Pactimibe (sulfate) (Standard)

Pactimibe (sulfate) (Standard) is the analytical standard of Pactimibe (sulfate) (HY-100401A) . This product is intended for research and analytical applications. 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[1]. 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[2].

Product Specifications

CAS Number

[608510-47-0]

Target

Acyltransferase; Reference Standards

Related Pathways

Metabolic Enzyme/Protease; Others

Field of Research

Cardiovascular Disease

Smiles

O=C(O)CC1=C(C)C2=C(N(CCCCCCCC)CC2)C(NC(C(C)(C)C)=O)=C1C.O=S(O)(O)=O.[1/2]

Molecular Formula

C25H40N2O3.1/2H2O4S

Molecular Weight

465.65

References & Citations

[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.|[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.|[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.