lipoprotein (a)

Muvalaplin (LY3473329) is an orally active lipoprotein (a) [Lp(a)] reagent that inhibits Lp(a) formation by blocking apo(a)-apo B100 interactions.

Lp-PLA2-IN-3 is a potent, orally bioactive lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, effectively inhibiting recombinant human [Lp-PLA2] with an IC50 value of 14 nM.

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.

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).

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.

Diaminopimelic acid or DAPA is a lysine-like amino acid derivative that is a key component of the bacterial cell wall. DAPA is incorporated or integrated into peptidoglycan of gram negative bacteria and is the attachment point for Braun's lipoprotein (BLP or Murein Lipoprotein). BLP is found in gram-negative cell walls and is one of the most abundant membrane proteins. BLP is bound at its C-terminal end (a lysine) by a covalent bond to the peptidoglycan layer (specifically to diaminopimelic acid molecules) and is embedded in the outer membrane by its hydrophobic head (a cysteine with lipids attached). BLP tightly links the two layers and provides structural integrity to the bacterial outer membrane. Diaminopimelic acid can be found in human urine or feces due to the lysis or enzymatic breakdown of gram negative gut microbes.

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.

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.

G0507 is a pyrrolopyrimidinedione compound that serves as a potent inhibitor of Escherichia coli growth, effectively inducing the extracytoplasmic σE stress response. It acts as a valuable chemical probe, specifically designed to dissect lipoprotein trafficking in Gram-negative bacteria. Notably, G0507 demonstrates strong inhibitory activity against the LolCDE ABC Transporter.

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

Lp-PLA2-IN-2 is a selective and potent lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor, with an IC50 of 120 nM for recombinant human Lp-PLA2.

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

Rilapladib (SB 659032) is a selective inhibitor of Lipoprotein-Associated Phospholipase A2 (Lp-PLA2, IC50 = 230 pM) and acts as an antagonist of the platelet-activating factor receptor.

Niceritrol (Cardiolipol) is a niacin ester that reduces cholesterol and triglycerides in total plasma and in the VLD and LD lipoprotein fractions.

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.

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.

Muvalaplin tetrahydrochloride (LY3473329) is an orally active lipoprotein (a)Lp(a) agent currently under investigation. Research on the oral formulation of Muvalaplin tetrahydrochloride is ongoing.

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).

MD-700 is an innovative isobenzofuranone that increases LDL receptor expression in HepG2 cells within 4 hours at a concentration of 0.03 microg ml. MD-700 selectively reduces levels of LDL and very low-density lipoprotein cholesterol.