lxrα

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

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.

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

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

TUG-1375 is an Agonist of Thiazolidine Free Fatty Acid Receptor 2

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

Gymnestrogenin has a dual LXRα± α2 antagonistic profile.

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.

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.

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

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.

AZ-2 is an inducer of ABCA1 and apoE. It enhances ABCA1 activity and decreases P2X7 receptor activity. AZ-2 activates endogenous LXR signaling but shows no direct LXRα or LXRβ agonist activity.

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.

22(S)-hydroxy Cholesterol is a synthetic oxysterol and a modulator of the liver X receptor (LXR). [1] t prevents monocyte chemoattractant protein 1 (MCP-1) expression induced by the LXR agonist GW 3965 in primary hepatocytes and downregulates mRNA expression of the LXR target genes CD36, ACSL1, and SCD-1 in human myotubes. It decreases triacylglycerol and diacylglycerol synthesis from labeled palmitate and acetate, respectively, in human myoblasts by 50% when used at a concentration of 10 uM. 22(S)-hydroxy Cholesterol also reduces fatty acid synthase (FAS) reporter activity through an LXR response element in the promoter region in COS-1 cells transfected with RXRα and LXRα and decreases the expression of MCP-1 and CCR2 in a mouse model of chronic ethanol consumption.[1] [2] Dietary supplementation of 22(S)-hydroxy cholesterol (30 mg/kg per day) leads to less body weight gain and lower liver triacylglycerol levels in rats when fed either a regular chow or high-fat diet as well as prevents an increase in plasma triacylglycerol levels resulting from a high-fat diet.[3]

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

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

CAY10771 is a dual agonist of farnesoid X receptor (FXR) and peroxisome proliferator-activated receptor δ (PPARδ).1It activates FXR and PPARδ in reporter assays using HEK293T cells (EC50s = 0.94 and 1.5 μM, respectively) and is selective for these receptors over retinoic acid receptor α (RARα), retinoid X receptor α (RXRα), PPARα, PPARγ, and liver X receptor α (LXRα) at 10 μM. 1.Schierle, S., Neumann, S., Heitel, P., et al.Design and structural optimization of dual FXR/PPARδ activatorsJ. Med. Chem.63(15)8369-8379(2020)

12R,13S-Dihydroxyfumitremorgin C (compound 1) acts as an LXRα agonist [1].

6-Thioinosine (6TI) is a purine antimetabolite, acts as an anti-adipogenesis agent.

Ibrolipim (NO-1886) attenuates high glucose-induced endothelial dysfunction in cultured human umbilical vein endothelial cells via PI3K Akt pathway.

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

Dendrogenin A (DDA) is a compound acting as a selective liver X receptor (LXR) modulator, cholesterol epoxide hydrolase inhibitor (Ki = 120 nM), and a metabolic product of cholesterol, originating from 5,6α-epoxy cholesterol through histamine conjugation via DDA synthase. This compound is present in non-cancerous human mammary epithelial cells and melanocytes, but absent or minimally present in various breast carcinoma, melanoma cells, and isolated human breast tumor tissues. DDA impedes the activation of LXRβ and LXRα induced by 22(R)-hydroxy cholesterol (IC50s = 76 and 362 nM, respectively), yet it also functions as a partial LXR agonist, boosting the protein levels of Nur77, NOR-1, LC3-I, and LC3-II in B16/F10 murine melanoma cells. It shows a preference for LXRα and LXRβ modulation while displaying selectivity over other receptors including pregnane X receptor (PXR), and various others at a concentration of 2.5 µM. Moreover, DDA enhances LC3-II protein levels in cancer cells and prompts autophagic cell death at specific concentrations. Notably, DDA (0.37 µg/kg) has been shown to diminish tumor growth in melanoma and mammary cancer murine models and promotes cancer cell differentiation both in vitro and in vivo.