ACAT Inhibitor

Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC₅₀ value of 24.6 μM for rat liver microsomal ACAT activity.

Enniatin B1 is a Fusarium mycotoxin. Enniatin B1 inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 73 μM in an enzyme assay using rat liver microsomes. Enniatin B1 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44/p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.

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. Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a K_i 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.

VULM 1457 is a potent inhibitor of cholesterol acyltransferase (acyl-CoA). VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM 1457 has the potential for the research of diabetes mellitus and hypercholesterolaemia.

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 K_i 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.

Ilekudinol B is an inhibitor of ACAT and PTP1B, with an IC₅₀ of 5.3 μM and a K_i of 11.6 μM against human PTP1B. Ilekudinol B inhibits the classical pathway of the complement system, with an IC₅₀ of 51 μM. Ilekudinol B inhibits TNF-α-induced cellular IL-8 secretion, promotes glucose uptake in skeletal muscle myotubes, and acts as an insulin mimetic and insulin sensitizer. Ilekudinol B can be used in research related to type 2 diabetes, obesity, and inflammatory diseases.

Enniatin B is a Fusarium mycotoxin. Enniatin B inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 113 μM in an enzyme assay using rat liver microsomes. Enniatins B decreases the activation of ERK (p44/p42).

447C88 is an acyl-coenzyme A cholesterol acyltransferase (ACAT) inhibitor with an IC₅₀ of 23 nM. 447C88 can reduce plasma cholesterol levels and can be used in the research of endocrine and metabolic diseases such as hyperlipidemia.

CL-283796 is a potent and orally active acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor. CL-283796 reduces low-density lipoprotein (LDL) cholesterol without affecting cholesterol absorption in African green monkeys. CL-283796 can be used for hypercholesterolemia research.

Phenylpyropene C (S14-95), a JAK/STAT pathway inhibitor, can inhibit IFN-γ mediated expression of the reporter gene (IC₅₀=5.4~10.8 μM). Phenylpyropene C also is an inhibitor of acyl-CoA, with an IC₅₀ of 16.0 μM.

Enniatin A is a Fusarium mycotoxin. Enniatin A inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity with an IC₅₀ of 22 μM in an enzyme assay using rat liver microsomes.