2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. LDLR

LDLR

Low-density lipoprotein receptor

The low-density lipoprotein receptor (LDLR) gene family includes LDLR, very LDLR, and LDL receptor-related proteins (LRPs) such as LRP1, LRP1b (aka LRP-DIT), LRP2 (aka megalin), LRP4, and LRP5/6, and LRP8 (aka ApoER2). LDLR family members constitute a class of closely related multifunctional, transmembrane receptors, with diverse functions, from embryonic development to cancer, lipid metabolism, and cardiovascular homeostasis.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-101529
    Imanixil
    		99.29%
    Imanixil (HOE-402 free base) is an orally active LDL receptor (LDLR) inducer. Imanixil can reduce cholesterol levels by inhibiting VLDL-lipid production. Imanixil can delay atherosclerosis profession. Imanixil can be used for the research of cardiovascular disease, such as atherosclerosis.
    Imanixil
  • HY-158424
    LSN3353871
    		Inhibitor 99.62%
    LSN3353871 is a potent inhibitor of lipoprotein(a) (Lp(a)) that can binds to Kringle IV (KIV) 8, KIV7-8 and KIV5-8, with Kd of 756 nM, 605 nM and 423 nM, respectively. LSN3353871 disrupts the formation of Lp(a) with the IC50 of 1.69 μM. LSN3353871 has oral bioactivity.
    LSN3353871
  • HY-109567
    Gemcabene
    		Inhibitor 99.91%
    Gemcabene (PD-72953), a first-in-class lipid-lowering agent, lowers low-density lipoprotein cholesterol (LDL-C), decreases triglycerides, and raises high-density lipoprotein cholesterol (HDL-C) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
    Gemcabene
  • HY-P10502A
    L57 acetate
    		99.01%
    L57 acetate is a Low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 acetate exhibits high affinity to LRP1 with Ki of 45 nM. L57 acetate exhibits blood-brain barrier (BBB) permeability and plasma stability. L57 acetate can be utilized as the carrier for CNS drug delivery.
    L57 acetate
  • HY-W018587
    TBPH
    TBPH is a brominated flame retardant. TBPH enhances hepatic steatosis, inflammation, and fibrosis in mice with nonalcoholic steatohepatitis (NASH). TBPH induces dysregulation of phospholipid metabolism, reducing cardiolipin (CL) and phosphatidylserine (PS) levels. TBPH leads to impaired endoplasmic reticulum-mitochondria (ER-Mito) contacts, subsequently causing mitochondrial dysfunction. TBPH induces lung injury through an inflammatory response mediated by mitochondria-derived ds-DNA. TBPH can be used to study the role of MFN2-mediated ER-mitochondria contacts in lipid metabolism homeostasis.
    TBPH
  • HY-125544
    LY 295427
    		Modulator 98.0%
    LY 295427 is a LDL receptor modulator and a hypocholesterolemic agent. LY 295427 derepresses the transcription of the LDLR (LDL Receptor). LY 295427 can be used for hypercholesterolemia research.
    LY 295427
  • HY-P99793
    Orticumab
    		Inhibitor ≥99.0%
    Orticumab (MLDL1278A) is an antibody targeting to oxidized or malondialdehyde-modified lipoprotein (LDL). Orticumab specifically inhibits oxidized low-density lipoproteins (oxLDL). Orticumab involves in modulation of autoimmune responses against oxLDL, improves atherosclerosis in animal model. Orticumab also can be used for research of psoriasis improvement.
    Orticumab
  • HY-B0374
    Moxonidine
    		99.72%
    Moxonidine (BDF5895) is an orally active imidazoline type 1 receptor (I1-R) agonist. Moxonidine activates imidazoline I1 receptors and α2 adrenoceptors, affecting oxidized low-density lipoprotein uptake. Moxonidine reduces atherosclerotic lesions and lowers blood pressure. Moxonidine can be used in the study of hypertension, heart failure, and atherosclerosis.
    Moxonidine
  • HY-120651
    LDL-IN-2
    		Inhibitor 99.0%
    LDL-IN-2 (compound 3) is an antioxidant against copper mediated low-density lipoproteins (LDL) oxidation.
    LDL-IN-2
  • HY-P10697A
    VH4127 TFA
    		Modulator
    VH4127 TFA is a cyclic peptide targeting the low density lipoprotein receptor (LDLR) with a KD of 18 nM for hLDLR. VH4127 TFA specifically binds to rodent and human epidermal growth factor (EGF) homology domain of LDLR.
    VH4127 TFA
  • HY-P10502
    L57
    		99.44%
    L57 is a low-density lipoprotein receptor-related protein 1 (LRP1)-binding peptide. L57 exhibits high affinity for LRP1, with an EC50 of 45 nM. L57 possesses blood-brain barrier (BBB) permeability and plasma stability. L57 can serve as a carrier for central nervous system drug delivery.
    L57
  • HY-W015600S
    2-Acetamidophenol-d3
    		99.48%
    2-Acetamidophenol-d3 (Orthocetamol-d3) is the deuterium labeled 2-Acetamidophenol (HY-W015600). 2-Acetamidophenol (Orthocetamol) is a regulator that targets ferroptosis and glutathione metabolic pathways, is the ortho-regioisomer of Paracetamol (HY-66005). 2-Acetamidophenol has anti-atherosclerotic activity, and inhibiting total cholesterol (TC) and triglyceride (TG) in a zebrafish hyperlipidemia model with IC50s for 30 μM and 40 μM, respectively. 2-Acetamidophenol upregulates the expression of glutathione synthesis-related genes (such as GCLC, GCLM, GSS) and iron ion transport genes (such as FPN1, FTH), reduces the accumulation of intracellular reactive oxygen species (ROS) and ferrous ions (Fe2+), and enhances the activity of glutathione peroxidase GPX4, thereby inhibiting macrophage phagocytosis of oxidized low-density lipoprotein (ox-LDL) and foam cell formation.
    2-Acetamidophenol-d<sub>3</sub>
  • HY-121212
    Icosabutate
    		Activator
    Icosabutate, an orally active ω-3 polyunsaturated fatty acid, is an aeicosapentaenoic acid (EPA) derivative. Icosabutate overcomes the drawbacks of unmodified EPA for liver targeting and improves insulin sensitivity, hepatic inflammation and fibrosis. Icosabutate is well tolerated, and efficacious in lowering non-high-density lipoprotein cholesterol (non-HDL-C) levels in persistent hypertriglyceridemia .
    Icosabutate
  • HY-N0430
    Coptisine
    Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease.
    Coptisine
  • HY-130587
    Sultosilic acid piperazine salt
    Sultosilic acid piperazine salt (Piperazine sultosylate; A-585) is a lipid-lowering agent. Sultosilic acid piperazine salt modifies the blood lipids levels, reduces platelet adhesiveness without promoting peroxisomal activity of hepatocytes or producing other adverse side-effects.
    Sultosilic acid piperazine salt
  • HY-142026
    Vitisin A
    		Inhibitor
    Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC50 values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.
    Vitisin A
  • HY-A0127
    Etofibrate
    		Activator 99.80%
    Etofibrate is the ethandiol-1,2 diester of the nicotinic and clofibric acids. Etofibrate has been shown to be a potent hypolipidemic agent in animal and human.
    Etofibrate
  • HY-109567A
    Gemcabene calcium
    		Inhibitor 98.0%
    Gemcabene calcium (PD-72953 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) and lowers pro-inflammatory acute-phase protein, C-reactive protein (CRP), exerting anti-inflammatory activity.
    Gemcabene calcium
  • HY-W423578
    LDLR regulator-1
    		Modulator 99.89%
    LDLR regulator-1 (Compound 7b) is a regulator of the low-density lipoprotein receptor (LDLR), capable of increasing the mRNA expression of LDLR.
    LDLR regulator-1
  • HY-100144
    Pirozadil
    		98.31%
    Pirozadil is a hypolipidemic agent.
    Pirozadil
Cat. No. Product Name / Synonyms Application Reactivity