2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. FXR

FXR

FXR; NR1H4

FXR

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Farnesoid X receptor (FXR) is a ligand-activated transcription factor belonging to the nuclear receptor superfamily. FXR regulates the expression of various genes by binding to DNA either as a monomer or a heterodimer with the common partner for NRs, retinoid x receptor (RXR), to FXR response elements. Two known FXR genes exist, the FXRα and FXRβ.

FXR is mainly expressed in liver and small intestine, where it plays an important role in bile acid, lipid, and glucose metabolism. FXR affects several metabolic pathways through its specific target genes, regulating bile acid (BA) synthesis and homeostasis, glucose and lipid metabolism, also exhibiting a crucial role in intestinal bacterial growth and liver regeneration.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-163466
    FXR agonist 7
    		Inhibitor
    FXR agonist 7 (compound 33) is a potent agonist of FXR, with EC50 of 0.1 nM. FXR agonist 7 shows high intestinal distribution, good anti-inflammatory activity.
    FXR agonist 7
  • HY-168332
    FXR agonist 11
    		Agonist
    FXR agonist 11 (Compound 14) is an FXR agonist with an EC50 of 1.2 μM and a maximum effect of 73.7%. FXR agonist 11 can significantly increase GSH levels in the liver and is used to study drug-induced liver injury diseases.
    FXR agonist 11
  • HY-139418
    PX20350
    		Agonist
    PX20350 is a FXR agonist with EC50s of 83 and 10 nM for mFXR and hFXR, respectively. PX20350 significantly induces NDRG2 mRNA expression. PX20350 potently reduces liver tumor cells (SK-GI-18 cells) growth and metastasis, and has anti-tumorigenic activity in orthotopic xenograft mouse models.
    PX20350
  • HY-W653920
    Tauro 6-ethlchenodeoxycholic acid-d5(sodium）
    		Agonist
    Tauro 6-ethlchenodeoxycholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid (HY-135399). Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
    Tauro 6-ethlchenodeoxycholic acid-d<sub>5</sub>(sodium）
  • HY-182026
    FXR agonist 17
    		Agonist
    FXR agonist 17 is an orally active, steroidal FXR agonist with EC50 values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC50 = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis.
    FXR agonist 17
  • HY-50108A
    (E)-GW 4064
    		Agonist
    (E)-GW 4064 is a FXR agonist.
    (E)-GW 4064
  • HY-122338
    Fexarine
    		Agonist
    Fexarine is a potent, non-steroidal and selective agonist of farnesoid X receptor (EC50: 38 nM). Fexarine can be used for the research of diseases linked to cholesterol, bile acids.
    Fexarine
  • HY-168516
    FXR/CES2 modulator 1
    		Inhibitor
    FXR/CES2 modulator 1 (compound LE-77) is a doul modulator that activates FXR and inhibits CES2. FXR/CES2 modulator 1 effectively mitigates the intestinal toxicity of irinotecan.
    FXR/CES2 modulator 1
  • HY-N11081
    Hexanorcucurbitacin D
    		Agonist
    Hexanorcucurbitacin D, a cucurbitacin, is a weak ecdysteroid receptor agonist. Hexanorcucurbitacin D can be isolated from Trichosanthes cucumeroides roots. Hexanorcucurbitacin D can be used for the research of cardiovascular disease (CVD).
    Hexanorcucurbitacin D
  • HY-W712932
    Chenodeoxycholic Acid-d7
    Chenodeoxycholic Acid-d7 (CDCA-d7) is the deuterium labeled Chenodeoxycholic Acid (HY-76847). Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid-d<sub>7</sub>
  • HY-169192
    BAR-2227
    		Agonist
    BAR-2227 (compound 3a) is a FXR agonist and LIFR inhibitor. BAR-2227 can be used to study liver fibrosis and inflammation.
    BAR-2227
  • HY-N3209
    Nelumol A
    		Agonist
    Nelumol A is a farnesoid X receptor (FXR) agonist.
    Nelumol A
  • HY-175516
    dual FXR/PPARδ agonist-2
    		Agonist
    dual FXR/PPARδ agonist-2 is a FXR/PPARδ dual agonist through hybridation of FXR agonist GW-4064 and PPARδ agonist GW-0742.dual FXR/PPARδ agonist-2 displays potent dual-target activities with a FXR agonistic EC50 of 12.28 nM and 69 % PPARδ activation at 100 nM. dual FXR/PPARδ agonist-2 shows anti-fibrotic effects in pulmonary fibrosis mouse model.
    dual FXR/PPARδ agonist-2
  • HY-W713010
    3-Epideoxycholic acid-d5
    3-Epideoxycholic acid-d5 is the deuterium labeled 3-Epideoxycholic acid (HY-48814). 3-Epideoxycholic acid is the microbial metabolite of Deoxycholic acid (HY-N0593). 3-Epideoxycholic acid targets FXR of dendritic cells, reduces their immunostimulatory properties, promotes the generation of Treg cells, and exhibits anti-inflammatory activity. 3-Epideoxycholic acid promotes the growth of bacteria Bacteroides.
    3-Epideoxycholic acid-d<sub>5</sub>
  • HY-181761
    FXR agonist 16
    		Agonist
    FXR agonist 16 is a FXR agonist with an EC50 of 2.2 μM. FXR agonist 16 activates FXR transcriptional activity, upregulates SHP and BSEP, and downregulates Cyp7a1. FXR agonist 16 exhibits hepatoprotective activity and reduces AST and ALT levels in free fatty acid-induced hepatocellular injury models. FXR agonist 16 can be used for the research of liver injury.
    FXR agonist 16
  • HY-183279
    FXR antagonist 4
    		Antagonist
    FXR antagonist 4 (Compound 4l) is an orally active, selective FXR antagonist with an IC50 of 0.70 μM. FXR antagonist 4 binds to FXR, differentially regulates bile acid and lipid transporter genes, and exerts no effect on gluconeogenesis-related genes. FXR modulator 1 activates the AMPK signaling pathway to inhibit fatty acid synthesis. FXR modulator 1 alleviates hepatic steatosis, ballooning degeneration and fibrosis, and improves dyslipidemia. FXR modulator 1 can be used for research on metabolic dysfunction-associated steatohepatitis.
    FXR antagonist 4
  • HY-135400S
    Glyco-obeticholic acid-d5
    		Agonist
    Glyco-obeticholic acid-d5 is the deuterium labeled Glyco-Obeticholic acid. Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.
    Glyco-obeticholic acid-d<sub>5</sub>
  • HY-179703
    FXR agonist 15
    		Agonist
    FXR agonist 15 is a selective, potent and orally active farnesoid X receptor (FXR) agonist with EC50 of 0.76 μM. FXR agonist 15 exhibits no obvious activation on other nuclear receptors including LXRα/β, PXR, PPARα/β/γ, THR-β, with EC50 values all >10 μM. FXR agonist 15 can alleviate steatosis, lobular inflammation, hepatocyte ballooning and liver fibrosis. FXR agonist 15 can be used for the research of nonalcoholic steatohepatitis (NASH).
    FXR agonist 15
  • HY-121110
    Fexarene
    		Agonist
    Fexarene is a potent and selective nonsteroidal Farnesoid X Receptor (FXR) agonist with an EC50 of 36 nM. Fexarene can be used in studies of cholesterol and bile acid metabolism.
    Fexarene
  • HY-W020788
    Benoxacor
    		Activator 99.39%
    Benoxacor (CGA 154281) is a herbicide safener and xenobiotic metabolism regulator. Benoxacor protects maize from the toxicity of metolachlor mainly by inducing detoxifying enzymes such as Glutathione S-transferase. Benoxacor also activates FXR, PXR and ERRα, and inhibits aromatase (aromatase). However, Benoxacor exhibits potential subacute oral toxicity and a high risk of hepatotoxicity in animal models. Benoxacor induces reactive oxygen species accumulation, interferes with embryonic heart development, and causes increased liver and kidney weights as well as alterations in gut microbiota in mice. Benoxacor can be used in studies related to hepatic steatosis, infertility, breast cancer and developmental toxicity.
    Benoxacor
Cat. No. Product Name / Synonyms Application Reactivity