189198-30-9

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

ACAT1: 4.9 μM (IC₅₀); ACAT2: 3.0 μM (IC₅₀); ACAT: 2 μM (IC₅₀, in the liver); ACAT: 2.7 μM (IC₅₀, in macrophages); ACAT: 4.7 μM (IC₅₀, in THP-1 cells); oleoyl-CoA: 5.6 μM (Ki); cholesteryl ester formation: 6.7 μM (IC₅₀)

[1] Naoki Terasaka, et al. ACAT inhibitor pactimibe sulfate (CS-505) reduces and stabilizes atherosclerotic lesions by cholesterol-lowering and direct effects in apolipoprotein E-deficient mice. Atherosclerosis. 2007 Feb;190(2):239-47. DOI:10.1016/j.atherosclerosis.2006.03.007
[2] Ken Kitayama, et al. Importance of acyl-coenzyme A:cholesterol acyltransferase 1/2 dual inhibition for anti-atherosclerotic potency of pactimibe. Eur J Pharmacol. 2006 Jul 1;540(1-3):121-30. DOI:10.1016/j.ejphar.2006.04.022
[3] Yasunobu Yoshinaka, et al. A selective ACAT-1 inhibitor, K-604, stimulates collagen production in cultured smooth muscle cells and alters plaque phenotype in apolipoprotein E-knockout mice. Atherosclerosis. 2010 Nov;213(1):85-91. DOI:10.1016/j.atherosclerosis.2010.08.048