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-134988
    EDP-305
    		Agonist
    EDP-305 is an orally active, potent and selective farnesoid X receptor (FXR) agonist, with EC50 values of 34 nM (chimeric FXR in CHO cells) and 8 nM (full-length FXR in HEK cells). EDP-305 shows a potent and consistent antifibrotic effect. EDP-305 can be used for primary biliary cholangitis (PBC) and non-alcoholic steatohepatitis (NASH) research.
    EDP-305
  • 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-15371R
    Forskolin (Standard)
    		Activator
    Forskolin (Standard) is the analytical standard of Forskolin. This product is intended for research and analytical applications. Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.
    Forskolin (Standard)
  • HY-N3431
    Kaempferol-7-O-rhamnoside
    		Agonist 99.18%
    Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure.
    Kaempferol-7-O-rhamnoside
  • HY-151481
    FXR antagonist 1
    		Antagonist 98.01%
    FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies.
    FXR antagonist 1
  • HY-138937
    NDB
    		Antagonist 98.94%
    NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.
    NDB
  • HY-W585876
    Chenodeoxycholic acid 3-glucuronide
    		Activator 99.9%
    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-149831
    ZLY28
    		Modulator 99.95%
    ZLY28 is the first-in-class intestinal restricted and orally active FXR and FABP1 dual modulator. ZLY28 also is a novel anti-NASH agent. ZLY28 can be used for the research of nonalcoholic steatohepatitis (NASH).
    ZLY28
  • HY-76847S3
    Chenodeoxycholic acid-d5
    		Activator 99.79%
    Chenodeoxycholic acid-d5 is the deuterium labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-d<sub>5</sub>
  • HY-109096
    Nidufexor
    		Agonist 99.67%
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
    Nidufexor
  • HY-135400
    Glyco-Obeticholic acid
    		Agonist 98.80%
    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-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-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-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-12222R
    Obeticholic acid (Standard)
    		Agonist
    Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. 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 (Standard)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity