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-10626
    T0901317
    		Agonist 99.85%
    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-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-108688
    GSK2033
    		Antagonist 99.53%
    GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
    GSK2033
  • HY-N2371
    27-Hydroxycholesterol
    		Agonist 99.77%
    27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.
    27-Hydroxycholesterol
  • HY-10627
    GW3965
    		Agonist 99.80%
    GW3965 is a potent, selective liver X receptor (LXR) agonist with EC50s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.
    GW3965
  • HY-182014
    TLC-2716
    		Inhibitor
    TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRα and LXRβ, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRα/β transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders.
    TLC-2716
  • HY-179278
    LXR agonist 4
    		Agonist
    LXR agonist 4 is a selective LXR inverse agonist with IC50 values of 7.6 (LXRα) and 2.9 μM (LXRβ), respectively. LXR agonist 4 exhibits selectivity over RORα and FXR. LXR agonist 4 robustly suppresses SREBP1c expression without altering ABCA1 or APOE. LXR agonist 4 displays antilipogenic properties and resolves fatty acid-induced steatosis. LXR agonist 4 can be used for the research of atherosclerosis and metabolic dysfunction-associated steatotic liver disease (MASLD).
    LXR agonist 4
  • HY-181226
    LXR modulator-1
    		Modulator
    LXR modulator-1 (Compound 21/3) is a LXR modulator with an EC50 of less than 100 nM. LXR modulator-1 can be used for studying LXR-mediated diseases such as non-alcoholic fatty liver disease.
    LXR modulator-1
  • HY-10629
    LXR-623
    		Agonist 99.95%
    LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
    LXR-623
  • HY-16940
    24(S)-Hydroxycholesterol
    		Agonist 99.75%
    24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
    24(S)-Hydroxycholesterol
  • HY-113224
    Desmosterol
    		Activator 99.84%
    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 . 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 .
    Desmosterol
  • HY-16972
    SR9243
    		Antagonist 99.17%
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
    SR9243
  • 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-N0835
    (20S)-Protopanaxatriol
    		Inhibitor 99.93%
    (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-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-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-129098
    DMHCA
    		Agonist 99.91%
    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 99.76%
    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-116969
    22(R)-Hydroxycholesterol
    		Agonist 99.86%
    22(R)-Hydroxycholesterol (Narthesterol) is an endogenous LXR agonist. 22(R)-Hydroxycholesterol (Narthesterol) can be used for tangier disease research.
    22(R)-Hydroxycholesterol
  • 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
Cat. No. Product Name / Synonyms Application Reactivity