LXR

GW3965 HCl is a selective and orally active liver X receptor (LXR) full agonist.

Mogroside II-A2, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.

T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively

Cerpegin is a naturally occurring pyridinone alkaloid isolated from Roxb, a tradional indian medicine used as an anti-inflammatory, analgesic, antiulcer and tranquilizer.

GW3965 is a potent, selective LXR agonist for hLXRα and hLXRβ with EC50 of 190 and 30 nM, respectively.

Sobetirome is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively to TRβ-1 with EC50 of 0.16 μM.

SR9243 is a potent and selective LXR inverse agonist. SR9243 kills cancer cells by inhibiting lipid production and the Warburg effect. It induces cell death in multiple types of cancer and does not cause the side effects that have derailed previous attempts to target these processes.

(20S)-Protopanaxatriol is a metabolite of ginsenoside, 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.

SR9238 is a potent and selective LXR inverse agonist (IC50 values are 43 and 214 nM for LXRβ and LXRα, respectively).

GSK-2033 is a potent cell-active LXR antagonist (pIC50 = 7.5). It enhances T-cell proliferation and blocks T 0901317-antiproliferative activity on T-cells and is cell permeable.

Rovazolac is a liver x receptor (LXR) modulator extracted from patent WO2013130892A1.

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

RGX-104 is a small-molecule LXR agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.

BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.

AZ876 is a novel high-affinity LXR agonist.

LXR-623 is a brain-penetrant partial LXRα and full LXRβ agonist, with IC50s of 24 nM and 179 nM, respectively.

RGX-104 free Acid is an orally bioavailable and potent liver-X nuclear hormone receptor (LXR) agonist that modulates innate immunity via transcriptional activation of the ApoE gene.

Yamogenin, a diastereomer of diosgenin, acts as an antagonist of the liver X receptor (LXR). It has been shown to inhibit triacylglyceride (TG) accumulation in HepG2 hepatocytes by downregulating fatty acid synthesis gene expression. This steroidal saponin exhibits in vitro cytotoxic, antioxidant, and antimicrobial properties, inducing cell death through both extrinsic and intrinsic apoptosis pathways. Yamogenin has potential applications in research focused on gastric cancer.

Taraxasterol is a pentacyclic triterpenoid that acts as an LXRα activator, demonstrating significant anti-inflammatory properties. Isolated from Taraxacum mongolicum, this compound has potential applications in the study of immune-inflammatory diseases, contributing to our understanding of metabolic regulation and inflammatory pathways. Researchers exploring therapeutic strategies for inflammatory conditions may find Taraxasterol an invaluable tool for investigation.

UAB116 is an agonist of the Liver X Receptor (LXR) and Retinoid X Receptor (RXR). It exhibits significant biological activity by diminishing the metastatic phenotype in hepatoblastoma, primarily through inhibition of the Wnt/β-Catenin signaling pathway via upregulation of TRIM29. UAB116 effectively reduces cell proliferation, stemness, and invasiveness in metastatic hepatoblastoma cells, making it a valuable tool for research in cancer biology and therapeutic development.

Saringosterol is an oral steroid and a potent LXR agonist derived from Sargassum muticum. It is known to effectively lower cholesterol levels while inhibiting the mRNA and protein expression of key regulators such as peroxisome proliferator-activated receptor γ (PPARγ) and CCAAT enhancer-binding protein α (C/EBPα). Due to its multifaceted biological activities, Saringosterol is utilized in research related to obesity, atherosclerosis, tuberculosis, and potential antidepressant therapies.

GAC0003A4 is an LXR (liver X receptor) degrader that inhibits LXR transcriptional activity. It effectively promotes the degradation of LXRβ protein, thereby decreasing its biological function. This compound shows potential for research applications in advanced pancreatic cancer and other refractory malignancies, making it a valuable tool for studying LXR-related pathways in cancer biology.