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

LXR

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.

LXR Related Products (30):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-108688
    GSK2033
    Antagonist 99.37%
    GSK2033 is a LXR antagonist with pIC50s of 7 and 7.4 for LXRα or LXRβ, respectively.
  • HY-10627A
    GW3965 hydrochloride
    Agonist 99.73%
    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-N2371
    27-Hydroxycholesterol
    Agonist 99.38%
    27-Hydroxycholesterol is a selective estrogen receptor modulator and an agonist of the liver X receptor.
  • 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.
  • HY-125772
    Acetyl podocarpic acid anhydride
    Agonist
    Acetyl podocarpic acid anhydride is a potent, semisynthetic liver X receptor(LXR) agonist derived from extracts of the mayapple. Acetyl podocarpic acid anhydride has the potential to be useful for the prevention and treatment of atherosclerosis, especially in the context of low HDL levels.
  • HY-123402
    GSK3987
    Agonist
    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.
  • 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.
  • HY-N0835
    (20S)-Protopanaxatriol
    Inhibitor 99.42%
    (20S)-Protopanaxatriol is a metabolite of ginsenoside. (20S)-Protopanaxatriol works through the glucocorticoid receptor (GR) and oestrogen receptor (ER), and is also a LXRα inhibitor. (20S)-Protopanaxatriol shows a broad spectrum of antitumor effects.
  • HY-16972
    SR9243
    Antagonist 99.65%
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
  • HY-129098
    DMHCA
    Agonist 99.19%
    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.
  • HY-101973
    XL041
    Agonist 99.44%
    XL041 (BMS-852927) is an LXRβ-selective agonist.
  • 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-111498
    RGX-104 hydrochloride
    Agonist 99.96%
    RGX-104 hydrochloride is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.
  • HY-18282
    AZ876
    Agonist 99.26%
    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-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.
  • 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.
  • 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-19919
    BMS-779788
    Agonist
    BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
  • HY-109073
    Rovazolac
    Modulator 99.79%
    Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.
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