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-153525
    FXR agonist 5
    		Agonist 99.83%
    FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation.
    FXR agonist 5
  • HY-13771R
    Ursodeoxycholic acid (Standard)
    		Antagonist
    Ursodeoxycholic acid (Standard) is the analytical standard of Ursodeoxycholic acid. This product is intended for research and analytical applications. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.
    Ursodeoxycholic acid (Standard)
  • HY-B0172R
    Lithocholic acid (Standard)
    		Antagonist
    Lithocholic acid (Standard) is the analytical standard of Lithocholic acid. This product is intended for research and analytical applications. Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.
    Lithocholic acid (Standard)
  • HY-W585876
    Chenodeoxycholic acid 3-glucuronide
    		Activator ≥99.0%
    Chenodeoxycholic acid 3-glucuronide is a metabolite of Chenodeoxycholic acid that can activate the key nuclear receptor (FXR), with an EC50 of 8 μM, and in HEK293T cells, the EC50 for activating FXR is 11 μM.
    Chenodeoxycholic acid 3-glucuronide
  • HY-153114
    HEC96719
    		Agonist 98.01%
    HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis.
    HEC96719
  • HY-76847R
    Chenodeoxycholic Acid (Standard)
    		Activator
    Chenodeoxycholic Acid (Standard) is the analytical standard of Chenodeoxycholic Acid. This product is intended for research and analytical applications. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid (Standard)
  • HY-12222S1
    Obeticholic Acid-d4
    		Agonist 99.84%
    Obeticholic Acid-d4 is the deuterium labeled Obeticholic acid. Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
    Obeticholic Acid-d<sub>4</sub>
  • HY-135399
    Tauro-obeticholic acid
    		Agonist 98.2%
    Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
    Tauro-obeticholic acid
  • HY-135400
    Glyco-Obeticholic acid
    		Agonist ≥98.0%
    Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.
    Glyco-Obeticholic acid
  • HY-W585920
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide
    		Control
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide is a metabolite of Chenodeoxycholic Acid (HY-76847).
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide
  • HY-N9933
    Tauro-β-muricholic acid
    		Antagonist 99.83%
    Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential.
    Tauro-β-muricholic acid
  • HY-101273
    BAR502
    		Agonist 99.53%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
    BAR502
  • HY-103704
    LY2562175
    		Agonist 99.49%
    LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.
    LY2562175
  • HY-76847S2
    Chenodeoxycholic acid-13C
    		Activator ≥98.0%
    Chenodeoxycholic acid-13C is the 13C-labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-<sup>13</sup>C
  • HY-100443B
    (R,R)-PX20606
    		Agonist
    (R,R)-PX20606 is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
    (R,R)-PX20606
  • HY-151481A
    β-FXR antagonist 1
    		Antagonist 99.80%
    β-FXR antagonist 1 (C 12), an isomer of FXR antagonist 1 (HY-151481) is a FXR antagonist.
    β-FXR antagonist 1
  • HY-13995
    Sevelamer
    		Inhibitor
    Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
    Sevelamer
  • HY-14908A
    Vidofludimus hemicalcium
    		Modulator
    Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.
    Vidofludimus hemicalcium
  • HY-100443
    PX20606
    		Agonist
    PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy.
    PX20606
  • HY-139562
    BMS-986318
    		Agonist
    BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis.
    BMS-986318
Cat. No. Product Name / Synonyms Application Reactivity