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. 상품명 효과 Purity Chemical Structure
  • HY-N3431
    Kaempferol-7-O-rhamnoside
    Agonist 99.18%
    Kaempferol-7-O-rhamnoside is a PD-1/PD-L1 inhibitor and farnesoid X receptor (FXR) agonist. Kaempferol-7-O-rhamnoside demonstrates cardioprotective potential targeting the AMPKα1 signaling pathway. Kaempferol-7-O-rhamnoside significantly upregulates the mRNA expression of AMPKα1 in H9c2 cardiomyocytes. Kaempferol-7-O-rhamnoside reverses APAP-induced reduction of glutathione (GSH) content and increase of ROS production in L02 cells. Kaempferol-7-O-rhamnoside has the potential for heart failure.
    Kaempferol-7-O-rhamnoside
  • HY-N0887
    Isoastragaloside I
    Activator 99.49%
    Isoastragaloside I is a natural compound found in Astragalus membranaceus, with oral activity and multiple biological activities such as anti-inflammatory and antioxidant properties. Isoastragaloside I inhibits Akt, NF-κB, MAPKs and PI3K, enhances the activity of hepatic FXR, regulates the TGF-β/Smads signaling pathway, and upregulates antioxidant molecules downstream of Nrf2. Isoastragaloside I inhibits the expression of NO, TNF-α, iNOS, COX-2, IL-1β and VCAM-1, and reduces intracellular ROS levels. Isoastragaloside I attenuates blood-brain barrier disruption, restores intestinal barrier function, increases β-cell mass, improves glucose homeostasis, and elevates circulating adiponectin levels. Isoastragaloside I can be used for the study of neuroinflammation-related neurodegenerative diseases, cholestatic liver disease, and diabetes.
    Isoastragaloside I
  • HY-133890
    Tauro-α-muricholic acid
    Activator 99.18%
    Tauro-α-muricholic acid (T-α-MCA) is a Taurine (HY-B0351)-conjugated primary Bile acid. Tauro-α-muricholic acid is a FXR antagonist with an IC50 of  28 µM. Tauro-α-muricholic acid attenuates other bile acid-activated FXR signaling. Tauro-α-muricholic acid can be used in the research of Alzheimer's disease, glucose metabolism, and lipid metabolism.
    Tauro-α-muricholic acid
  • HY-149831
    ZLY28
    Modulator 99.95%
    ZLY28 is the first-in-class intestinal restricted and orally active FXR and FABP1 dual modulator. ZLY28 also is a novel anti-NASH agent. ZLY28 can be used for the research of nonalcoholic steatohepatitis (NASH).
    ZLY28
  • HY-147296
    Omesdafexor
    Agonist 99.09%
    Omesdafexor (MET409) is an orally active FXR agonist with a unique non-bile acid structure. Omesdafexor can be used for the study of non-alcoholic steatohepatitis (NASH).
    Omesdafexor
  • HY-W585920
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide
    Control
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide is a metabolite of Chenodeoxycholic Acid (HY-76847).
    Chenodeoxycholic acid 24-acyl-β-D-glucuronide
  • HY-107859S
    Tris(2-chloroethyl)phosphate-d12
    99.15%
    Tris(2-chloroethyl)phosphate-d12 is the deuterium labeled Tris(β-chloroethyl) phosphate. Tris(2-chloroethyl) phosphate is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation.
    Tris(2-chloroethyl)phosphate-d<sub>12</sub>
  • HY-109096
    Nidufexor
    Agonist 99.67%
    Nidufexor (LMB763) is an orally-available farnesoid X receptor (FXR) agonist for the research of nonalcoholic steatohepatitis (NASH).
    Nidufexor
  • HY-N1423B
    Glycocholic acid hydrate
    Inhibitor
    Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid hydrate
  • HY-163071
    V023-9340
    Antagonist 99.83%
    V023-9340 is a potent FXR inhibitor with IC50 of 4.27 μM that can be used in NASH (nonalcoholic steatohepatitis) research.
    V023-9340
  • HY-150787
    BMS-986339
    Agonist 99.74%
    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-135400
    Glyco-Obeticholic acid
    Agonist 98.80%
    Glyco-obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is a farnesoid X receptor (FXR) agonist.
    Glyco-Obeticholic acid
  • HY-153525
    FXR agonist 5
    Agonist 99.83%
    FXR agonist 5 (compound 1) is a FXR agonist. FXR agonist 5 can be used for research in diseases or disorders caused by metabolic inflammation.
    FXR agonist 5
  • HY-169792
    HPG1860
    Agonist 99.9%
    HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC50 values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH).
    HPG1860
  • HY-138937
    NDB
    Antagonist 98.36%
    NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.
    NDB
  • 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-153114
    HEC96719
    Agonist 98.01%
    HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis.
    HEC96719
  • HY-12222S1
    Obeticholic acid-d4-1
    Agonist 99.84%
    Obeticholic Acid-d4 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.
    Obeticholic acid-d<sub>4</sub>-1
  • HY-135399
    Tauro-obeticholic acid
    Agonist 98.2%
    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-142159
    FXR/TGR5 agonist 1
    Agonist 98.03%
    FXR/TGR5 agonist 1 has agonist action on FXR and TGR5, and can be used for the research of fatty liver disease.
    FXR/TGR5 agonist 1
Cat. No. 상품명 / Synonyms Application Reactivity