lxrβ

GSK2033 is an antagonist of LXR (pIC50s: 7 and 7.4 for LXRα or LXRβ, respectively).

BMS-779788 (XL-652) is an LXRα/β partial agonist (IC50: 68/14 nM).

LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with an EC50 of 7 nM.

LXRβ agonist-3 is a potent and selective LXRβ (liver X receptor β) agonist (EC50: 0.095 μM). LXRβ agonist-3 effectively inhibits U87EGFRvIII cells (IC50: 3.75 μM). .

GW6340 is a selective LXR agonist with potential anticancer activity that promotes macrophage reverse cholesterol transport (mRCT) and can be used to study atherosclerosis.

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.

GW3965 hydrochloride (GW3965 HCl) is an effective and specific LXR agonist for hLXRα β (EC50: 190 30 nM).

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.

SR9243, an LXR inverse agonist, can induce LXR-corepressor interaction; shows anticancer activity and selectively targets the lipogenesis and Warburg effect.

(20S)-Protopanaxatriol (g-PPT)(g-PPT), a metabolite of ginsenoside, could regulate endothelial cell functions through the estrogen receptor and glucocorticoid receptor.

DMHCA is a selective LXR agonist with anti-inflammatory activity, which induces ABCA1 expression and upregulates FASN and SREBP-1alpha gene expression.

Larsucosterol trimethylamine (DUR-928 trimethylamine) is a potent liver X receptor (LXR) antagonist that modulates endogenous epigenetics, reduces lipid accumulation in hepatocytes, attenuates lipopolysaccharide (LPS) and TNFα-induced inflammatory responses in macrophages, and alleviates LPS- and acetaminophen (ATMP)-induced multi-organ damage.

Iristectorigenin B (Iristectrigenin B) is a potent hepatic X-receptor (LXR) modulator and a small molecule compound isolated from *Belamcanda chinensis*. It promotes the expression of ABCA264 and ABCG7 in macrophage RAW 1.1 cells.

27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) is a selective modulator of estrogen receptor and an agonist of the liver X receptor.

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).

XL041 (BMS-852927) is an agonist selective for LXRβ.

SR9238 is a synthetic agonist of liver X receptor inverse (IC50s: 214 nM and 43 nM for LXRα and LXRβ, respectively).

LXR-623 (WAY 252623) is an orally bioavailable and highly specifical synthetic modulator of LXR.

7α,24(S)-Dihydroxycholesterol ((3β,7α,24S)-Cholest-5-ene-3,7,24-triol) acts as a ligand for liver X receptors (LXR), specifically binding to the ligand-binding domains of LXRα and LXRβ. This compound is synthesized through the E-α,β-unsaturated ketone process, starting with arsindole and J-secondary-butyl dimethylsiloxy-bis-positive-5-cholestenal as the initial materials. It undergoes a series of transformations to produce 7α,24(S)-dihydroxycholesterol.

PFM046 is an antagonist of the liver X receptor (LXR), effectively inhibiting the activation of LXRα and LXRβ, with IC50 values of 2.04 μM and 1.58 μM respectively. It reduces the expression of SCD1 and FASN while increasing ABCA1 expression, and demonstrates antitumor activity in mouse models.

LXRα agonist 1 (Compound 40) is a selective activator of LXRα, with an EC50 of 42 nM, and also demonstrates some activation effects on LXRβ, with an EC50 of 266 nM. It promotes target gene transcription by stabilizing the ligand-binding domain (LBD) of LXRα. When combined with the Raf inhibitor Sorafenib, LXRα agonist 1 shows significant antitumor activity in liver cancer cells. This compound is applicable in research focused on lipotoxicity-related cancers.

E17110 is an LXRβ agonist. E17110 exhibited a significant activation effect on LXRβ (EC50: 0.72 μmol/L). E17110 also increased the expression of ABCA1 and ABCG1 in RAW264.7 macrophages. E17110 significantly decreased cellular lipid accumulation and promoted cholesterol efflux in RAW264.7 macrophages.

IMB-808 is an LXRα β dual agonist that promotes ABCA1 expression and cholesterol efflux without inducing lipidogenesis in HepG2 cells. IMB-808 can be used in atherosclerosis research.

GSK3987 is an LXR ligand. GSK3987 recruits the steroid receptor coactivator-1 to human LXRalpha and LXRbeta with EC50s of 40 nM.