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

LXR

Liver X receptor

LXR

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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-10627A
    GW3965 hydrochloride
    		Agonist 99.96%
    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
  • HY-10626
    T0901317
    		Agonist 99.93%
    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
  • HY-108688
    GSK2033
    		Antagonist 98.22%
    GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
    GSK2033
  • HY-N2371
    27-Hydroxycholesterol
    		Agonist 99.74%
    27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.
    27-Hydroxycholesterol
  • HY-16972
    SR9243
    		Antagonist 98.88%
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
    SR9243
  • HY-N0246R
    Saikosaponin A (Standard)
    		Activator
    Saikosaponin A (Standard) is the analytical standard of Saikosaponin A. This product is intended for research and analytical applications. Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also act as a potential peroxisome proliferator-activated receptor-γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis.
    Saikosaponin A (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-149132
    Dendrogenin A
    Dendrogenin A (DDA) is a ligand for liver X receptor (LXR), that induces the expression of sodium/iodine symporter, and increases iodine uptake. Dendrogenin A induces cell differentiation of MCF-7, and reactivates the function of lactating cells. Dendrogenin A induces the expressions of the TSH receptor, thyroid peroxidase, and thyroglobulin, and affects thyroid hormone generation. Dendrogenin A exhibits cytotoxicity in cancer cell B-CPAP and 8505c with IC50 of 4.1 and 6.2 µM. Dendrogenin A arrests the cell cycle at G0/G1 phase.
    Dendrogenin A
  • HY-10629
    LXR-623
    		Agonist 99.48%
    LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
    LXR-623
  • HY-N1178
    Taraxasterol
    		99.41%
    Taraxasterol is a pentacyclic triterpenoid compound isolated from Taraxacum mongolicum. Taraxasterol is an LXRα activator, with metabolic and anti-inflammatory effects. Taraxasterol may be used in research on immune-inflammatory diseases.
    Taraxasterol
  • HY-N0246
    Saikosaponin A
    		Activator 99.31%
    Saikosaponin A is the main active ingredient in Bupleurum chinense, which can regulate lipid metabolism and promote cholesterol efflux in early atherosclerosis. In addition, Saikosaponin A may also serve as a potential peroxisome proliferator-activated receptor γ (PPAR-γ) agonist, significantly promoting the expression of PPAR-γ. Saikosaponin A can be used in the study of hyperlipidemic pancreatitis.
    Saikosaponin A
  • HY-101442
    SR9238
    		Antagonist 99.89%
    SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
    SR9238
  • HY-N2370
    24-Hydroxycholesterol
    		Activator 99.90%
    24-Hydroxycholesterol is a natural sterol, which serves as a positive allosteric modulator of N-Methyl-d-Aspartate (NMDA) receptorsR, and a potent activator of the transcription factors LXR.
    24-Hydroxycholesterol
  • HY-N0835
    (20S)-Protopanaxatriol
    		Inhibitor 99.91%
    (20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and estrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
    (20S)-Protopanaxatriol
  • HY-129098
    DMHCA
    		Agonist 99.80%
    DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects?and can be used for the research of cholesterol homeostasis diabetes.
    DMHCA
  • HY-111498A
    RGX-104
    		Agonist 99.97%
    RGX-104 is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
    RGX-104
  • HY-18282
    AZ876
    		Agonist 99.93%
    AZ876 is a potent and high-affinity LXR agonist. AZ876 displays 25-fold and 2.5-fold more potent than GW3965 (HY-10627) on human (h)LXRα and hLXRβ respectively.
    AZ876
  • HY-123402
    GSK3987
    		Agonist 99.75%
    GSK3987 is a pan LXRα/β agonist with EC50s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation.
    GSK3987
  • HY-139576B
    Larsucosterol (trimethylamine)
    		Antagonist
    Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
    Larsucosterol (trimethylamine)
  • HY-101973
    XL041
    		Agonist 99.19%
    XL041 (BMS-852927) is an LXRβ-selective agonist.
    XL041
Cat. No. Product Name / Synonyms Application Reactivity