lipoprotein

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

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

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.

1. Pseudoprotodioscin has moderate cytotoxicity.

Ibrolipim (NO-1886) attenuates high glucose-induced endothelial dysfunction in cultured human umbilical vein endothelial cells via PI3K/Akt pathway.

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.

Lipoprotein lipase (LPL) is an enzyme, mainly involved in lipid metabolism, that hydrolyzes triglycerides in lipoproteins.LPL can be a target for obesity/diabetes-related cardiovascular diseases and has an important role in lowering triglyceride levels and improving cardiovascular.

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).

ApolipoproteinKV domain (67-77) is an 11-amino-acid peptide isolated from the KV domain of human apolipoprotein a (ApoA), known for its anti-angiogenic and anti-tumor activities. It targets the angiogenesis c-Src/ERK pathway by blocking activation signals received from vascular endothelial growth factor (VEGF). ApolipoproteinKV domain (67-77) is applicable in cancer research.

Bococizumab(PF-04950615) is a humanized mAb against PCSK9 and an inhibitor of the synthesis of PCSK9 in the liver that reduces the amount of low-density lipoprotein cholesterol (LDL-C) in the blood.Bococizumab is used to treat hypercholesterolemia.

Tirzepatide (LY-3298176) is a dual agonist of glucose-dependent polypeptide (GIP) (EC50=0.042 nM) and glucagon-like peptide-1 (GLP-1) (EC50=0.086 nM) receptors, and it has neuroprotective activity. It can improve blood pressure and lower low-density lipoprotein (LDL) cholesterol and triglycerides, and can be used to study diabetes and obesity.

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.

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.

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.

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.

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.