high-density

BLT-1 is a scavenger receptor BI (SR-BI)inhibitor.

Torcetrapib (CP-529414) is a cholesteryl ester transfer protein (CETP) inhibitor designed to reduce the heterotypic transfer of cholesteryl ester from HDL to LDL and/or VLDL. It failed in phase III trials due to an excess of deaths.

High density lipoprotein (HDL) (human) is a functional lipoprotein capable of binding to receptors such as scavenger receptor B1 (SR-B1), ABCA1, and ABCG1. It facilitates the removal of excess cholesterol from peripheral tissues through reverse cholesterol transport (RCT), transferring it to the liver for metabolism. Additionally, it activates endothelial nitric oxide synthase (eNOS) to produce nitric oxide (NO), offering antioxidant, anti-inflammatory, and vascular endothelial protection. High density lipoprotein (human) is a potential candidate for cardiovascular disease research, including atherosclerosis.

Bezafibrate (BM15075) is an antilipemic agent that lowers CHOLESTEROL and TRIGLYCERIDES. It decreases LOW-DENSITY LIPOPROTEINS and increases HIGH-DENSITY LIPOPROTEINS.

Gemfibrozil (CI-719) interacts with peroxisome proliferator-activated receptors (PPARalpha) resulting in PPARalpha-mediated stimulation of fatty acid oxidation and an increase in lipoprotein lipase (LPL) synthesis. Gemfibrozil is a fibric acid derivative with hypolipidemic effects. This enhances triglyceride-rich lipoprotein clearance and reduces the expression of apolipoprotein C-III (apoC-III). The reduction in hepatic production of apoC-III result in the subsequent reduction of serum levels of very-low-density-lipoprotein cholesterol (VLDL-C). In addition, gemfibrozil-mediated PPARalpha stimulation of apoA-I and apoA-II expression results in an increase in high-density lipoprotein cholesterol (HDL-C).

Sucrose-epichlorohydrin copolymer (Polysucrose 400) is a high molecular weight polymer of sucrose co-polymerized with epichlorohydrin for density gradient separation of cells, cell membranes, organelles, and viral cells and protein liqudi-liquid phase separation (LLPS).

Arachidic acid (Icosanoic Acid) is a saturated fatty acid found naturally in fish and vegetable oils (such as those from peanuts). It can also be formed by the hydrogenation of arachidonic acid. Diets rich in saturated fatty acids, such as arachidic acid, are known to increase serum low-density lipoproteins resulting in high blood cholesterol levels.

CDD3505 (4-nitro-1-trityl-1H-imidazole) increases high-density lipoprotein cholesterol by targeting hepatic CYP3A.

CDD3506 (1-TRITYL-1H-IMIDAZOL-4-AMINE) increases high-density lipoprotein cholesterol by targeting hepatic CYP3A.

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) is a lipid-lowering agent with anti-inflammatory activity. Gemcabene lowers low-density lipoprotein cholesterol and triglycerides, raises high-density lipoprotein cholesterol, and decreases pro-inflammatory acute-phase protein, C-reactive protei

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 serves as a lipid-lowering agent that enhances the expression of low-density lipoprotein receptor (LDLR) protein and reduces PCSK9 protein expression in hepG2 cells. Additionally, in crab-eating macaques on a high-fat diet, it lowers serum LDL-C, TC, and liver enzyme ALT levels, reduces body weight and fat, and boosts bone mineral content. PCSK9-IN-29 is useful for studies involving non-alcoholic fatty liver disease and obesity.

CP 524515 is a potent inhibitor of cholesterol ester transfer protein (CETP), which results in increased levels of high-density lipoprotein cholesterol.

BLT-4 is a specific and reversible inhibitor of scavenger receptor class B type I (SR-BI). It effectively blocks the SR-BI-mediated transfer of lipids between high-density lipoprotein (HDL) and cells.

KR31173 is an AT1 antagonist with an IC50 of 3.27 nM. When labeled with the 11C isotope, KR31173 can be used as a tracer for positron emission tomography (PET). In mice, KR31173 exhibits favorable biodistribution and pharmacological characteristics. It selectively binds to organs in CD-1 mice known to have a high density of AT1 angiotensin receptors.

GPR109 receptor agonist-3 is an orally active GPR109 receptor agonist with an IC50 of 310 nM. It retains the antioxidant and cytoprotective properties of lipoic acid. In rats on a high-fat diet, GPR109 receptor agonist-3 reduces total cholesterol (TC), triglycerides (TG), and low-density lipoprotein cholesterol (LDL-C), while increasing high-density lipoprotein cholesterol (HDL-C). This compound is applicable for atherosclerosis research.

THR-β agonist 11 is an orally active and selective thyroid hormone receptor (THR-β) agonist. It demonstrates robust cholesterol-lowering effects in cholesterol-fed rats. In a high-fat diet-carbon tetrachloride (HFD-CCl4) induced model of metabolic dysfunction-associated steatohepatitis (MASH) in mice, THR-β agonist 11 significantly reduces serum total triglycerides (TG), low-density lipoprotein cholesterol (LDL-cholesterol), liver total cholesterol (TC), and TG levels. Additionally, it alleviates hepatic steatosis, inflammation, and fibrosis. THR-β agonist 11 is applicable in the study of MASH and other fibrotic diseases.

CP-800569 is an orally active inhibitor of cholesteryl ester transfer protein (CETP). It effectively reduces low-density lipoprotein and postprandial triglycerides while increasing high-density lipoprotein. CP-800569 is applicable in the study of metabolic diseases.

7,7-Azo-3-α,12-α-dihydroxycholanic acid is a light-unstable (photo-crosslinking) derivative of cholic acid with reduced affinity for high-density lipoprotein (HDL).

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, a natural secondary bile acid, enhances high-density lipoprotein function, reduces farnesoid X receptor antagonist bile acids, and induces potent cytotoxicity, apoptosis, and IL-8 synthesis.

Oleic acid-2,6-diisopropylanilide is an inhibitor of acylCoA:cholesterol acyltransferase (ACAT), an intracellular cholesteryl ester synthase involved in dietary cholesterol absorption, with an IC50 of 7 nM. When administered at 0.05% to rabbits or rats on a high fat, high cholesterol diet, it reduces low-density lipoproteins and increases high-density lipoprotein levels.

Pinolenic acid is a polyunsaturated fatty acid found in Korean pine (Pinus orientalis) and maritime pine (Pinus pinaster) seed oils, which exhibit lipid-lowering properties. In transgenic mice expressing human ApoA1, a diet containing maritime pine seed oil (MPSO) reduced high-density lipoprotein and ApoA1 levels and diminished cholesterol efflux in vitro. Korean pine seed oil supplements may aid in reducing obesity by decreasing appetite, as evidenced by increased levels of satiety hormones CCK and GLP-1 and reduced desire to eat. Pinolenic acid, which is not metabolically converted to arachidonic acid, can lower arachidonic acid levels in the phosphatidylinositol fraction of HepG2 cells from 15.9% to 7.0%. The neutral, more lipophilic form of pinolenic acid is pinolenic acid ethyl ester.