lxrβ

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

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

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).

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

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

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).

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

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

LXR agonist4 is a selective LXR inverse agonist, with IC50 values of 7.6 μM for LXRα and 2.9 μM for LXRβ. It exhibits selectivity for RORα and FXR. Additionally, LXR agonist4 markedly inhibits the expression of SREBP1c without affecting the expression of ABCA1 or APOE. It possesses anti-lipogenic properties and can prevent fat accumulation induced by fatty acids. This compound is useful for research in atherosclerosis and metabolic dysfunction-associated steatotic liver disease (MASLD).

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.

LXRmodulator-1 (Compound 21/3) is an LXR regulator with an EC50 of less than 100 nM. It can be utilized in the study of LXR-mediated conditions, such as non-alcoholic fatty liver disease.

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.

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

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). .

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.

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.

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

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

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.

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