1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. LXR

LXR

LXRs (Liver X Receptor α and β) are nuclear receptors that act as ligand-activated transcription factors. LXR activation causes upregulation of genes involved in reverse cholesterol transport (RCT), including ABCA1 and ABCG1 transporters, in macrophage and intestine.

LXRα/β are ligand-activated transcription factors of the nuclear hormone receptor superfamily that stimulate transcription of several genes, including ABCA1 and apoE. LXRα and LXRβ respond to the same oxysterol ligands and activate transcription as obligate heterodimeric complexes with retinoid X receptors.

Synthetic LXR agonists activate both LXRα and LXRβ, cross the blood-brain barrier, and efficiently induce expression of LXR target genes including ABCA1 and apoE.

LXR Related Products (20):

Cat. No. Product Name Effect Purity
  • HY-10626
    T0901317 Agonist 99.91%
    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.
  • HY-10627A
    GW3965 hydrochloride Agonist 99.70%
    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.
  • HY-108688
    GSK2033 Antagonist 99.37%
    GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
  • HY-N2371
    27-Hydroxycholesterol Agonist 99.38%
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • HY-111498
    RGX-104 Agonist 99.96%
    RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-16940
    24(S)-Hydroxycholesterol Agonist
    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.
  • HY-10629
    LXR-623 Agonist 99.51%
    LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.
  • HY-101973
    XL041 Agonist 99.44%
    XL041 (BMS-852927) is an LXRβ-selective agonist.
  • HY-101442
    SR9238 Antagonist 99.94%
    SR9238 is a synthetic liver X receptor (LXR) inverse agonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ, respectively.
  • HY-16972
    SR9243 Antagonist 99.65%
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
  • HY-N0835
    (20S)-Protopanaxatriol Inhibitor >98.0%
    (20S)-Protopanaxatriol is a metabolite of ginsenoside, works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor.
  • HY-N2370
    24-Hydroxycholesterol Activator >98.0%
    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.
  • HY-111498A
    RGX-104 free Acid Agonist 99.97%
    RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-19919
    BMS-779788 Agonist 98.23%
    BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
  • HY-18282
    AZ876 Agonist 99.89%
    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.
  • HY-109073
    Rovazolac Modulator 99.79%
    Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.
  • HY-N0246
    Saikosaponin A Activator 99.43%
    Saikosaponin A is an active component of Bupleurum falcatum, up-regulates LXRα expression, with potent anti-inflammatory activity.
  • HY-N3216
    Nagilactone B Agonist >98.0%
    Nagilactone B, extracted from the root bark of Podocarpus nagi, is a liver X receptor (LXR) agonist.
  • HY-N2273
    Gymnestrogenin Antagonist
    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.
  • HY-N2078
    Yamogenin Antagonist 99.20%
    Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
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