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-N0805R
    Alisol B 23-acetate (Standard)
    Activator
    Alisol B 23-acetate (Standard) is the analytical standard of Alisol B 23-acetate (HY-N0805). This product is intended for research and analytical applications. Alisol B 23-acetate is an orally active prototerpane-type triterpenoid. Alisol B 23-acetate can be isolated from Alisma orientalis. Alisol B 23-acetate induces Apoptosis, promotes ROS generation, downregulates CDK4/6, MMP-2/9, upregulates cleaved PARP, activates FXR and inhibits Syk. Alisol B 23-acetate has anti-inflammatory and hepatoprotective activities. Alisol B 23-acetate protects the kidney from ischemia-reperfusion injury. Alisol B 23-acetate has anticancer activity against ovarian cancer, colon cancer, lung cancer, and gastric cancer. Alisol B 23-acetate can be used in the study of atherosclerosis and allergic asthma.
    Alisol B 23-acetate (Standard)
  • HY-135103S
    Tauro-β-muricholic acid-d4 sodium
    Antagonist
    Tauro-β-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
    Tauro-β-muricholic acid-d<sub>4</sub> sodium
  • HY-117918
    ST-1892
    Agonist
    ST-1892 (compound 14) is a highly potent FXR agonist (EC50=7.2 nM) that can be used to study diseases or disorders caused by metabolic inflammation.
    ST-1892
  • HY-113567
    GSK2324
    Agonist
    GSK2324 (Compd 1c) is a FXR agonist for diabetes study, with an EC50 of 120 nM. GSK2324 exhibits t1/2 values of 84 min (mouse), 170 min (rat), 110 min (beagle) and 120 min (cyno), respectively.
    GSK2324
  • HY-107738R
    Guggulsterone (Standard)
    Antagonist
    Guggulsterone (Standard) is the analytical standard of Guggulsterone (HY-107738). This product is intended for research and analytical applications. Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
    Guggulsterone (Standard)
  • HY-133969
    5β-Cholane
    Activator
    5β-Cholane is a farnesoid X receptor (FXR) activator. 5β-Cholane can be used for the research of cholesterol and lipid-related diseases.
    5β-Cholane
  • HY-135399A
    Tauro-obeticholic acid sodium
    Agonist
    Tauro-obeticholic acid sodium is an active metabolite of Obeticholic acid (HY-12222). Obeticholic acid is a potent, selective and orally active FXR agonist.
    Tauro-obeticholic acid sodium
  • HY-W756134
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide-d5 sodium
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide-d5 sodium is the deuterium labeled Chenodeoxycholic acid 24-acyl-β-D-glucuronide sodium. Chenodeoxycholic acid 24-acyl-β-D-glucuronide sodium is a metabolite of Chenodeoxycholic Acid (HY-76847).
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide-d<sub>5</sub> sodium
  • HY-76847S4
    Chenodeoxycholic acid-d2
    Activator
    Chenodeoxycholic acid-d2 (CDCA-d2) is 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>2</sub>
  • HY-10626R
    T0901317 (Standard)
    Agonist
    T0901317 (Standard) is the analytical standard of T0901317. This product is intended for research and analytical applications. T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
    T0901317 (Standard)
  • HY-N9933S
    Tauro-β-muricholic acid-d4-1 sodium
    Antagonist
    Tauro-β-muricholic acid-d4-1 (T-βMCA-d4-1) sodium is the deuterium labeled Tauro-β-muricholic acid (HY-N9933).
    Tauro-β-muricholic acid-d<sub>4</sub>-1 sodium
  • HY-121153
    Altenusin
    Agonist
    Altenusin shows markedly DPPH radical scavenging activities.
    Altenusin
  • HY-50911R
    Turofexorate isopropyl (Standard)
    Agonist
    Turofexorate isopropyl (Standard) is the analytical standard of Turofexorate isopropyl. This product is intended for research and analytical applications. Turofexorate isopropyl (FXR-450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
    Turofexorate isopropyl (Standard)
  • HY-168629
    FXR agonist 9
    Inhibitor
    FXR agonist 9 (compound 26) is an oral active and selectivity FXR partial agonist with the EC50 of 0.09 µM (75.13 % maximum efficacy). FXR agonist 9 ameliorates pathological features in HFD and CCl4(HY-Y0298)-induced metabolic dysfunction-associated steatohepatitis mice.
    FXR agonist 9
  • HY-10912R
    Fexaramine (Standard)
    Agonist
    Fexaramine (Standard) is the analytical standard of Fexaramine. This product is intended for research and analytical applications. Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.
    Fexaramine (Standard)
  • HY-163072
    FXR antagonist 3
    Antagonist
    FXR antagonist 3 (V02-8) is an intestine-specific farnesoid X receptor (FXR) antagonist, with an IC50 of 0.89 μM.
    FXR antagonist 3
Cat. No. Product Name / Synonyms Application Reactivity