1. Metabolic Enzyme/Protease
  2. FXR

FXR

Farnesoid X receptor (FXR) is a nuclear hormone receptor critically involved in the regulation of bile acid homeostasis. It is now recognized that bile acids serve as the natural ligands for FXR. Once activated, FXR in turn induces the expression of another nuclear hormone receptor, small heterodimer partner (SHP).

FXR, which is highly expressed in the liver, intestine, kidney, adrenal glands, and adipose tissue, is a master regulator of the synthesis and pleiotropic actions of endogenous bile acids (BAs).

FXR activation inhibits BA synthesis and has anti-inflammatory effects in atherosclerosis, inflammatory bowel disease, and experimental cholestasis, whereas TGR5 activation, via cAMP-mediated pathways, reduces proinflammatory cytokine production in macrophages and Kupffer cells.

FXR Related Products (15):

Cat. No. Product Name Effect Purity
  • HY-12222
    INT-747 Agonist >98.0%
    INT-747 is a potent and selective FXR agonist (EC50=99 nM) endowed with anticholestatic activity.
  • HY-50108
    GW 4064 Agonist 99.42%
    GW 4064 is a potent FXR agonist with EC50 of 65 nM.
  • HY-10626
    T0901317 Agonist 99.64%
    T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 (mu)M, respectively, inhibits nuclear factor/(kappa)B (NF/(kappa)B).
  • HY-10912
    Fexaramine Agonist 99.47%
    Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity relative to natural compounds.
  • HY-12434
    INT-767 Agonist >98.0%
    INT-767 is a potent agonist for both FXR (mean EC50, 30 nM by PerkinElmer AlphaScreen assay) and TGR5 (mean EC50, 630 nM by time resolved-fluorescence resonance energy transfer).
  • HY-N0933
    Androsterone Activator >98.0%
    Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
  • HY-103704
    LY2562175 Agonist
    LY2562175 is a potent and selective FXR agonist with an EC50 of 193 nM.
  • HY-100443B
    (-)-PX20606 trans isomer Agonist
    (-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
  • HY-50911
    WAY-362450 Agonist 99.41%
    WAY-362450 is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
  • HY-107418
    Tropifexor Activator 99.33%
    Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
  • HY-13995A
    Sevelamer hydrochloride Inhibitor 98.00%
    Sevelamer Hcl is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  • HY-76847
    Chenodeoxycholic Acid Activator >98.0%
    Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-100443A
    PX20606 trans racemate Agonist 99.01%
    PX20606 trans racemate is a FXR agonist with EC50s of 32 and 34 nM for FXR in FRET and M1H assay, respectively.
  • HY-13995
    Sevelamer Inhibitor
    Sevelamer is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  • HY-101273
    BAR502 Agonist >98.0%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.