high-density

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。

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。

High density lipoprotein (HDL) (human) 是一种功能性脂蛋白，能够与清道夫受体 B1 (SR-B1)、ABCA1 和 ABCG1 结合。通过逆向胆固醇转运 (RCT)，它从外周组织清除多余胆固醇并将其送至肝脏进行代谢，同时激活内皮型一氧化氮合酶 (eNOS) 以生成一氧化氮 (NO)，从而发挥抗氧化、抗炎和血管内皮保护作用。High density lipoprotein (human) 在心血管疾病研究中具有潜力，如动脉粥样硬化。

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)。

Arachidic acid (Icosanoic Acid) 是一种存在于所有哺乳动物细胞中的长链脂肪酸，通常酯化为膜磷脂，是人体组织中丰富的多不饱和脂肪酸之一。

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。

KR31173 是一种AT1拮抗剂，IC50为3.27 nM。经^11C同位素标记后，KR31173 可被用作正电子发射断层扫描 (PET) 示踪剂。在小鼠试验中，KR31173 展现了出色的生物分布和药理特性，能够选择性结合于CD-1小鼠已知具有高密度AT1血管紧张素受体的器官。

GPR109 receptor agonist-3 是GPR109受体激动剂，具有口服活性，IC50为310 nM。它保留硫辛酸的抗氧化和细胞保护作用，在高脂饮食的大鼠中降低总胆固醇 (TC)、甘油三酯 (TG)、以及低密度脂蛋白胆固醇 (LDL-C)，同时增加高密度脂蛋白胆固醇 (HDL-C)。GPR109 receptor agonist-3 可用于研究动脉粥样硬化。

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.