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-N3216
    Nagilactone B
    		Agonist ≥98.0%
    Nagilactone B is a liver X receptor (LXR) agonist.
    Nagilactone B
  • HY-137307
    Cholest-5-ene-3ß,22(S)-diol
    		Antagonist
    Cholest-5-ene-3ß,22(S)-diol ((22S)-Hydroxycholesterol) is an orally active oxysterol with no significant cytotoxic, oxidative, or inflammatory effects on human prokaryotic leukemia cells. Cholest-5-ene-3ß,22(S)-diol inhibits weight gain and increased serum triacylglycerol (TAG) levels in rat models.
    Cholest-5-ene-3ß,22(S)-diol
  • HY-154928
    GW6340
    		Agonist 99.64%
    GW6340 is an intestinal-specific LXR agonist. GW6340 promotes macrophage reverse cholesterol transport (mRCT).
    GW6340
  • HY-D1734
    FITC-GW3965
    		Agonist 98.0%
    FITC-GW3965 is a fluorescence-labelled liver X receptor β (LXRβ) agonist GW3965 (HY-10627). FITC-GW3965 is a tracer, that can be designed by replacing the trifluoromethyl of GW3965 with an amide to link the FITC. FITC-GW3965 can be used to study the function of LXRβ.
    FITC-GW3965
  • HY-W414823
    24,25-Epoxycholesterol
    		Agonist 99.80%
    24,25-Epoxycholesterol is an oxysterol agonist of the liver X receptor that can inhibit the activity of 3-hydroxy-3-methylglutaryl-CoA reductase (HMG-CoA reductase) in liver cells. 24,25-Epoxycholesterol regulates cholesterol metabolism in the liver.
    24,25-Epoxycholesterol
  • HY-N2273
    Gymnestrogenin
    		Antagonist 99.32%
    Gymnestrogenin is a pentahydroxytriterpene from the leaves of Gymnema sylvestre R.Br. Gymnestrogenin is a LXR antagonist with IC50s of 2.5 and 1.4 μM for LXRα and LXRβ transactivation, respectively. Gymnestrogenin reduces the transcriptional activity of LXR even on its own promoter, thus reducing the mRNA expression.
    Gymnestrogenin
  • HY-154825
    20-Hydroxyvitamin D3
    		≥98.0%
    20-Hydroxyvitamin D3 (20(OH)D3) is a hydroxy metabolite of vitamin D3. 20-Hydroxyvitamin D3 functions as a ligand for vitamin D receptor (VDR), aryl hydrocarbon receptor (AhR), liver X receptor (LXR), and retinoic acid-related orphan receptor (ROR). 20-Hydroxyvitamin D3 inhibits cell proliferation, induces differentiation. 20-Hydroxyvitamin D3 can be used for inflammatory and autoimmune diseases study.
    20-Hydroxyvitamin D3
  • 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-139576A
    Larsucosterol sodium
    		Antagonist
    Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1.
    Larsucosterol sodium
  • HY-100469
    LXRβ agonist-2
    		Agonist
    LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
    LXRβ agonist-2
  • HY-113224R
    Desmosterol (Standard)
    		Activator
    Desmosterol (Standard) is the analytical standard of Desmosterol. This product is intended for research and analytical applications. Desmosterol is a cholesterol-like molecule. In the Bloch pathway of cholesterol biosynthesis, Desmosterol is a direct precursor of cholesterol. As an endogenous metabolite, Desmosterol is used to study cholesterol metabolism [1]. Desmosterol is an LXR activator and SREBP inhibitor, which can suppress macrophage inflammasome activation and prevent vascular inflammation and atherosclerosis. A reduction in Desmosterol promotes the production of mitochondrial reactive oxygen species (ROS) in macrophages and pyrin domain-dependent inflammasome activation of NLRP3. Desmosterol holds potential for research in inflammation, metabolism, and cardiovascular diseases [1][2][3].
    Desmosterol (Standard)
  • HY-N1178R
    Taraxasterol (Standard)
    Taraxasterol (Standard) is the analytical standard of Taraxasterol. This product is intended for research and analytical applications. 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 (Standard)
  • HY-170570
    PFM046
    		Antagonist
    PFM046 is the antagonist for liver X receptor (LXR), that inhibits the activation of LXRα and LXRβ with IC50 of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models.
    PFM046
  • HY-146288
    LXR agonist 2
    		Agonist
    LXR agonist 2 (compound 18rr) is a potent LXR (liver X receptor) agonist. LXR agonist 2 can stabilize NCOA1 (co-activator), leading to LXR agonism.
    LXR agonist 2
  • HY-W754708
    Ouabagenin
    		Activator
    Ouabagenin is a naturally occurring LXR ligand with LXR selective agonist activity. Ouabagenin acts as an EC 3.6.3.9 (Na(+)/K(+)- transport ATPase) inhibitor.
    Ouabagenin
  • HY-173230
    ABCA1 inducer 2
    		Activator
    ABCA1 inducer 2 is a non-lipotropic ABCA1 inducer. ABCA1 inducer 2 upregulates the expression of ABCA1 by targeting the LXR pathway. ABCA1 inducer 2 can reduce ox-LDL-induced lipid accumulation and thus inhibit foam cell formation. ABCA1 inducer 2 has anti-atherosclerotic potential.
    ABCA1 inducer 2
  • HY-N0835R
    (20S)-Protopanaxatriol (Standard)
    		Inhibitor
    (20S)-Protopanaxatriol (Standard) is the analytical standard of (20S)-Protopanaxatriol. This product is intended for research and analytical applications. (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 (Standard)
  • HY-RS09529
    NR1H2 Human Pre-designed siRNA Set A
    		Inhibitor

    NR1H2 Human Pre-designed siRNA Set A contains three designed siRNAs for NR1H2 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.
    NR1H2 Human Pre-designed siRNA Set A
  • HY-173393
    LXRα agonist 1
    		Agonist
    LXRα agonist 1 (Compound 40) is a selective LXRα agonist (EC50: 42 nM). LXRα agonist 1 also has a certain agonistic effect on LXRβ (EC50: 266 nM). LXRα agonist 1 promotes target gene transcription by stabilizing the ligand binding domain (LBD) of LXRα. LXRα agonist 1 exhibits potent antitumor effects in hepatocellular carcinoma cells when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the study of lipotoxic cancers.
    LXRα agonist 1
  • HY-134969
    TFCA
    		Antagonist
    TFCA is a liver X receptor α (LXRα) antagonist. TFCA inhibits ligand-activated LXRα coactivation and transcriptional expression of the downstream target genes involved in fatty acid synthesis. TFCA attenuates ligand-induced lipogenesis and fatty liver by selectively inhibiting LXRα in the liver.
    TFCA
Cat. No. Product Name / Synonyms Application Reactivity