lxr

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.

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.

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

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.

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

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

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

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.

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

LXR (Liver X receptor) agonist 1 is a potent agonist targeting LXR-α (AC50: 1.5 nM) and LXR-β (AC50: 12 nM), with demonstrated research potential in atherosclerosis.

BE1218 is a liver X receptor (LXR) inverse agonist, active on LXRα and LXRβ, with IC50 values of 9 nM and 7 nM, respectively.

LXR agonist 2 is a potent agonist of the LXR (liver X receptor). LXR agonist 2 stabilises NCOA1 (coactivator), which in turn agonises the LXR.

LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, targeting LXRβ (IC50: 0.36 μM) and LXRα (IC50: 2.25 μM). It serves as an adipogenesis inhibitor, downregulating LXR target genes SREBP-1c, ACC, FAS, and SCD-1, and demonstrates hypolipidemic activity in Triton WR-1339-induced hyperlipidemic mice.

Compound 10, Aminooxy CatB-LXR, constitutes an agent-linker conjugate for antibody-drug conjugates (ADC) [1].

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

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.

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). .

Larsucosterol ammonium salt is the salt form of Larsucosterol (DUR-928) and a derivative of 25HC3S.Larsucosterol is a DNA methyltransferase inhibitor (DNMT), a potent hepatic X-receptor (LXR) antagonist, an endogenous oxysterol sulfate, and an epigenetic modulator, regulate lipid metabolism, reduce inflammation and treat liver disease.

GW3965 is a potent and selective agonist of liver X receptor (LXR) with EC50 values of 190 nM for hLXRα and 30 nM for hLXRβ [1] [2] [3].

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).