cholesterol acyltransferase

VULM 1457 是有效的胆固醇酰基转移酶抑制剂，具有显著的降血脂活性，并改善了整体心肌缺血再灌注损伤结果。VULM 1457 显著降低肾上腺髓质素的产生和分泌，并下调人肝母细胞上的 AM 受体。VULM 1457 具有研究糖尿病和高胆固醇血症的潜力。

OSMI-1 是一种 O-GlcNAc 转移酶 (OGT) 抑制剂 (IC50=2.7 μM)，具有口服活性和细胞渗透性。OSMI-1 可以抑制蛋白质 O-GlcNA 酰化，而不会定性地改变细胞表面 N- 或 O- 连接的聚糖。

Xanthohumol 是从啤酒花中分离到的黄酮类化合物，可抑制 COX-1 和 COX-2 活性，具有抗肿瘤，抗血管生成的作用，还具有抗多种病毒的活性。

2-Furoic acid (Furan-2-carboxylic acid) 2-Furoic acid 能够降低血清中胆固醇和甘油三酯的水平，具有抗血脂作用。

Avasimibe (PD-148515) 是一种口服有效的酰基辅酶 A: 胆固醇酰基转移酶 (ACAT) 抑制剂，对 ACAT1和 ACAT2的 IC50分别为 24 和 9.2 µM。Avasimibe 在前列腺癌中有研究的价值。

K-604 dihydrochloride 是酰基辅酶 A：胆固醇酰基转移酶 1 的选择性抑制剂，IC50为 0.45±0.06 μM。

Nevanimibe hydrochloride (PD-132301 hydrochloride) 是一种口服有效的，选择性酰基辅酶 A：胆固醇 O-酰基转移酶 1 抑制剂，EC50为 9 nM。它抑制 ACAT2，EC50为 368 nM。它诱导细胞凋亡，具有抗肾上腺皮质癌的潜力。

PF-06424439 methanesulfonate 是一种口服有效咪唑并吡啶二酰基甘油酰基转移酶 2 (DGAT2)选择性抑制剂，IC50是14 nM。PF-06424439 methanesulfonate 具有缓慢可逆，时间依赖性的特点，其相对于酰基-CoA 底物以非竞争性模式抑制 DGAT2。

Glabrol 是分离自甘草根的乙醇提取物中的一种异戊二烯类黄酮，是一种有效且非竞争性的酰基辅酶 A：胆固醇酰基转移酶（ACAT）抑制剂，抑制大鼠肝脏微粒体 ACAT 的IC50为 24.6 μM。

Lecimibide (DuP 128) 是一种有效且具有选择性的酰辅酶 A 胆固醇酰基转移酶(ACAT)抑制剂，可用于研究由于高脂带来的疾病。

Eflucimibe (L0081) 是一种酰基辅酶A：胆固醇酰基转移酶抑制剂，可用于治疗心血管疾病和内分泌与代谢疾病，可用于研究动脉粥样硬化和高脂血症。

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.

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 crosss the blood-brain barrier. Enniatin B1 decreases the activation of ERK (p44 p42). Enniatin B1 inhibits moderately TNF-α-induced NF-κB activation.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.

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

KY-455为新型酰基辅酶A：胆固醇酰基转移酶（ACAT）抑制剂。该化合物在抑制兔肠道、肝脏、巨噬细胞及肾上腺中的ACAT活性方面表现出效力，其IC50值依次为0.4、0.9、2.9和4.1 μmol L。

YM-750 是一种有效的酰基:胆固醇酰基转移酶(ACAT)抑制剂，IC50为0.18 μM。

Guineesine is an Acyl-CoA. It acts by inhibiting cholesterol acyltransferase.

Acaterin, an inhibitor of acyl-CoA: cholesterol acyltransferase (ACAT), inhibits synthesis of cholesteryl ester in macrophage J774.

SMP-797 HCl, an ACAT (acyl-CoA-cholesterol acyltransferase) inhibitor, is used potentially for the treatment of Hyperlipidemia.

AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol. Oleic acid-2,6-diisopropylanilide is an inhibitor of acylCoA:cholesterol acyltransferase with an IC50 of 7 nM. When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide decreased low density lipoproteins and elevated high density lipoprotein levels when administered at 0.05%.

Acyl-coenzyme A: cholesterol acyltransferase-1 and -2 (ACAT-1 and ACAT-2) catalyze the formation of cholesterol esters from cholesterol and long chain fatty acyl-coenzyme A, and may play a role in the development of atherosclerosis. CAY10485 inhibits human ACAT-1 and ACAT-2 with an IC50 values of 95 and 81 μM, respectively. It also inhibits copper-mediated oxidation of low density lipoproteins by 91% at a concentration of 2 μM.

Beauveriolide I is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.78 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide I also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 6 μM).2 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)

Beauveriolide III is a cyclodepsipeptide that has been found inBeauveriaand an inhibitor of lipid droplet formation.1It inhibits lipid droplet formation when used at concentrations of 3 and 10 μM, as well as inhibits cholesterol synthesis (IC50= 0.41 μM), in primary mouse peritoneal macrophages.1,2Beauveriolide III also inhibits acyl-coenzyme A:cholesterol acyltransferase (ACAT) activity in mouse macrophage membranes (IC50= 5.5 μM).2Beauveriolide III (25 and 50 mg kg) reduces the size of aortic atherosclerotic lesions inLdlr- -andApoE- -mouse models of atherosclerosis. 1.Namatame, I., Tomoda, H., Si, S., et al.Beauveriolides, specific inhibitors of lipid droplet formation in mouse macrophages, produced by Beauveria sp. FO-6979J. Antibiot. (Tokyo)52(1)1-6(1999) 2.Namatame, I., Tomoda, H., Ishibashi, S., et al.Antiatherogenic activity of fungal beauveriolides, inhibitors of lipid droplet accumulation in macrophagesProc. Nat. Acad. Sci. USA101(3)737-742(2004)