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

LDLR Inhibitor

LDLR Inhibitors (30):

Cat. No. Product Name Effect Purity
  • HY-152857
    Muvalaplin
    Inhibitor 99.96%
    Muvalaplin (LY3473329) is an orally active, selective small molecule inhibitor of lipoprotein (a) (Lp (a)) that disrupts the initial non-covalent interaction between apo(a) and apoB100, preventing the disulphide bond and Lp(a) formation. Muvalaplin reduces the levels of Lp (a) in transgenic mice and in cynomolgus monkeys.
  • HY-179459
    SJ-300
    Inhibitor
    SJ-300 is a potent and selective, orally active and brain-penetrat DKK3-LRP1 interaction inhibitor. SJ-300 restores clearance in AD models. SJ 300 binds to mLRPIV with a Kd of 7.9 μM, inhibits the DKK3 mLRPIV complex with an IC50 of 3.2 μM, and does not disrupt the binding of to LRP1. SJ 300 rescues cognitive function and ameliorates neuropathology ( plaque reduction ≈ 73.3 %) in vivo. SJ 300 can be employed for research in Alzheimer’s disease.
  • HY-181997
    LDLRAP1-IN-1
    Inhibitor
    LDLRAP1-IN-1 (Compound B19) is a LDLRAP1 inhibitor and antiviral agent, with an IC50 of 4.98 μM for disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 covalently modifies the C119 residue of LDLRAP1 at the LDLRAP1-LDLR binding interface, thereby disrupting the interaction between LDLRAP1 and LDLR. LDLRAP1-IN-1 exhibits antiviral activity against HCoV-OC43.
  • HY-P990202
    Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4)
    Inhibitor
    Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4) is a mouse-derived IgG1 κ type antibody, targeting to mouse/rat/human LRP1/CD91. Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4) binds to the β chain of LRP1. Anti-Mouse/Rat/Human LRP1/CD91 Antibody (11H4) can be used for western blot (WB) and other detections.
  • HY-145001
    20-HC-Me-Pyrrolidine
    Inhibitor 99.69%
    20-HC-Me-Pyrrolidine (compound AI-3d) is a potent Aster protein inhibitor with IC50s of 0.11 μM, 0.06 μM, and 0.71 μM for Aster-A, Aster-B, and Aster-C, respectively. 20-HC-Me-Pyrrolidine blocks the ability of Asters to bind and transfer cholesterol. 20-HC-Me-Pyrrolidine also inhibits the movement of low-density lipoprotein (LDL) cholesterol to the endoplasmic reticulum (ER).
  • HY-14668
    Lomitapide mesylate
    Inhibitor 99.61%
    Lomitapide (AEGR-733; BMS-201038) mesylate is an orally active microsomal triglyceride transfer protein (MTP) inhibitor and a selective mTORC1 inhibitor with lipid-lowering activity and BBB permeability. Lomitapide mesylate significantly reduces plasma LDL levels by blocking the assembly and secretion of very-low-density lipoprotein (VLDL). Lomitapide mesylate inhibits mTORC1 in an ATP-dependent manner, thereby inducing AMPK-independent autophagic cell death and suppressing cancer cell growth and apoptosis. Lomitapide mesylate also enhances tumor infiltration of CD8+ T cells. In addition, Lomitapide mesylate inhibits HDAC, improves endothelial function, effectively alleviates vascular inflammation and oxidative stress, and exerts neuroprotective effects in a cerebral ischemia/reperfusion injury model. Lomitapide mesylate can be used in research on related diseases such as colorectal cancer, breast cancer, melanoma, ischemic stroke, and familial hypercholesterolemia.
  • HY-18778
    Obicetrapib
    Inhibitor 99.93%
    Obicetrapib (TA-8995; DEZ-001) is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).
  • HY-W015600
    2-Acetamidophenol
    Inhibitor 99.73%
    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.
  • 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.
  • 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.
  • 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.
  • HY-120651
    LDL-IN-2
    Inhibitor 99.0%
    LDL-IN-2 (compound 3) is an antioxidant against copper mediated low-density lipoproteins (LDL) oxidation.
  • 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.
  • 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.
  • HY-P990143
    Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6)
    Inhibitor
    Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) is an anti-mouse/rat/bovine VLDL-R IgG1 monoclonal antibody. Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) can specifically recognize VLDLR type-I and type-II expressed in CHO cells. Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) can be used to detect the expression of VLDLR in different cells and tissues. Anti-Mouse/Rat/Bovine VLDL-R Antibody (IgG-6A6) often used in western blot experiments.
  • HY-U00054
    LDL-IN-3
    Inhibitor
    LDL-IN-3 is an anti-atherosclerotic compound extracted from patent WO/2005/039596A1, example C25 and patent US 6133467, example 3.
  • HY-W015600R
    2-Acetamidophenol (Standard)
    Inhibitor
    2-Acetamidophenol (Standard) is the analytical standard of 2-Acetamidophenol. This product is intended for research and analytical applications. 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.
  • HY-177291
    LAB687
    Inhibitor
    LAB687 is a microsomal triglyceride transfer protein (MTP) inhibitor with an IC50 of 0.9 nM for apolipoprotein B (apoB) secretion in HepG2 cells. LAB687 also acts as a Smoothened (Smo) antagonist, with IC50 values of 2.48 μM and 3.42 μM against mouse and human Smo receptors, respectively. LAB687 reduces triglyceride and low-density lipoprotein cholesterol (LDL-C) levels, and inhibits the Hedgehog signaling pathway. LAB687 can be used in studies related to Hedgehog-dependent cancers.
  • HY-167873
    Habenariol
    Inhibitor
    Habenariol is a substantial phenolic antioxidant activity that can be isolated from the freshwater orchid, Habenaria repens.
  • HY-18778B
    Obicetrapib potassium
    Inhibitor
    Obicetrapib (TA-8995; DEZ-001) potassium is an orally active cholesteryl ester transfer protein (CETP) inhibitor. Obicetrapib potassium potently reduces atherogenic lipoproteins (such as LDL-C, ApoB, Lp (a)) and increases HDL-C. Obicetrapib potassium can be used for the research of dyslipidemia and atherosclerotic cardiovascular disease (ASCVD).