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.

LDL-IN-3 shows anti-atherosclerotic and antioxidant activities.

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

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.

BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of animal, plant, and fungal sterols.

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.

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

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.

Moxonidine (BDF5895) is a selective agonist at the imidazoline receptor subtype 1, acting as an antihypertensive drug.

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.

Pirozadil shows hypolipidemic activity.

Etofibrate is a combination of clofibrate and niacin, used to treat hyperlipemia.

Nicanartine is a cholesterol inhibitor that is used to treat cardiovascular disease and can be used to study atherosclerosis.

20-HC-Me-Pyrrolidine is a potent Aster protein inhibitor with IC50=0.06~0.71 μm for Aster-A, Aster-B, and Aster-C that blocks the ability of Aster proteins to bind and transfer cholesterol, including inhibiting the movement of LDL cholesterol to the endoplasmic reticulum.

2-Acetamidophenol (Orthocetamol) has analgesic and antipyretic effects. 2-Acetamidophenol is an isomer of Paracetamol (4-acetamidophenol).

Recaticimab (SHR-1209) is a humanized monoclonal antibody targeting PCSK9. By binding to PCSK9, Recaticimab promotes LDL receptor stabilization and surface expression on hepatocytes, leading to reduced plasma LDL cholesterol levels. Recaticimab is under study as a therapeutic candidate for hypercholesterolemia and related cardiovascular disorders.

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.

Colesevelam Hydrochloride is a bile acid sequestrant with a higher affinity for glycocholic acid in vitro. Colesevelam Hydrochloride inhibits bile acid reabsorption, leading to increased bile acid synthesis and reduces cholesterol levels in patients with

1,2-Cyclohexanedione exhibits binding activity toward ketopantoyl-lactone reductase from Candida parapsilosis and is widely used in biochemical experiments and drug synthesis research.

Piceatannol 4'-O-glucoside (Piceatannol 4'-O-β-D-glucopyranoside) is a natural antioxidant, a glucoside extracted from rhubarb, which is used in the study of diabetes.

Anti-oxLDL Antibody is a human-derived antibody expressed in CHO cells, specifically targeting oxLDL. It features a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 150 kDa. For isotype control, refer to HumanIgG1kappa, Isotype Control.

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).