2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. FXR

FXR

FXR; NR1H4

FXR

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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-135399
    Tauro-obeticholic acid
    		Agonist ≥98.0%
    Tauro-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
    Tauro-obeticholic acid
  • HY-135400
    Glyco-Obeticholic acid
    		Agonist ≥98.0%
    Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.
    Glyco-Obeticholic acid
  • 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-101273
    BAR502
    		Agonist 99.53%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
    BAR502
  • HY-103704
    LY2562175
    		Agonist 99.49%
    LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.
    LY2562175
  • HY-76847S2
    Chenodeoxycholic acid-13C
    		Activator ≥98.0%
    Chenodeoxycholic acid-13C is the 13C-labeled Chenodeoxycholic Acid. Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
    Chenodeoxycholic acid-<sup>13</sup>C
  • HY-100443B
    (R,R)-PX20606
    		Agonist
    (R,R)-PX20606 is a FXR agonist with EC50s of 18 and 29 nM for FXR in FRET and M1H assay, respectively.
    (R,R)-PX20606
  • HY-151481A
    β-FXR antagonist 1
    		Antagonist 99.80%
    β-FXR antagonist 1 (C 12), an isomer of FXR antagonist 1 (HY-151481) is a FXR antagonist.
    β-FXR antagonist 1
  • 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.
    Sevelamer
  • HY-14908A
    Vidofludimus hemicalcium
    		Modulator
    Vidofludimus (4sc-101; SC12267) hemicalcium is an orally active inhibitor for dihydroorotate dehydrogenase (DHODH) and also is a novel modulator for farnesoid X receptor (FXR). Vidofludimus hemicalcium, as an immunomodulatory agent, can be used for the research of autoimmune disorders such as inflammatory bowel disease (IBD). Vidofludimus hemicalcium also can be used for the research of fatty liver by targeting FXR.
    Vidofludimus hemicalcium
  • HY-100443
    PX20606
    		Agonist
    PX20606 is an orally active agonist for farnesoid X receptor (FXR), with EC50 220 nM (mFXR) and 50 nM (hFXR), measured by Gal4-FXR assay. PX20606 induces the expression of tumor suppressor gene NDRG2, inhibits the tumor growth and metastasis in mouse HCC model. PX20606 exhibits hepatoprotective efficacy.
    PX20606
  • HY-139562
    BMS-986318
    		Agonist
    BMS-986318 is a potent nonbile acid FXR agonist with EC50s of 53 and 350 nM in the FXR Gal4 and SRC-1 recruitment assays, respectively. BMS-986318 has a suitable ADME profile, and demonstrates efficacy in the mouse bile duct ligation model of liver cholestasis and fibrosis.BMS-986318 can be used for the research of nonalcoholic steatohepatitis.
    BMS-986318
  • HY-150787
    BMS-986339
    		Agonist
    BMS-986339 is an orally active, potent FXR agonist. BMS-986339 forms H-bond with His298 and ASN287 residues. BMS-986339 can be used in the research of primary biliary cirrhosis (PBC), primary sclerosing cholangitis (PSC), and nonalcoholic steatohepatitis (NASH), anti-fibrosis.
    BMS-986339
  • 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.
    NR1H4 activator 1
  • HY-12222S
    Obeticholic acid-d5
    		Agonist
    Obeticholic acid-d5 is the deuterium labeled Obeticholic acid. 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[1][2][3].
    Obeticholic acid-d<sub>5</sub>
  • HY-N4063
    Hedragonic acid
    		Agonist
    Hedragonic acid is an oleane-type triterpenoid compound, which can be isolated from the stems and roots of the southern snake vine. Hedragonic acid is a ligand and agonist for FXR. Hedragonic acid protected mice from liver damage caused by acetaminophen overdose and reduced liver inflammation.
    Hedragonic acid
  • 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-164799
    FXR agonist 12
    		Agonist
    FXR agonist 12 (Compound C7) is the orally active agonist for FXR. FXR agonist 12 down-regulates bile acid synthesis-related genes, and up-regulates bile acid transport-related genes in HepG2 cells. FXR agonist 12 improves ANIT-induced cholestasis, ameliorates the liver damage and fibrosis in mouse NASH models.
    FXR agonist 12
  • HY-N10640
    Alismanol M
    		Agonist
    Alismanol M is a farnesoid X receptor (FXR) agonist with an EC50 value of 50.25 μM. Alismanol M is a protostane-type triterpenoid that can be isolated from the rhizome of Alisma orientale. Alismanol M can be used for the research of cholestasis and nonalcoholic steatohepatitis.
    Alismanol M
  • 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[1][2][3].
    Tauro-β-muricholic acid-d<sub>4</sub> sodium
Cat. No. Product Name / Synonyms Application Reactivity