1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. LOX-1

LOX-1

Lectin-like oxidized low-density lipoprotein receptor-1

Unlike native low-density lipoprotein (LDL), modified LDL such as oxidized, carbamylated, or acetylated LDL are not recognized by the native LDL receptor (LDL-R).1 Rather, modified LDL binds to the lectin-like oxidized LDL receptor-1 (LOX-1).Upon activation by modified LDL, LOX-1 induces endothelial dysfunction and uptake of the modified lipids.2 Endothelial dysfunction is the first stage in atherogenesis.3 Thus, the identification of LOX-1 through expression cloning as a major receptor for oxLDL in endothelial cells (ECs) supports a putative role for modified LDL in atherogenesis and has taken centre stage in cardiovascular research.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-23999
    BI-0115
    99.71%
    BI-0115 is a selective inhibitor of LOX-1 (IC50=5.4 µM) that blocks cellular uptake of oxLDL. BI-0115 binding triggers receptor inhibition by formation of dimers of the homodimeric ligand binding domain.
    BI-0115
  • HY-149922
    DKI5
    Inhibitor 98.12%
    DKI5, also known as (E)-N’-benzylidenehydrazinecarbothiohydrazide, is a LOX-1 inhibitor with an IC50 value of 22.5 μM.
    DKI5
  • HY-P99646
    Golocdacimab
    Inhibitor 99.09%
    Golocdacimab (MEDI6570) is a fully human anti-LOX-1 monoclonal antibody. Golocdacimab (MEDI6570) has the potential for the research of type 2 diabetes.
    Golocdacimab
  • HY-149269
    COX-2-IN-30
    Inhibitor
    COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
    COX-2-IN-30
  • HY-116763
    COX-2/5-LOX-IN-4
    Inhibitor
    COX-2/5-LOX-IN-4 (Compound 1) is a dual inhibitor that acts on both COX-2 and 5-LOX, with IC50 values of 0.05 μM for COX-2 and 0.003 μM for 5-LOX. By inhibiting the arachidonic acid metabolism pathway, COX-2/5-LOX-IN-4 reduces the production of prostaglandins and leukotrienes, alleviating inflammatory responses. In a rat ear edema model, intravenous administration (0.01 and 0.1 mg/kg) reduced edema by 41% and 44%, respectively, demonstrating significant anti-inflammatory effects. COX-2/5-LOX-IN-4 shows promise for studying the mechanisms of inflammatory diseases.
    COX-2/5-LOX-IN-4
Cat. No. Product Name / Synonyms Application Reactivity