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

LXR

Liver X receptor

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 99.89%
    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 99.92%
    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 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 99.96%
    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-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-N12619
    12R,13S-Dihydroxyfumitremorgin C
    Agonist
    12R,13S-Dihydroxyfumitremorgin C (compound 1) is a LXRα agonist.
    12R,13S-Dihydroxyfumitremorgin C
  • 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-101442
    SR9238
    Antagonist 99.87%
    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 99.42%
    (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-N0246
    Saikosaponin A
    Activator 99.31%
    Saikosaponin A is an active component of Bupleurum chinensis, up-regulates LXRα expression, with potent anti-inflammatory activity.
    Saikosaponin A
  • 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-139576B
    Larsucosterol (trimethylamine)
    Antagonist ≥98.0%
    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
  • 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-16940
    24(S)-Hydroxycholesterol
    Agonist 99.55%
    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-19919
    BMS-779788
    Agonist 99.86%
    BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
    BMS-779788
Cat. No. Product Name / Synonyms Application Reactivity