Description
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 µM and 3.0 µM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 µM, 2.7 µM, 4.7 µM in the liver, macrophages and THP-1 cells, respectively. Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 µM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 µM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity