1. Signaling Pathways
  2. Metabolic Enzyme/Protease
    Vitamin D Related/Nuclear Receptor
  3. LXR

LXR

Liver X receptor

LXRs (Liver X Receptor α and β) are members of the nuclear hormone receptor superfamily of ligand-activated transcription factors. LXRs are oxysterol-activated transcription factors that upregulate a suite of genes that together promote coordinated mobilization of excess cholesterol from cells and from the body. The LXRs, like other nuclear receptors, are anti-inflammatory, inhibiting signal-dependent induction of pro-inflammatory genes by nuclear factor-κB, activating protein-1, and other transcription factors.

LXRα is expressed predominately in some tissues, including the liver, kidney, macrophages, and adipose tissue. However, LXRβ is ubiquitously expressed. Activating LXRα (mainly expressed in liver) results in high triglyceride production, and growing evidence suggests that selective LXRβ agonists can reduce this side effect.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-10627AR
    GW3965 hydrochloride (Standard)
    Agonist
    GW3965 (hydrochloride) (Standard) is the analytical standard of GW3965 (hydrochloride). This product is intended for research and analytical applications. GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
    GW3965 hydrochloride (Standard)
  • HY-14353
    GSK-9772
    Modulator
    GSK-9772 is a Liver X Receptor (LXR) modulator of the N-phenyl tertiary amine class (NPTAs) with high affinity for LXR β ligand (IC50=30 nM). GSK-9772 has anti-inflammatory activity by binding to LXR, specifically by interacting with the region associated with the transcriptional repression function of the receptor, thereby inhibiting the expression of pro-inflammatory genes. GSK-9772 can be used in the study of inflammatory and neurodegenerative diseases.
    GSK-9772
  • HY-N2078R
    Yamogenin (Standard)
    Antagonist
    Yamogenin (Standard) is the analytical standard of Yamogenin. This product is intended for research and analytical applications. Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes. Yamogenin is a steroidal saponin that can be obtained from plant species with in vitro cytotoxicity, antioxidant, and antimicrobial properties. Yamogenin induces cell death via the extrinsic and intrinsic way of apoptosis. Yamogenin inhibits protein denaturation with an IC50 of 1421.92 μg/mL. Yamogenin can be studied in research on gastric cancer.
    Yamogenin (Standard)
  • HY-138007
    SR-1903
    Agonist
    SR-1903 is an inverse agonist of RORγ and PPARγ (IC50 of ∼100 nM and 209 nM for RORγ and PPARγ, respectively) and a LXR agonist. SR-1903 exhibits anti-inflammatory and anti-diabetic efficacy in collagen-induced arthritis and diet-induced obesity mouse models.
    SR-1903
  • HY-108688R
    GSK2033 (Standard)
    Antagonist
    GSK2033 (Standard) is the analytical standard of GSK2033 (HY-108688). This product is intended for research and analytical applications. GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
    GSK2033 (Standard)
  • HY-10626R
    T0901317 (Standard)
    Agonist
    T0901317 (Standard) is the analytical standard of T0901317. This product is intended for research and analytical applications. T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
    T0901317 (Standard)
  • HY-18282R
    AZ876 (Standard)
    Agonist
    AZ876 (Standard) is the analytical standard of AZ876. This product is intended for research and analytical applications. AZ876 is a selective, orally active agonist of liver X receptor (LXRα/β) (Ki=0.007 μM [LXRα, human], 0.011 μM [LXRβ, human]. AZ876 induces the expression of target genes such as ABCA1 and ABCG1, promotes reverse cholesterol transport (RCT) and regulates lipid metabolism and anti-inflammatory effects. AZ876 increases cardiac polyunsaturated fatty acid levels, reduces myocardial fibrosis, and reduces lesion area and monocyte adhesion in atherosclerosis models. AZ876 can be used in cardiovascular disease research, such as preventing and treating β-adrenergic-induced cardiac diastolic dysfunction and inhibiting the progression of atherosclerosis.
    AZ876 (Standard)
  • HY-10627R
    GW3965 (Standard)
    Agonist
    GW3965 (Standard) is the analytical standard of GW3965 (HY-10627). This product is intended for research and analytical applications. GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
    GW3965 (Standard)
  • HY-180863
    NR1H3 modulator-1
    NR1H3 modulator-1 is a NR1H3 modulator.
    NR1H3 modulator-1
  • HY-N4247R
    Kuwanon G (Standard)
    Activator
    Kuwanon G (Standard) is the analytical standard of Kuwanon G (HY-N4247). This product is intended for research and analytical applications. Kuwanon G is a flavonoid compound and an antagonist of the bombesin receptor. Kuwanon G has multiple activities such as bactericidal, anti-tumor, anti-inflammatory, antioxidant, anti-atherosclerotic, and neuroprotective effects. Kuwanon G exhibits strong antibacterial activity against oral pathogens, especially cariogenic bacteria and periodontal pathogens. Kuwanon G can induce apoptosis and inhibit proliferation, migration, and invasion of tumor cells. Kuwanon G can be used in the research of diseases such as gastric cancer and atherosclerosis.
    Kuwanon G (Standard)
  • HY-10629R
    LXR-623 (Standard)
    Agonist
    LXR-623 (Standard) is the analytical standard of LXR-623. This product is intended for research and analytical applications. LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
    LXR-623 (Standard)
Cat. No. Product Name / Synonyms Application Reactivity