LXR Agonist

T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

GW3965 hydrochloride is a potent and selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

27-Hydroxycholesterol (27-OHC) is a selective estrogen receptor modulator and an agonist of the liver X receptor.

GW3965 is a potent, selective liver X receptor (LXR) agonist with EC₅₀s of 190 nM and 30 nM for hLXRα and hLXRβ, respectively.

AU403 is a potent, brain-penetrant, isoform-selective LXRβ/PPARδ dual agonist (EC₅₀ ≈ 45 nM for LXRβ and EC₅₀ ≈ 40 nM for PPARδ). AU403 is designed to bypass LXRα-driven hepatotoxicity. AU403 significantly improves cognitive functions and reduces amyloid-β plaque burden in 3xTg-AD mice. AU403 is a promising dual-acting agonist for the research of Alzheimer’s disease.

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

24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.

DMHCA, a potent and selective LXR agonist, specifically activates the cholesterol efflux arm of the LXR pathway without stimulating triglyceride synthesis. DMHCA has anti-inflammatory effects?and can be used for the research of cholesterol homeostasis diabetes.

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

22(R)-Hydroxycholesterol (Narthesterol) is an endogenous LXR agonist. 22(R)-Hydroxycholesterol (Narthesterol) can be used for tangier disease research.

AZ876 is a selective, orally active agonist of liver X receptor (LXRα/β) (K_i=0.007 μM [LXRα, human], 0.011 μM [LXRβ, human]. AZ876 induces the expression of target genes such as ABCA1 and ABCG1, promotes reverse cholesterol transport (RCT) and regulates lipid metabolism and anti-inflammatory effects. AZ876 increases cardiac polyunsaturated fatty acid levels, reduces myocardial fibrosis, and reduces lesion area and monocyte adhesion in atherosclerosis models. AZ876 can be used in cardiovascular disease research, such as preventing and treating β-adrenergic-induced cardiac diastolic dysfunction and inhibiting the progression of atherosclerosis.

GSK3987 is a pan LXRα/β agonist with EC₅₀s of 50 nM, 40 nM for LXRα-SRC1 and LXRβ-SRC1, respectively. GSK3987 increases the expression of ABCA1 and SREBP-1c. GSK3987 induces cellular cholesterol efflux and triglyceride accumulation.

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

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

LXRβ ligand 1 is a LXR β ligand-binding domain agonist, with an EC₅₀ of 57 μM and a K_i of 28 μM against human LXR β. LXRβ ligand 1 forms hydrogen bonds with His435, stabilizes the His-Trp activation switch, and locks the ligand-binding domain in an agonist conformation; its tert-butyl moiety occupies a hydrophobic subpocket, while its phenyl moiety forms a π-π stacking interaction with Phe329. LXRβ ligand 1 serves as a structural unit for the development of LXRβ modulators.

25-Hydroxytachysterol3 is the metabolite of Vitamin D3 (HY-15398). 25-Hydroxytachysterol3 inhibits the proliferation of epidermal keratinocytes and dermal fibroblasts, stimulates the expression of differentiation- and antioxidant-related genes in keratinocytes. 25-Hydroxytachysterol3 activates vitamin D receptor (VDR) and aryl hydrocarbon receptor (AhR), liver X receptor α/β (LXR α/β) and peroxisome proliferator-activated receptor γ (PPARγ), stimulates the expression of CYP24A1.

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

IMB-808 is a potent LXRα/β dual agonist with EC₅₀ values of 0.53 μM and 0.15 μM (0.15 μM, using GAL4-pGL4-luc reporter plasmid) for LXRβ and LXRα, respectively. IMB-808 promotes expression of genes related to reverse cholesterol transport (ABCA1 and ABCG1). IMB-808 can be used for the study of atherosclerosis research.

24S,25-Epoxycholesterol is an agonist for Liver X Receptor (LXR). 24S,25-Epoxycholesterol exhibits properties in regulating the cholesterol efflux, inhibiting tumor growth against gastric cancer and glioblastoma and inducing apoptosis in BMMC cells.

LXR (Liver X receptor) agonist 1 is potent LXR agonist with AC₅₀s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis.