lxr

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.

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-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.

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.

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.

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.

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).

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.

Nagilactone B is extracted from the root bark of Podocarpus nagi and it also is a liver X receptor (LXR) agonist.

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

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

SIRT6 activator2 (compound 31) is a sirtuin6 activator known for its anti-lipid accumulation properties. It significantly downregulates LXR, SREBP-1c, and their target genes, making it valuable for research into lipid metabolism-related diseases.

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.