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 (24):

Cat. No. Product Name Effect Purity
  • HY-15371
    Forskolin Activator 98.52%
    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.
  • 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.
  • HY-50108
    GW 4064 Agonist 99.76%
    GW 4064 is a potent FXR agonist with an EC50 of 65 nM.
  • HY-10626
    T0901317 Agonist 99.91%
    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 Agonist 99.33%
    Tropifexor (LJN452) is a highly potent agonist of FXR with an EC50 of 0.2 nM.
  • HY-135103
    Tauro-β-muricholic acid sodium Antagonist
    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.
  • HY-125996
    NR1H4 activator 1 Agonist
    NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
  • HY-135399
    Tauro-Obeticholic acid Agonist
    Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
  • 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-109083
    Cilofexor Agonist 99.82%
    Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) treatment.
  • HY-10912
    Fexaramine Agonist 99.24%
    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-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-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-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-N0933
    Androsterone Activator >98.0%
    Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
  • 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-109096
    Nidufexor Agonist 99.83%
    Nidufexor is a farnesoid X receptor (FXR) agonist.
  • 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-101273
    BAR502 Agonist >98.0%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
Isoform Specific Products

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