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

FXR

FXR; NR1H4

FXR

Related Products

PDF 0.6 MB

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-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-W754548
    Glycocholic acid-13C2,d4N
    		Inhibitor
    Glycocholic acid-13C2,d4 is the deuterium labeled and 13C-labeled Glycocholic acid (HY-N1423). Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
    Glycocholic acid-<sup>13</sup>C<sub>2</sub>,d<sub>4</sub>N
  • HY-121238R
    Hyocholic Acid (Standard)
    		Inhibitor
    Hyocholic Acid (Standard) is the analytical standard of Hyocholic Acid. This product is intended for research and analytical applications. Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes [1][2][3].
    Hyocholic Acid (Standard)
  • HY-183692
    FXR agonist 18
    		Agonist
    FXR agonist 18 is an orally active FXR agonist, with an EC50 of 10 nM against human FXR and an EC50 of 1360 nM against human TGR5. FXR agonist 18 inhibits inflammatory responses by reducing nitrite production, downregulating the expression of pro-inflammatory genes (Tnf, Adgre1, Cyp8b1, upregulating the expression of FXR, Hmox1, Nqo1, Nrf2, and enhancing antioxidant responses. FXR agonist 18 ameliorates liver fibrosis in mice, exhibits protective effects in mice with cholestatic liver injury, and shows anti-MASH efficacy. FXR agonist 18 can be used in studies of metabolic dysfunction-associated steatohepatitis.
    FXR agonist 18
  • HY-168713
    LZ-007
    		Agonist
    LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
    LZ-007
  • HY-149971
    XJ02862-S2
    		Agonist
    XJ02862-S2 shows potent FXR agonistic activity. XJ02862-S2 is a promising lead compound for the research of NAFLD.
    XJ02862-S2
  • HY-N15305
    Ferolin
    		Agonist
    Ferolin is the agonist for farnesoid X receptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation.
    Ferolin
  • HY-P1624A
    Teduglutide TFA
    		Activator
    Teduglutide TFA is a dipeptidyl peptidase IV resistant glucagon-like peptide 2 (GLP-2) analogue. Teduglutide TFA can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide TFA can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
    Teduglutide TFA
  • HY-121238S1
    Hyocholic acid-d5
    		Inhibitor
    Hyocholic Acid-d5 is the deuterium labeled Hyocholic Acid.
    Hyocholic acid-d<sub>5</sub>
  • HY-114392R
    Gly-β-MCA (Standard)
    		Inhibitor
    Gly-β-MCA (Standard) is the analytical standard of Gly-β-MCA. This product is intended for research and analytical applications. 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[1].
    Gly-β-MCA (Standard)
  • HY-148874
    FXR antagonist 2
    		Antagonist
    FXR antagonist 2 (compound A-26) is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 can be used in the study of hyperlipidemia and type 2 diabetes.
    FXR antagonist 2
  • HY-178959
    FXR agonist 13
    		Agonist
    FXR agonist 13 is a selective, orally active, potent FXR agonist (EC50 = 0.097 μM) and has favorable hepatic microsomal metabolic stability. FXR agonist 13 exhibits moderate affinity for FXR-LBD upon direct binding (KD = 14.74 μM). FXR agonist 13 displays good selectivity against related nuclear receptors, including LXRα/β, PPARα/γ/δ, PXR, and TGR5. FXR agonist 13 can be used for the study of metabolic-associated steatohepatitis (MASH).
    FXR agonist 13
  • HY-13771S1
    Ursodeoxycholic acid-13C
    		Antagonist
    Ursodeoxycholic acid-13C is the 13C labeled Ursodeoxycholic acid. Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
    Ursodeoxycholic acid-<sup>13</sup>C
  • HY-111049
    GSK8062
    GSK8062 is a farnesoid X receptor (FXR) agonist with activity that improves compound development parameters. Analog 1c of GSK8062 showed a reduction in weight gain and serum glucose levels.
    GSK8062
  • HY-N1749
    2-Oxokolavenol
    		Agonist
    2-Oxokolavenol is a selective agonist targeting the farnesoid X receptor (FXR), with an EC50 of ~3.7 μM. 2-Oxokolavenol exerts its activity against Acetaminophen (HY-66005)-induced hepatocyte damage in an FXR-dependent manner by binding to the FXR ligand-binding pocket, recruiting co-activators, and inducing FXR transcriptional activity. 2-Oxokolavenol can be naturally extracted from Aglaia spectabilis (a plant of the Aglaia genus in the Meliaceae family) and can be used in research related to liver diseases.
    2-Oxokolavenol
  • HY-109083A
    Cilofexor tromethamine
    		Agonist
    Cilofexor tromethamine (GS-9674 tromethamine) is a nonsteroidal farnesene oxide receptor agonist with activity in improving markers of cholestasis and liver injury. Cilofexor tromethamine was shown to be well tolerated in patients without cirrhosis and resulted in significant improvements in liver biochemical parameters and cholestatic markers. Cilofexor tromethamine offers a potential inhibitory option for the management of primary sclerosing cholangitis.
    Cilofexor tromethamine
  • HY-180221
    FXR agonist 14
    		Agonist
    FXR agonist 14 (Compound V15) is a partial, selective, orally active FXR agonist with an EC50 of 0.67 nM. FXR agonist 14 ameliorates pathological features in high-fat and high-sugar diet-induced MASH mice. FXR agonist 14 shows significant anti-cholestatic liver disease effects.
    FXR agonist 14
  • HY-N3891
    Fargesone A
    		Agonist
    Fargesone A is a potent and selective FXR agonist. Fargesone A shows anti-inflammatory activity.
    Fargesone A
  • HY-N7781R
    (-)-(E)-Guggulsterone (Standard)
    		Antagonist
    (-)-(E) -guggulsterone (Standard) is the analytical standard for (-)-(E) -guggulsterone ((E)-Guggulsterone) (HY-N7781). (-)-(E)-Guggulsterone is an orally active natural stereoisomer of Guggulsterone (HY-107738). (-)-(E)-Guggulsterone is an antagonist for the Farnesoid X Receptor (FXR) with an IC50 of 24.06 μM and possesses potent hypolipidemic properties. (-)-(E)-Guggulsterone suppresses dengue virus (DENV) replication by upregulating antiviral interferon responses by inducing HO-1 expression via Nrf2 activation. (-)-(E)-Guggulsterone exhibits antibacterial activities against Bacillus subtilis, Staphylococcus aureus and Pseudomonas aeruginosa. (-)-(E)-Guggulsterone has cardiac protective and antioxidant activities in rats.
    (-)-(E)-Guggulsterone (Standard)
Cat. No. Product Name / Synonyms Application Reactivity