liver x receptor

GW3965 hydrochloride (GW3965 HCl) belongs to synthetic small molecules and is a liver X receptor (LXR) agonist (hLXRα EC50 = 190 nM; hLXRβ EC50 = 30 nM) with subtype selectivity, cell permeability, and oral activity. This compound is used in research related to metabolism, inflammation, and neuropathic pain.

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

Rovazolac (ALX-101) is a liver x receptor (LXR) modulator used in the study of immune system disorders and atopic dermatitis.

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.

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

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

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.

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

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

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.

(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.

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.

AZ876 is a potent, highly selective LXR agonist with Ki/EC50 of 7/6 nM and 11/73 nM for hLXRα and hLXRβ respectively.

Gymnemagenin is a potent and selective antagonist for the β isoform of LXR, it has antihyperglycemic activity.

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

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).

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.

Yamogenin is a diastereomer of diosgenin, which we have identified as the compound responsible for the anti-hyperlipidemic effect of fenugreek.

RGX-104 (RGX-104 free Acid) free Acid is an agonist of potent liver-X nuclear hormone receptor (LXR)

Licochalcone E is a potential LXRβ agonist.