low-density

Rosuvastatin (ZD4522) is an inhibitor of HMG-CoA reductase (HMGCR) (IC50=11 nM), selective and competitive. Rosuvastatin has hypolipidemic and antiatherosclerotic effects.

Oxidized low density lipoprotein (Human) (Human ox-LDL) plays a crucial role in atherogenesis and contributes to endothelial dysfunction through the cytoplasmic adapter protein TRAF3IP2. This compound also promotes endothelial cell activation, leads to increased production of adhesion molecules, and reduces eNOS activity and NO production. Additionally, Human ox-LDL activates the NLRP3 inflammasome in macrophages.

Low-density lipoprotein (human) is one of the five main lipoproteins responsible for transporting cholesterol to various tissues such as the adrenal glands, gonads, muscle, and adipose tissue.

Oxidized low density lipoprotein (mouse) is a modified form of low-density lipoprotein (LDL). It induces atherosclerosis (AS) by promoting endothelial dysfunction and accelerating the growth and migration of vascular smooth muscle cells (VSMCs).

Cerivastatin is an orally active and highly effective HMG-CoA reductase inhibitor with anticancer and lipid-lowering effects. Cerivastatin can reduce low-density lipoprotein cholesterol levels, inhibit the proliferation and invasion of MDA-MB-231 cells, and can be used to study primary hyperlipidemia.

Imanixil (HOE-402 free base) is an LDL receptor (LDLR) inducer, a hypolipidemic and hypocholesterolemic compound with antiatherogenic activity that inhibits the production of very low-density lipoproteins (VLDLs).Imanixil acts by stimulating the LDL receptor pathway.

Atorvastatin Sodium (Lipitor) is a competitive inhibitor of HMG-CoA reductase and increases the expression of low density lipoprotein (LDL) receptors on hepatocytes. Atorvastatin Sodium treatment inhibits aquaporin 4 to reduce ischaemic brain oedema.

Levosemotiadil(SA 3212) is a novel calcium antagonist and a very potent inhibitor of low-density lipoprotein oxidation.Levosemotiadil may be used to prevent lethal cardiac arrhythmias.

Apomine (SR-9223i), an inhibitor of HMG-CoA-reductase, promotes apoptosis of myeloma cells in vitro and has been implicated in the regulation of myeloma in vivo. Apomine accelerates the degradation of 3-hydroxy-3-methylglutaryl-CoA reductase and stimulates low-density lipoprotein receptor activity. Apomine enhances the antitumor effect of lovastatin on myeloma cells by downregulating 3-hydroxy-3-methylglutaryl-CoA reductase.

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).

Rosuvastatin calcium (ZD4522) , a selective and competitive inhibitor of hepatic hydroxymethyl-glutaryl coenzyme A (HMG-CoA) reductase, has antilipidemic activity.

Pitavastatin calcium (NK-104) is a potent inhibitor of HMG-CoA reductase (Ki: 1.7 nM). It lowers both total cholesterol and low-density lipoprotein cholesterol in animals and humans. Metabolism of pitavastatin by the cytochrome P450 system is minimal, reducing the risk of drug-drug interactions.

3-Chloro-L-Tyrosine (Chlorotyrosine), a specific marker of myeloperoxidase-catalyzed oxidation, is markedly elevated in low-density lipoprotein isolated from human atherosclerotic intima. In particular, myeloperoxidase halogenates tyrosine residues in plasma proteins and generates 3-chlorotyrosine (CY). The detection of free chlorotyrosine in blood or urine arises from the degradation of these chlorinated proteins. CY concentrations may be useful for monitoring the activation of neutrophils in asthmatic patients.

Lomitapide (AEGR-733) is a small molecule inhibitor of microsomal triglyceride transfer protein (MTP), an enzyme located in the lumen of the endoplasmic reticulum responsible for absorbing dietary lipids and transferring triglycerides onto apolipoprotein B (apo-B) in the assembly of very-low-density lipoprotein.

Cerivastatin sodium (BAY W 6228 sodium) is an orally active and highly potent HMG-CoA reductase inhibitor with lipid-lowering activity that can reduce low-density lipoprotein cholesterol levels. Cerivastatin sodium has anticancer effects and can be used to study primary hyperlipidemia.

Ro 48-8071 fumarate, an inhibitor of OSC (Oxidosqualene cyclase; IC50=6.5 nM), exhibits LDL (low-density lipoprotein) cholesterol-lowering activity.

Pravastatin is a lipoprotein-lowering drug via reversibly inhibiting hydroxymethylglutaryl-CoA (HMG-CoA) reductase and the synthesis of very-low-density lipoproteins.

Triarachidin (1,2,3-Trieicosanoyl Glycerol) is a triarachidic acid triglyceride. Triglycerides (TGs) are also known as triacylglycerols or triacylglycerides. TGs are the main constituent of vegetable oil and animal fats. TGs are major components of very low density lipoprotein (VLDL) and chylomicrons, play an important role in metabolism as energy sources and transporters of dietary fat. They contain more than twice the energy (9 kcal g) of carbohydrates and proteins.

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

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.

PCSK9-IN-30 (Compound 3f), a PCSK9 inhibitor, effectively targets a cryptic binding groove on PCSK9, thereby preventing PCSK9 from associating with the low-density lipoprotein receptor (LDLR) (IC 50 = 537 nM). This inhibition aids in the restoration of low-density lipoprotein (LDL) uptake by liver cells and significantly reduces plasma cholesterol levels. Demonstrating good bioavailability in mice, PCSK9-IN-30 holds potential for research within cardiovascular disease contexts.

OxLig-1 (7-Ketocholesteryl-9-carboxynonanoate) constitutes a lipid component of oxidized low-density lipoprotein (oxLDL) and serves as a critical ligand for β-glycoprotein I (β(2)-GPI). It induces nuclear translocation by activating the NF-κB pathway. Additionally, oxLig-1 is utilized in the study of atherosclerosis (AS).