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-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-121238S1
    Hyocholic acid-d5
    		Inhibitor
    Hyocholic Acid-d5 is the deuterium labeled Hyocholic Acid.
    Hyocholic acid-d<sub>5</sub>
  • 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.
    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-N7781R
    (-)-(E)-Guggulsterone (Standard)
    		Antagonist
    (-)-(E) -guggulsterone (Standard) is the analytical standard for (-)-(E) -guggulsterone ((E)-Guggulsterone) (HY-N7781). (-)-(E)-Guggulsterone is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
    (-)-(E)-Guggulsterone (Standard)
  • 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-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-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
Cat. No. Product Name / Synonyms Application Reactivity