1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. 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 (18):

Cat. No. Product Name Effect Purity
  • HY-12222
    Obeticholic acid Agonist >98.0%
    Obeticholic acid (INT-747) is a potent and selective farnesoid X receptor (FXR) agonist with an EC50 of 99 nM.
  • HY-50108
    GW 4064 Agonist 99.42%
    GW 4064 is a potent FXR agonist with EC50 of 65 nM.
  • HY-10626
    T0901317 Agonist 99.89%
    T0901317 is a potent and selective agonist for LXR and FXR, with EC50s of 50 nM and 5 μM, respectively[1,2]. T0901317 induces its anti-proliferative and cytotoxic effects via an LXR-independent mechanism. T0901317 significantly suppresses cell proliferation and induces programmed cell death in a dose- and time-dependent manner. T0901317 can protect mice from high fat diet-induced obesity and insulin resistance.
  • HY-107418
    Tropifexor Activator 99.33%
    Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
  • 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-107738
    Guggulsterone Antagonist 99.50%
    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.
  • HY-10912
    Fexaramine Agonist 98.78%
    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 dual farnesoid X receptor (FXR)/TGR5 agonist with mean EC50s of 30 and 630 nM, respectively.
  • HY-109083
    Cilofexor Agonist 99.82%
    Cilofexor is a farnesoid X receptor (FXR) agonist.
  • HY-50911
    Turofexorate isopropyl Agonist 99.41%
    Turofexorate isopropyl (WAY-362450) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM.
  • HY-13995A
    Sevelamer hydrochloride Inhibitor >98.0%
    Sevelamer hydrochloride is a phosphate binding drug used to treat hyperphosphatemia in patients with chronic kidney disease; consists of polyallylamine that is crosslinked with epichlorohydrin.
  • HY-N0933
    Androsterone Activator >98.0%
    Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
  • HY-114392
    Gly-β-MCA Inhibitor >98.0%
    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.
  • 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-101273
    BAR502 Agonist >98.0%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
  • HY-100443B
    (-)-PX20606 trans isomer Agonist 98.39%
    (-)-PX20606 trans isomer is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
  • HY-103704
    LY2562175 Agonist 99.87%
    LY2562175 is a potent and selective FXR agonist with an EC50 of 193 nM.
  • 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.
Isoform Specific Products

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.