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Metabolism

ATP Citrate Lyase

(11)

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(36)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(33)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(85)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(47)

Stearoyl-CoA Desaturase (SCD)

Liver X Receptor

The liver X receptor (LXR) is a member of the nuclear receptor family of transcription factors and is closely related to nuclear receptors such as the PPARs, FXR and RXR. Liver X receptors (LXRs) are important regulators of cholesterol, fatty acid, and glucose homeostasis. LXRs were earlier classified as orphan nuclear receptors, however, upon discovery of endogenous oxysterols as ligands, they were subsequently deorphanized.Two isoforms of LXR have been identified and are referred to as LXRα and LXRβ.

Filter HomeSignaling PathwaysMetabolismLiver X Receptor

GW3965 hydrochloride

T6310405911-17-3

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

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GSK2033

T154271221277-90-2

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

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27-Hydroxycholesterol

TQ027420380-11-4

27-Hydroxycholesterol (25(R)-27-hydroxy Cholesterol) is a selective modulator of estrogen receptor and an agonist of the liver X receptor.

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SR9243

T18011613028-81-1

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

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AZ876

T5178898800-26-5

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

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RGX-104 hydrochloride

T5128610318-03-1

RGX-104 hydrochloride (SB742881) is a liver X receptor (LXR) agonist with potential immunomodulating and antineoplastic activities. It modulates innate immunity via transcriptional activation of the ApoE gene.

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Licochalcone E

TN1055864232-34-8

Licochalcone E is a potential LXRβ agonist.

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Saikosaponin A

T276820736-09-8

Saikosaponin A has a variety of pharmacological benefits, including antiepileptic, anti-osteoporosis, antioxidant, anti-in ammatory, immunomodulatory, and anti-bacterial activities. It can effectively attenuate neuropathic pain in CCI rats by inhibiting the activation of p38 MAPK and NF-κB signaling pathways in spinal cord. It can inhibit NMDA receptor current and persistent sodium current, and inhibit the TNF-α level, the IL-1β production, and cysteine-aspartic acid protease (caspase)-1 activity.

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T0901317

T6690293754-55-9

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).

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LXR-623

T1783875787-07-8

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

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SR9238

T169301416153-62-2

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

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Larsucosterol trimethylamine

T74147

Larsucosterol trimethylamine (DUR-928 trimethylamine) is a potent liver X receptor (LXR) antagonist that modulates endogenous epigenetics, reduces lipid accumulation in hepatocytes, attenuates lipopolysaccharide (LPS) and TNFα-induced inflammatory responses in macrophages, and alleviates LPS- and acetaminophen (ATMP)-induced multi-organ damage.

$192

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(20S)-Protopanaxatriol

T281034080-08-5

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

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RGX-104

T7768610318-54-2

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

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GSK3987

T27478264206-85-1

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

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DMHCA

T4089879066-03-8

DMHCA is a selective LXR agonist with anti-inflammatory activity, which induces ABCA1 expression and upregulates FASN and SREBP-1alpha gene expression.

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Iristectorigenin B

TN235986849-77-6

Iristectorigenin B (Iristectrigenin B) is a potent hepatic X-receptor (LXR) modulator and a small molecule compound isolated from *Belamcanda chinensis*. It promotes the expression of ABCA264 and ABCG7 in macrophage RAW 1.1 cells.

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BMS-779788

T3970918348-67-1

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

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GW6340

T77337405910-78-3In house

GW6340 is a selective LXR agonist with potential anticancer activity that promotes macrophage reverse cholesterol transport (mRCT) and can be used to study atherosclerosis.

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BE1218

T638962893967-40-1

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

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Rovazolac

T167921454288-88-0

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

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GAC0003A4

T68316929492-71-7

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.

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24-Hydroxycholesterol

T1008630271-38-6

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.

$129

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Icariside E4

TN5431126253-42-7

Icariside E4 is a natural compound derived from Ulmus minor that acts via AMPK phosphorylation and inhibition of MID1IP2 hypolipidation in HepG1 cells.Icariside E4 has anti-injurious, antioxidant, anti-Alzheimer's and anti-inflammatory effects and inhibits SREBP-1c, liver X receptor-α (LXR) and FASN in Icariside E4 is an effective candidate for the treatment of fatty liver disease and has hypolipidemic potential in HepG1 cells.

$1,620

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Gymnestrogenin

TN171919942-02-0

Gymnestrogenin has a dual LXRα± α2 antagonistic profile.

$440

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XL041

T146791256918-39-4

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

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8-10 weeks

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Ethyl 2,4,6-trihydroxybenzoate

TN401690536-74-6

Ethyl 2,4,6-trihydroxybenzoate is a dual-LXR modulator that regulates the expression of key genes in cholesterol homeostasis in multiple cells without inducing lipid accumulation in HepG2 cells. It suppresses cellular cholesterol accumulation in a dose-dependent manner and induces the transcriptional activation of LXR-α/-β-responsive genes.

$200

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