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

FXR

FXR; NR1H4

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-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-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-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-76847A
    Chenodeoxycholic acid sodium
    Antagonist
    Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid 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-160929
    Linafexor
    Agonist
    Linafexor (CS-0159) is an agonist for farnesoid X receptor (FXR).
    Linafexor
  • 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-121153
    Altenusin
    Agonist
    Altenusin shows markedly DPPH radical scavenging activities.
    Altenusin
  • 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[1].
    Glyco-obeticholic acid-d<sub>5</sub>
  • HY-133890
    Tauro-α-muricholic acid
    Activator
    Tauro-alpha-muricholic acid (T-alpha-MCA) is a bile acid that belongs to a class of compounds that are synthesized in the liver and play an important role in the digestive process. Tauro-α-muricholic acid activates Farni X receptors (FXR) which are involved in the regulation of bile acid synthesis, metabolism and transport. Tauro-alpha-muricholic acid can be used in the study of metabolic syndrome and cardiovascular disease.
    Tauro-α-muricholic acid
  • HY-159845
    Lecufexor
    Agonist
    Lecufexor is a farnesoid X receptor (FXR) agonist.
    Lecufexor
  • HY-135399S
    Tauro-obeticholic acid-d5 sodium
    Agonist
    Tauro-obeticholic acid-d5 sodium is deuterium labeled Tauro-obeticholic acid. Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
    Tauro-obeticholic acid-d<sub>5</sub> sodium
  • HY-110066R
    (Z)-Guggulsterone (Standard)
    Antagonist
    (Z)-Guggulsterone (Standard) is the analytical standard of (Z)-Guggulsterone. This product is intended for research and analytical applications. (Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis. (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection.
    (Z)-Guggulsterone (Standard)
  • HY-76847S1
    Chenodeoxycholic Acid-d9
    Activator
    Chenodeoxycholic Acid-d9 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>9</sub>
  • HY-151959
    FXR agonist 4
    Inhibitor
    FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD).
    FXR agonist 4
  • HY-163071
    V023-9340
    Antagonist
    V023-9340 is a potent FXR inhibitor with IC50 of 4.27 μM that can be used in NASH (nonalcoholic steatohepatitis) research.
    V023-9340
Cat. No. Product Name / Synonyms Application Reactivity