LXR-623 is a novel and brain-penetrant LXR agonist with IC50 values of 179 and 24 nM for LXRα and LXRβ, respectively.

Saikosaponin A, a natural product isolated and purified from the root of Bupleurum chinense DC., with antioxidant activity, has an inhibitory activity against allergic asthma and an anti-inflammatory activity by inhibiting the MAPK and NF-κB pathways in LPS-stimulated RAW 264.7 cells, shows the most potent cytotoxicity against human cancer cells, and is an inhibitory for cell growth and DNA synthesis with 50-μg/mL.

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

T0901317 is a selective agonist for LXR and FXR with EC50 of 50 nM and 5 μM, respectively.

SR9243 is a LXR inverse agonist that induces LXR-corepressor interaction and shows anticancer activity and selectively targets the warburg effect and lipogenesis.

SR9238 is a potent synthetic LXR antagonist with IC50s of 214 nM and 43 nM for LXRα and LXRβ respectively.

AZ876 is a high-affinity LXR agonist.

RGX104 free acid is an agonist of liver-X nuclear hormone receptor (LXR), it can regulate the immune process by activating the ApoE gene.

GW3965 HCl is a selective and non-steroidal LXR agonist with EC50 values of 190 and 30 nM for hLXRα and hLXRβ, respectively.

27-Hydroxycholesterol is an endogenous oxysterol with multiple biological functions, including activity as a selective estrogen receptor modulator (SERM) (a mixed, tissue-specific agonist-antagonist of the estrogen receptor (ER)) and as an agonist of the liver X receptor (LXR). It is a metabolite of cholesterol that is produced by the enzyme CYP27A1.