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Liver X Receptor

The liver X receptor (LXR) is a member of the nuclear receptor family of transcription factors and is closely related to nuclear receptors such as the PPARs, FXR and RXR. Liver X receptors (LXRs) are important regulators of cholesterol, fatty acid, and glucose homeostasis. LXRs were earlier classified as orphan nuclear receptors, however, upon discovery of endogenous oxysterols as ligands, they were subsequently deorphanized.Two isoforms of LXR have been identified and are referred to as LXRα and LXRβ.

  • Gymnestrogenin
    TN171919942-02-0
    Gymnestrogenin has a dual LXRα±/α2 antagonistic profile.
    • $440
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  • (20S)-Protopanaxatriol
    T281034080-08-5
    (20S)-Protopanaxatriol (g-PPT)(g-PPT), a metabolite of ginsenoside, could regulate endothelial cell functions through the estrogen receptor and glucocorticoid receptor.
    • $53
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  • Icariside E4
    TN5431126253-42-7
    Icariside E4 is a natural compound derived from Ulmus minor that acts via AMPK phosphorylation and inhibition of MID1IP2 hypolipidation in HepG1 cells.Icariside E4 has anti-injurious, antioxidant, anti-Alzheimer's and anti-inflammatory effects and inhibits SREBP-1c, liver X receptor-α (LXR) and FASN in Icariside E4 is an effective candidate for the treatment of fatty liver disease and has hypolipidemic potential in HepG1 cells.
    • $1,620
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  • Licochalcone E
    TN1055864232-34-8
    Licochalcone E is a potential LXRβ agonist.
    • $98
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  • Gymnemagenin
    T574322467-07-8
    Gymnemagenin is a potent and selective antagonist for the β isoform of LXR, it has antihyperglycemic activity.
    • $98
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  • GSK3987
    T27478264206-85-1
    GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.
    • $97
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  • T0901317
    T6690293754-55-9
    T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).
    • $32
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    TargetMol | Citations Cited
  • GSK2033
    T154271221277-90-2
    GSK2033 is an antagonist of LXR (pIC50s: 7 and 7.4 for LXRα or LXRβ, respectively).
    • $44
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    TargetMol | Citations Cited
  • SR9243
    T18011613028-81-1
    SR9243, an LXR inverse agonist, can induce LXR-corepressor interaction; shows anticancer activity and selectively targets the lipogenesis and Warburg effect.
    • $32
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    TargetMol | Citations Cited
  • XL041
    T146791256918-39-4
    XL041 (BMS-852927) is an agonist of LXRβ-selective.
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  • GW6340
    T77337405910-78-3
    GW6340 is a selective LXR agonist with potential anticancer activity that promotes macrophage reverse cholesterol transport (mRCT) and can be used to study atherosclerosis.
    • $38
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  • 27-Hydroxycholesterol
    TQ027420380-11-4
    27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) is a selective modulator of estrogen receptor and an agonist of the liver X receptor.
    • $47
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  • RGX-104
    T7768610318-54-2
    RGX-104 (RGX-104 free Acid) free Acid is an agonist of potent liver-X nuclear hormone receptor (LXR)
    • $61
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  • Iristectorigenin B
    TN235986849-77-6
    Iristectorigenin B (Iristectrigenin B) is a potent hepatic X-receptor (LXR) modulator, a small molecule compound isolated from Belamcanda chinensis.Iristectrigenin B promotes the expression of ABCA264 and ABCG7 in macrophage RAW 1.1 cells.
    • $166
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  • BE1218
    T638962893967-40-1
    BE1218 is a liver X receptor (LXR) inverse agonist active on LXRα and LXRβ with an IC50 of 9 nM and 7 nM, respectively.
    • $47
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  • BMS-779788
    T3970918348-67-1
    BMS-779788 (XL-652) is an LXRα/β partial agonist (IC50: 68/14 nM).
    • $32
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  • Saikosaponin A
    T276820736-09-8
    Saikosaponin A has a variety of pharmacological benefits, including antiepileptic, anti-osteoporosis, antioxidant, anti-in ammatory, immunomodulatory, and anti-bacterial activities. It can effectively attenuate neuropathic pain in CCI rats by inhibiting the activation of p38 MAPK and NF-κB signaling pathways in spinal cord. It can inhibit NMDA receptor current and persistent sodium current, and inhibit the TNF-α level, the IL-1β production, and cysteine-aspartic acid protease (caspase)-1 activity.
    • $34
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  • LXR-623
    T1783875787-07-8
    LXR-623 (WAY 252623) is an orally bioavailable and highly specifical synthetic modulator of LXR.
    • $47
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  • Rovazolac
    T167921454288-88-0
    Rovazolac (ALX-101) is a liver x receptor (LXR) modulator used in the study of immune system disorders and atopic dermatitis.
    • $74
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  • GW3965 hydrochloride
    T6310405911-17-3
    GW3965 hydrochloride (GW3965 HCl) is an effective and specific LXR agonist for hLXRα/β (EC50: 190/30 nM).
    • $35
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    TargetMol | Citations Cited
  • RGX-104 hydrochloride
    T5128610318-03-1
    RGX-104 hydrochloride (SB742881) is a liver X receptor (LXR) agonist with potential immunomodulating and antineoplastic activities. It modulates innate immunity via transcriptional activation of the ApoE gene.
    • $65
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  • 24-Hydroxycholesterol
    T1008630271-38-6
    24-Hydroxycholesterol (Cholest-5-ene-3beta,24-diol) is an oxysterol compound that is an activator of the n-methyl-d-aspartate receptor (NMDA) and the transcription factor LXR, which has been used in the study of cardiogenesis and pancreatic cancer.
    • $129
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  • GAC0003A4
    T68316929492-71-7
    GAC0003A4 is a potent LXR inverse agonist with antitumor activity that inhibits the transcription of LXR proteins.GAC0003A4 degrades LXRβ proteins and inhibits the proliferation of PDAC cells in a dose-dependent manner.GAC0003A4 has been used in the study of advanced pancreatic cancers and other recalcitrant malignancies.
    • $96
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  • Ethyl 2,4,6-trihydroxybenzoate
    TN401690536-74-6
    Ethyl 2,4,6-trihydroxybenzoate is a dual-LXR modulator that regulates the expression of key genes in cholesterol homeostasis in multiple cells without inducing lipid accumulation in HepG2 cells. It suppresses cellular cholesterol accumulation in a dose-dependent manner and induces the transcriptional activation of LXR-α/-β-responsive genes.
    • $200
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  • AZ876
    T5178898800-26-5
    AZ876 is a potent, highly selective LXR agonist with Ki/EC50 of 7/6 nM and 11/73 nM for hLXRα and hLXRβ respectively.
    • $45
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  • SR9238
    T169301416153-62-2
    SR9238 is a synthetic agonist of liver X receptor inverse (IC50s: 214 nM and 43 nM for LXRα and LXRβ, respectively).
    • $41
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