一种ACAT1/2双重抑制剂，对于ACAT1的IC50值为4.9μM，对于ACAT2的IC50值为3.0μM。Pactimibe(CS-505freebase)抑制ACAT，其IC50值在肝细胞中是2.0μM，在巨噬细胞中是2.7μM，在THP-1细胞中是4.7μM。Pactimibe(CS-505freebase)非竞争性抑制oleoyl-CoA，Ki是5.6μM。此外，Pactimibe(CS-505freebase)明显抑制胆固醇酯的形成，IC50是6.7μM。Pactimibe(CS-505freebase)具有抗动脉粥样硬化的潜力，可降低血浆胆固醇的活性。
Pactimibe, also known as CS-505, is a ACAT inhibitor. Pactimibe stabilizes atherosclerotic plaque through macrophage acyl-CoA:cholesterol acyltransferase inhibition in WHHL rabbits. Pactimibe reduces and stabilizes atherosclerotic lesions by cholesterol-lowering and direct effects in apolipoprotein E-deficient mice. Pactimibe inhibits cholesterol absorption from the intestine, reduces cholesteryl ester formation in the liver, and enhances its elimination from the body. The Triton WR-1339 experiment showed that pactimibe inhibited secretion of very low density lipoprotein cholesterol from the liver. These results suggest that pactimibe is likely to have multiple mechanisms of action responsible for its effectiveness in reducing serum cholesterol.
