acyl-coenzyme

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。

Acyl coenzyme A synthetase (ACS)，一种生化研究中常用的酶，主要通过两步硫酯化反应激活脂肪酸与辅酶A结合，形成酰基辅酶A。该过程为脂质代谢中的多种合成与分解代谢途径，以及参与TCA循环中的有氧呼吸提供了关键中间物。

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。

CL 277082 (Ddpmhu) 是一种酰基辅酶A：胆固醇O-酰基转移酶抑制剂，抑制肉芽肿组织 ACAT 活性。

Erucic acid (13(Z)-Docosenoic Acid) 是单不饱和脂肪酸，分离自萝卜的种子。Erucic acid 可以容易地穿过血脑屏障，使大脑中长链脂肪酸的积累正常化。Erucic acid 能够改善认知障碍并有效预防痴呆。

2-Hydroxyoctanoic acid 是中链酰基辅酶 A 合成酶抑制剂 (Ki:500 μM)。

Coenzyme A 是所有活细胞中必需的辅助因子，由泛酸，三磷酸腺苷和半胱氨酸合成的。Coenzyme A 与过氧化物酶 5 共价结合导致其过氧化物酶活性完全抑制，通过 DTT 还原能够逆转。Coenzyme A 及其硫酯衍生物是主要分解代谢，合成代谢途径和基因表达调控的关键参与者。

Nevanimibe is an orally active and selective inhibitor of acyl-coenzyme A:cholesterol O-acyltransferase 1 (ACAT1) (EC50 of 9 nM).

Pyripyropene A is a potent and selective inhibitor of sterol O-acyltransferase 2 (SOAT2) acyl-coenzyme A:cholesterol acyltransferase 2 (ACAT2)(IC50 of 0.07 µM).

Triacsin C (WS 1228A) 来自金黄色链霉菌 (Streptomyces aureofaciens) ，是一种花生四烯酰辅酶A合成酶和非特异性长链酰辅酶A合成酶的差异抑制剂，抗动脉粥样硬化活性，抑制 ACSL 活性， 抑制 TAG 积聚成脂滴 (LD) 。Triacsin C 可用于研究轮状病毒感染和阿尔茨海默症。

Pentanoyl Coenzyme A (pentanoyl-CoA) Free acid 是短链脂肪酰辅酶 A，也是 3-氧代丙酰辅酶 A 的代谢产物。

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。

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。

Lauroyl-coenzyme A can function as an acyl group carrier, acetyl-CoA. It can be used as an intermediate in lipid metabolism and is involved in lipid biosynthesis and fatty acid transport.

Linoleoyl-coenzyme A is a substrate used to investigate the specificity and kinetics of acyl-CoA.

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)

Terpendole I is a fungal metabolite that has been found in A. yamanashiensis.1 It is a weak inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 145 μM) and is active against the bacteria B. cereus and B. subtilis (MICs = 100 μg/ml for both) but not S. aureus, P. aeruginosa, or K. pneumoniae (MICs = >200 μg/ml for all) or the fungus C. albicans (MIC = 200 μg/ml).1,2 It is cytotoxic to HeLa cells with an IC50 value of 52.6 μM.3 |1. Tomoda, H., Tabata, N., Yang, D.-J., et al. Terpendoles, novel ACAT inhibitors produced by Albophoma yamanashiensis. III. Production, isolation and structure elucidation of new components. J. Antibiot. (Tokyo) 48(8), 793-804 (1995).|2. Zhao, J.-C., Wang, Y.-L., Zhang, T.-Y., et al. Indole diterpenoids from the endophytic fungus Drechmeria sp. as natural antimicrobial agents. Phytochemistry 148, 21-28 (2018).|3. Nagumo, Y., Motoyama, T., Hayashi, T., et al. Structure-activity relationships of terpendole E and its natural derivatives. ChemistrySelect 2(4), 1533-1536 (2017).

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. CAY10486 inhibits human ACAT-1 and ACAT-2 equally with an IC50 value of approximately 60 μM. It also inhibits copper-mediated oxidation of low density lipoproteins by about 28% at a concentration of 3 μM.

Terpendole C is an indole diterpene alkaloid fungal metabolite originally isolated from A. yamanashiensis and an inhibitor of acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 2.1 μM in rat liver microsomes). It also inhibits ACAT in J774 macrophages (IC50 = 0.46 μM) without affecting cell growth.

Isobutyryl coenzyme A (isobutyryl-CoA) is a short-chain branched acyl CoA. Isobutyryl-CoA is a substrate for isobutyryl-CoA dehydrogenase (IBDH) in the catabolism of valine and an intermediate in the synthesis of isobutyryl-L-carnitine , which accumulates in IBDH deficiency.

Penicillide is a fungal metabolite originally isolated from Penicillium that has diverse biological activities. It is an inhibitor of calpain 2/m-calpain (IC50 = 7.1 μM) and acyl-coenzyme A:cholesterol acyltransferase (ACAT; IC50 = 22.9 μM). It is also an antagonist of oxytocin receptors (IC50 = 67 μM). Penicillide inhibits RNA synthesis in P388 murine leukemia cells.