LDLR

Evolocumab is an inhibitor of the humanized monoclonal antibody PCSK9. It binds to circulating PCSK9 protein, resulting in inhibition of PCSK9 binding to LDLR. It can be used in studies of hypercholesterolemia and atherosclerotic cardiovascular disease.

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.

1. Coptisine (Coptisin) treatment increases cell viability based on its reversal effect on the enhanced activity of Indoleamine 2, 3-dioxygenase . 2. Coptisine treats myocardial I/R likely through suppressing myocardial apoptosis and inflammation by inhibiting the Rho/ROCK pathway. 3. Coptisine is a potential anti-osteosarcoma drug candidate, via exerting a strong anti-osteosarcoma effect with very low toxicity . 4. Coptisine with a high dosage could inhibit cholesterol synthesis via suppressing the HMGCR expression and promoting the use and excretion of cholesterol via up-regulating LDLR and CYP7A1 expression. 5. Coptisine suppresses adhesion, migration and invasion of MDA-MB-231 breast cancer cells in vitro, the down-regulation of MMP-9 in combination with the increase of TIMP-1 possibly contributing to the anti-metastatic function for breast cancer.

PCSK9-IN-10, a potent and orally active inhibitor of Proprotein Convertase Subtilisin/Kexin Type 9 (PCSK9), exhibits a half-maximal inhibitory concentration (IC50) of 6.4 µM. By enhancing the expression of Low-Density Lipoprotein Receptor (LDLR) protein and reducing PCSK9 expression, PCSK9-IN-10 effectively decreases atherosclerosis progression. This compound holds promise for hyperlipidemia research applications.

Pep 2-8 ammonium salt is Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9.

PCSK9-IN-11 (compound 5r) is a potent PCSK9 inhibitor with oral activity, exhibiting inhibitory activity on PCSK9 transcription in HepG2 cells (IC50 = 5.7 μM) and capable of increasing LDL receptor (LDLR) protein levels. PCSK9-IN-11 is applicable for atherosclerosis research.

Propane-1,2,3-triyl tripalmitate (Glycerol Tripalmitate) is a triacylglycerol found in dietary fats. In hamsters fed a diet enriched with it, Tripalmitin increases body weight, elevates plasma LDL levels, and reduces hepatic LDL receptor mRNA levels. It inhibits glucose-stimulated insulin secretion and decreases the viability of INS1 cells dose-dependently. Tripalmitin is used in cosmetic products for skin conditioning and as a thickening agent, and it forms lipid matrices of nanoparticles for drug delivery.

Orticumab (MLDL1278A) is a recombinant human monoclonal antibody engineered to specifically bind to epitopes on oxidized low-density lipoprotein (oxLDL). it demonstrates therapeutic potential by modulating autoimmune responses against oxLDL, thereby improving atherosclerotic plaque pathology, and also shows significant promise for the treatment of autoimmune inflammatory conditions such as psoriasis.

KYLO-0603 is an orally active and selective THR-β agonist with an EC50 of 31.07 nM. It effectively reduces serum cholesterol and low-density lipoprotein cholesterol levels. By activating THR-β receptors, KYLO-0603 enhances the expression of THR-regulated genes like iodothyronine deiodinase 1 (Dio1), malic enzyme 1 (Me1), and thyroid hormone-responsive (Thrsp) gene, while it inhibits the expression of inflammatory and fibrosis-related genes, including low-density lipoprotein receptor (LDL-R) gene. This compound is applicable for the study of metabolic associated steatohepatitis (MASH) and liver fibrosis.

S 12340 is a potent inhibitor of the oxidative modification of low-density lipoprotein.

IETP2 targets low-density lipoprotein receptor-related protein 1 (LRP1) with a KD of 738 nM, making it useful for delivering drugs and imaging agents across the blood-labyrinth barrier (BLB).

LY 295427 is a bioactive chemical.

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.

Milpocitide, a (293-333)-peptide fragment of the human low-density lipoprotein receptor (LDLR), specifically corresponds to the EGF-like domain 1 [1].