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-15371
    Forskolin
    Activator 99.78%
    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
  • HY-12222
    Obeticholic acid
    Agonist ≥98.0%
    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
  • HY-50108
    GW 4064
    Agonist 98.92%
    GW 4064 is a potent FXR agonist with an EC50 of 65 nM.
    GW 4064
  • HY-76847
    Chenodeoxycholic Acid
    Activator ≥98.0%
    Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic Acid
  • HY-10626
    T0901317
    Agonist 99.89%
    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
  • 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-N9933
    Tauro-β-muricholic acid
    Antagonist
    Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential.
    Tauro-β-muricholic acid
  • HY-50108A
    (E)-GW 4064
    Agonist
    (E)-GW 4064 is a FXR agonist.
    (E)-GW 4064
  • HY-B0172
    Lithocholic acid
    Antagonist 99.99%
    Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.
    Lithocholic acid
  • HY-107738
    Guggulsterone
    Antagonist 99.95%
    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, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively.
    Guggulsterone
  • HY-114392
    Gly-β-MCA
    Inhibitor 99.74%
    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.
    Gly-β-MCA
  • HY-110066
    (Z)-Guggulsterone
    Antagonist 99.30%
    (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
  • HY-110267
    DY268
    Antagonist 99.32%
    DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI).
    DY268
  • HY-107418
    Tropifexor
    Agonist 99.35%
    Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM.
    Tropifexor
  • HY-109083
    Cilofexor
    Agonist 99.82%
    Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
    Cilofexor
  • HY-14908
    Vidofludimus
    Modulator 99.11%
    Vidofludimus is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus also can be used for the research of fatty liver by targeting FXR.
    Vidofludimus
  • HY-135103
    Tauro-β-muricholic acid sodium
    Antagonist 98.60%
    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 sodium
  • HY-10912
    Fexaramine
    Agonist 99.24%
    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
  • HY-12434
    INT-767
    Agonist ≥98.0%
    INT-767 is a dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
    INT-767
  • HY-109096
    Nidufexor
    Agonist 99.41%
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
    Nidufexor
Cat. No. Product Name / Synonyms Application Reactivity