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-121238R
    Hyocholic Acid (Standard)
    		Inhibitor
    Hyocholic Acid (Standard) is the analytical standard of Hyocholic Acid. This product is intended for research and analytical applications. Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes [1][2][3].
    Hyocholic Acid (Standard)
  • 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-142159
    FXR/TGR5 agonist 1
    		Agonist
    FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the research of fatty liver disease.
    FXR/TGR5 agonist 1
  • HY-168713
    LZ-007
    		Agonist
    LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
    LZ-007
  • 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-149971
    XJ02862-S2
    		Agonist
    XJ02862-S2 shows potent FXR agonistic activity. XJ02862-S2 is a promising lead compound for the research of NAFLD.
    XJ02862-S2
  • 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-N15305
    Ferolin
    		Agonist
    Ferolin is the agonist for farnesoid X receptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation.
    Ferolin
  • HY-P1624A
    Teduglutide TFA
    		Activator
    Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
    Teduglutide TFA
  • HY-114392R
    Gly-β-MCA (Standard)
    		Inhibitor
    Gly-β-MCA (Standard) is the analytical standard of Gly-β-MCA. This product is intended for research and analytical applications. Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders[1].
    Gly-β-MCA (Standard)
  • HY-168331
    FXR agonist 10
    		Agonist
    FXR agonist 10 (Compound 27) is an agonist for FXR with an EC50 of 14.26 μM. FXR agonist 10 upregulates the expression of SHP and BSEP proteins, downregulates the expression of NTCP and CYP7A1 proteins. FXR agonist 10 ameliorates the ANIT-induced cholestasis in mouse model.
    FXR agonist 10
  • HY-148874
    FXR antagonist 2
    		Antagonist
    FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes.
    FXR antagonist 2
  • HY-13771S1
    Ursodeoxycholic acid-13C
    		Antagonist
    Ursodeoxycholic acid-13C is the 13C labeled Ursodeoxycholic acid. 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. Orally active[1][2].
    Ursodeoxycholic acid-<sup>13</sup>C
  • HY-111049
    GSK8062
    GSK8062 is a farnesoid X receptor (FXR) agonist with activity that improves compound development parameters. Analog 1c of GSK8062 showed a reduction in weight gain and serum glucose levels.
    GSK8062
  • HY-109083A
    Cilofexor tromethamine
    		Agonist
    Cilofexor tromethamine (GS-9674 tromethamine) is a nonsteroidal farnesene oxide receptor agonist with activity in improving markers of cholestasis and liver injury. Cilofexor tromethamine was shown to be well tolerated in patients without cirrhosis and resulted in significant improvements in liver biochemical parameters and cholestatic markers. Cilofexor tromethamine offers a potential inhibitory option for the management of primary sclerosing cholangitis.
    Cilofexor tromethamine
  • HY-N3891
    Fargesone A
    		Agonist
    Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity.
    Fargesone A
  • HY-169792
    HPG1860
    		Agonist
    HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC50 values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH).
    HPG1860
  • 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-50108A
    (E)-GW 4064
    		Agonist
    (E)-GW 4064 is a FXR agonist.
    (E)-GW 4064
Cat. No. Product Name / Synonyms Application Reactivity