high-density

是胆固醇酯转移蛋白 (CETP) 选择性抑制剂。根据人血浆的抑制曲线，Torcetrapib (CP-529414) 对CETP 的最有效浓度为 37 nM。

BLT-1 是一种氨基硫脲铜螯合剂，是一种选择性清除受体 B1 型 (SR-BI) 抑制剂，抑制高密度脂蛋白 (HDL) 和 SR-BI 介导的细胞之间的脂质转移。

Bezafibrate (BM15075) 是一种降血脂剂，是PPAR 的激动剂，对人以及鼠PPARα、PPARγ和PPARδ的EC50分别为 50、60和20 μM， 以及 90、55 和110 μM。

Gemfibrozil (CI-719) 是一种PPAR-α激活剂，可作为降脂药。它也是P450非选择性抑制剂，对 CYP2C9、2C19、2C8 和 1A2 的Ki 值分别为 5.8、24、69 和 82 μM。

Sucrose-epichlorohydrin copolymer（Polysucrose 400，聚蔗糖 400）是蔗糖与环氧氯丙烷共聚合的高分子量聚合物，用于细胞、细胞膜、细胞器、病毒细胞的密度梯度分离和蛋白液相分离 (LLPS)。

CDD3505 (4-nitro-1-trityl-1H-imidazole) 能够诱导肝CYP3A 的活动，增强高密度脂蛋白胆固醇的水平。

CDD3506 (1-TRITYL-1H-IMIDAZOL-4-AMINE) 能够诱导肝CYP3A 的活动，增强高密度脂蛋白胆固醇的水平。

Gemcabene calcium , a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) andexerting anti-inflammatory activity, lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP).

Gemcabene (PD-72953) 是一种具有抗炎活性的降脂剂。 Gemcabene 降低低密度脂蛋白胆固醇和甘油三酯，提高高密度脂蛋白胆固醇，并降低促炎急性期蛋白、C 反应蛋白。

CP-532623, a close structural analog of Torcetrapib, is a CETP inhibitor with highly lipophilic properties. It elevates high-density lipoprotein cholesterol.

PCSK9-IN-29 是一种有效的降脂药物。在 hepG2 细胞中，该化合物能够增强低密度脂蛋白受体 (LDLR) 的表达，同时减少 PCSK9 蛋白的表达。此外，在食用高脂肪饮食的食蟹猴体内，PCSK9-IN-29 能显著降低血清中 LDL-C、TC 以及肝酶 ALT 的水平，有效减轻体重和体脂，并提升骨矿物质含量。该化合物主要用于非酒精性脂肪性肝炎与肥胖症的研究领域。

CP 524515 是一种胆固醇酯转移蛋白 (CETP) 的有效抑制剂，能够增加高密度脂蛋白胆固醇水平。

BLT-4 是一种专门针对清道夫受体 B 类 I 型 (SR-BI) 的可逆抑制剂。BLT-4 能抑制 SR-BI 介导的高密度脂蛋白 (HDL) 与细胞的脂质转移。

E-3030 free acid is a peroxisome proliferator-activated receptor (PPAR) agonist. E-3030 decreased blood glucose, triglyceride, non-esterified fatty acids, and insulin levels and increased blood adiponectin levels. Triglyceride- and non-high-density lipopr

Hyodeoxycholic acid sodium salt is a natural secondary bile acid. It improves high-density lipoprotein function, reduces farnesoid X receptor antagonist bile acids, and induces strong cytotoxicity, apoptosis, and IL-8 synthesis.

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%.

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils. Both oils have been found to have lipid-lowering properties. A diet containing maritime pine seed oil (MPSO) lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. Korean pine seed oil supplements may help in obesity by reduction of appetite. People taking this oil had an increase in the satiety hormones CCK and GLP-1 and a reduced desire to eat. The activity of the oil is attributed to pinolenic acid. Pinolenic acid is not converted to arachidonic acid metabolically and can reduce arachidonic acid levels in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. Pinolenic acid ethyl ester is a neutral, more lipophilic form of the free acid.

Peroxisome proliferator-activated receptors (PPARs) α, δ, γ are ligand-activated nuclear transcription factors involved in the regulation of energy homeostasis as well as insulin sensitivity and glucose metabolism. Pharmacologies of PPARδ receptor agonists, though relatively obscure, have recently been reported to elevate high-density lipoprotein (HDL) cholesterol and lower plasma triglyceride (TG) levels in obese insulin resistant rhesus monkeys. CAY10592 is a full PPARδ agonist (EC50 = 30 nM) in a fatty acid oxidation assay of rat L6 muscle cells with desirable oral pharmacokinetic properties. In a transactivation assay using human PPAR receptors, CAY10592 acts as a selective partial PPARδ agonist (EC50 = 53 nM) with no effect on PPARα or PPARγ activity up to 30 μM. Chronic treatment of high fat fed ApoB100/CETP-transgenic mice with CAY10592 at a dose of 20 mg/kg increases HDL levels, decreases LDL and TG levels, and improves insulin sensitivity.

The early stage of atherosclerosis is characterized by the aggregation of foam cells, so called a fatty streak, in the inner arterial wall. CAY10487 inhibits formation of fatty streak lesions of the thoracic aorta in high cholesterol-fed rabbits without affecting plasma lipid profiles or significantly inhibiting ACAT-1 or ACAT-2 activity. The percent area occupied by the atherosclerotic lesion in rabbits supplemented with 0.05% CAY10487 in the diet was 16.1% compared to 53.5% in control rabbits. CAY10487 also exhibits antioxidant activity, inhibiting copper-mediated oxidation of low-density lipoprotein by about 75% at a concentration of 2 μM.

5(Z),11(Z),14(Z)-Eicosatrienoic acid is a polyunsaturated fatty acid found in various natural sources including maritime pine (Pinus pinaster) seed oil (MPSO), gymnospermae leaves and seeds, and freshwater gastropods. A diet containing MPSO lowered high-density lipoprotein and ApoA1 levels in transgenic mice expressing human ApoA1. MPSO was found to diminish cholesterol efflux in vitro. 5(Z),11(Z),14(Z)-Eicosatrienoic acid methyl ester, when topically applied, reduces inflammatory processes, potentially by displacing arachidonic acid from phospholipid pools and reducing downstream inflammatory products such as prostaglandin E2 and leukotrienes.

Bile acids are essential for solubilization and transport of dietary lipids, are the major products of cholesterol catabolism, and are physiological ligands for farnesoid X receptor (FXR), a nuclear receptor that regulates genes involved in lipid metabolism.1They are also inherently cytotoxic, as physiological imbalance contributes to increased oxidative stress.2,3Bile acid-controlled signaling pathways are promising novel targets to treat such metabolic diseases as obesity, type II diabetes, hyperlipidemia, and atherosclerosis.Guggulsterone, derived from resin of the guggul tree, is a competitive antagonist of FXR bothin vitroandin vivo.4Thecisstereoisomer of guggulsterone, (E)-guggulsterone, decreases chenodeoxycholic acid (CDCA)-induced FXR activation with an IC50value of 15 μM.5,6By inhibiting CDCA-induced transactivation of FXR, guggulsterone lowers low-density lipoprotein cholesterol and triglyceride levels in rodents fed a high cholesterol diet.4 1.Makishima, M., Okamoto, A.Y., Repa, J.J., et al.Identification of a nuclear receptor for bile acidsScience2841362-1365(1999) 2.Barbier, O., Torra, I.P., Sirvent, A., et al.FXR induces the UGT2B4 enzyme in hepatocytes: A potential mechanism of negative feedback control of FXR activityGastroenterology1241926-1940(2003) 3.Tan, K.P., Yang, M., and Ito, S.Activation of nuclear factor (erythroid-2 like) factor 2 by toxic bile acids provokes adaptive defense responses to enhance cell survival at the emergence of oxidative stressMol. Pharmacol.72(5)1380-1390(2007) 4.Urizar, N.L., Liverman, A.B., Dodds, D.T., et al.A natural product that lowers cholesterol as an anatagonist ligand for FXRScience296(5573)1703-1706(2002) 5.Cui, J., Huang, L., Zhao, A., et al.Guggulsterone is a farnesoid X receptor antagonist in coactivator association assays but acts to enhance transcription of bile salt export pumpThe Journal of Biological Chemisty278(12)10214-10220(2003) 6.Wu, J., Xia, C., Meier, J., et al.The hypolipidemic natural product guggulsterone acts as an antagonist of the bile acid receptorMolecular Endocrinology16(7)1590-1597(2002)

Palmitoleic acid is a common constituent of the triglycerides of human adipose tissue. Palmitoleic acid-based diets raise low-density lipoprotein cholesterol and diminish high-density lipoprotein cholesterol, even when dietary intake of cholesterol is maintained at a low level. Palmitelaidic acid is the trans isomer of the 16:1 fatty acid palmitoleic acid. While its effects on cholesterol levels are poorly studied, palmitelaidic acid can have very different effects from those of palmitoleic acid on lipid metabolism and mobilization. Palmitelaidic acid methyl ester is an ester version of the free acid which may be more amenable for the formulation of fatty acid-containing diets and dietary supplements.

MK-8262, an orally active and potent cholesteryl ester transfer protein (CETP) inhibitor (IC 50 = 53 nM, log D = 5.3), is a bistrifluoromethyl analogue that shows promise in research related to high-density lipoprotein (HDL) and low-density lipoprotein (LDL) with potential implications for coronary heart disease (CHD).

(20R)-Protopanaxadiol ((20R)-Protopanaxdiol) 是黑参中20(R)-人参皂甙 Rg3的一种三萜皂苷代谢物。它抑制幽门螺杆菌的生长，有抗肿瘤活性和细胞毒性。