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Metabolism

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(40)

Glyoxalase

(2)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(33)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(94)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(46)

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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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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GSK2033

T154271221277-90-2

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

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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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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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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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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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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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Licochalcone E

TN1055864232-34-8

Licochalcone E is a potential LXRβ agonist.

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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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(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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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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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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BMS-779788

T3970918348-67-1

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

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AN0128

T26624872044-70-7

AN0128 (CRM-0005) is an anti-inflammatory boron-containing antibacterial agent that inhibits S. aureus, S. epidermidis, P. acnes, B. subtilis, and suppresses pro-inflammatory cytokine production in macrophage cell lines by inhibiting the p38 MAP kinase signaling pathway. It can be used in dermatological research.

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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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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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Gymnemagenin

T574322467-07-8

Gymnemagenin is a potent and selective antagonist for the β isoform of LXR, it has antihyperglycemic activity.

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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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Larsucosterol Ammonium salt

T41015L2655654-16-1

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.

$335

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Gymnestrogenin

TN171919942-02-0

Gymnestrogenin has a dual LXRα± α2 antagonistic profile.

$440

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24(S)-hydroxy Cholesterol

T21562474-73-7

24(S)-hydroxy Cholesterol (24S-OHC) is the terminal product of the cholesterol elimination pathway in neural tissues. It is an LXR agonist and a selective positive allosteric modulator of NMDARs. It can serve as a biomarker for NPD, induce cognitive decline in mice, and is useful for studying neurological diseases.

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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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