ACAT

ACAT-IN-1 cis isomer is a potent ACAT inhibitor (IC50: 100 nM) used for the study of immune system-related diseases.

Lecimibide (DuP 128) is a potent and selective inhibitor of acyl coenzyme A:cholesterol acyltransferase (ACAT), useful for studying high-lipid-related diseases.

Monatepil maleate (AJ-2615 maleate) is an orally active Ca2+-channel and α1-adrenoceptor antagonist and non-competitive heparanoyl-coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with antihypertensive activity.Monatepil maleate is used in studies of hyperlipidemia and atherosclerosis. Monatepil maleate is used to study hyperlipidemia and atherosclerosis.

Monatepil 2maleate is an orally active Ca2+-channel antagonist and ACAT inhibitor with alpha(1)-adrenergic receptor blocking activity and antiarrhythmic properties that inhibit vasoconstriction.Monatepil 2maleate may be used to study atherosclerosis.

TMP-153 is a novel and potent ACAT inhibitor with an IC50 value of 5-10 nM for intestinal and hepatic ACAT in animals.TMP-153 has a hypocholesterolemic effect, inhibiting cholesterol uptake and lowering plasma cholesterol in rats and hamsters.

Cyclandelate (BS 572), a direct-acting smooth muscle relaxant, is used to dilate blood vessels.

Rimonabant (SR141716) is an inverse agonist for the cannabinoid receptor CB1. It is an anorectic anti-obesity drug produced and marketed by Sanofi-Aventis. Its main avenue of effect is a reduction in appetite. Rimonabant is the first selective CB1 receptor blocker to be approved for use anywhere in the world. Rimonabant is approved in 38 countries including the E.U., Mexico, and Brazil. It was rejected for approval for use in the United States.

VULM 1457 is a potent ACAT inhibitor. VULM 1457 has remarkable hypolipidaemic activity and improves the overall myocardial ischaemia-reperfusion injury outcomes. VULM1457 significantly reduces production and secretion of adrenomedullin (AM) and down-regulates AM receptors on human hepatoblastic cells.

Lateritin (Bassiatin) is An Acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor and a platelet aggregation inhibitor from the mycelial cake of Gibberella lateritium. Bassiatin is the (3S,6R) isomer.

RP 70676 is a potent ACAT inhibitor(rat and rabbit ACAT with IC50 of 25 and 44 nM ).

YM17E is an inhibitor of ACAT with IC50 of 44 nM in rabbit liver microsomes in vitro.

Enniatin A, a Fusarium mycotoxin, inhibits acyl-CoA: cholesterol acyltransferase (ACAT) with an IC50 of 22 μM in rat liver microsome enzyme assays.

Enniatins B decreases the activation of ERK (p44/p42). 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.

Enniatin B1, a Fusarium mycotoxin, crosses the blood-brain barrier, decreases the activation of ERK (p44/p42), and inhibits moderately TNF-α-induced NF-κB activation. Furthermore, it inhibits acyl-CoA: cholesterol acyltransferase (ACAT) activity, exhibiting an IC50 of 73 μM in rat liver microsome enzyme assays.

Beauvericin, a Fusarium mycotoxin, inhibits acyl-CoA:cholesterol acyltransferase (ACAT) in rat liver microsomal enzyme assays with an IC50 value of 3 μM.

E-5324 is potent cholesterol acyltransferase (ACAT) inhibitor (IC50s: 44 to 190 nM).

FR-190809 is a nonadrenotoxic and orally efficacious inhibitor of acyl-CoA:cholesterol O-acyltransferase (ACAT) (IC50: 45 nM).

PD 128042 (CI 976) is a potent, orally active, and selective ACAT inhibitor (IC50: 73 nM) as well as a lysophospholipid acyltransferase (LPAT) inhibitor. CI 976 inhibits Golgi-associated LPAT activity (IC50: 15 μM) and multiple membrane trafficking steps.

YM-750 is a potent inhibitor of acyl-CoA:cholesterol acyltransferase (ACAT), with an IC50 value of 0.18 μM. ACAT is an enzyme that catalyzes the conversion of cholesterol and long-chain fatty-acyl-coenzyme A into cholesteryl esters.

Avasimibe (PD-148515) is an orally bioavailable inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT, IC50: 3.3 μM) that prevents cholesterol deposition in the arterial wall. It also inhibits human P450 isoenzymes CYP2C9/1A2/2C19 (IC50: 2.9/13.9/26.5 μM).

RP-64477 is the cholesterol esterifying enzyme Acyl-coenzyme A:cholesterol O-acyltransferase (ACAT) inhibitor.

ACAT-IN-10 dihydrochloride is a compound that serves as an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT).ACAT-IN-10 dihydrochloride effectively hampers NF-κB mediated transcription, albeit to a lesser extent.

ACAT-IN-5 (example 19) is an inhibitor of acyl-Coenzyme A: cholesterol acyltransferase (ACAT) that effectively suppresses NF-κB-mediated transcription.

ACAT-IN-8 (example 206) is a compound that inhibits acyl-Coenzyme A: cholesterol acyltransferase (ACAT), an enzyme involved in cholesterol modulation, and also inhibits NF-κB-mediated transcription.