 µM. This compound demonstrates significant anti-atherosclerotic potential by lowering plasma cholesterol levels, making it valuable for research in cardiovascular diseases and lipid metabolism.
Pactimibe is a dual inhibitor of acyl-CoA:cholesterol acyltransferase 1 and 2 (ACAT1/2), exhibiting IC50 values of 4.9 µM and 3.0 µM, respectively. It effectively inhibits ACAT activity in liver, macrophages, and THP-1 cells with IC50s of 2.0 µM, 2.7 µM, and 4.7 µM. Additionally, Pactimibe noncompetitively inhibits oleoyl-CoA with a Ki of 5.6 µM and reduces cholesteryl ester formation with an IC50 of 6.7 µM. This compound demonstrates significant anti-atherosclerotic potential by lowering plasma cholesterol levels, making it valuable for research in cardiovascular diseases and lipid metabolism.
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