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

FXR Antagonist

FXR Antagonists (29):

Cat. No. Product Name Effect Purity
  • HY-B0172
    Lithocholic acid
    		Antagonist 99.96%
    Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.
  • HY-13771
    Ursodeoxycholic acid
    		Antagonist 99.94%
    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. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.
  • HY-107738
    Guggulsterone
    		Antagonist 99.83%
    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, with IC50s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.
  • HY-110267
    DY268
    		Antagonist 99.32%
    DY268 is a farnesoid X receptor (FXR) antagonist (IC50=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC50 value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI).
  • HY-110066
    (Z)-Guggulsterone
    		Antagonist 99.41%
    (Z)-Guggulsterone, a constituent of Indian Ayurvedic medicinal plant Commiphora mukul, inhibits the growth of human prostate cancer cells by causing apoptosis. (Z)-Guggulsterone inhibits angiogenesis by suppressing the VEGF–VEGF-R2–Akt signaling axis. (Z)-Guggulsterone is also a potent FXR antagonist. (Z)-Guggulsterone reduces ACE2 expression and SARS-CoV-2 infection.
  • HY-135103
    Tauro-β-muricholic acid sodium
    		Antagonist 99.54%
    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-13771A
    Ursodeoxycholic acid sodium
    		Antagonist 99.06%
    Ursodeoxycholic acid (Ursodeoxycholate) sodium 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 sodium 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 sodium can be used for the research of a variety of hepatic and gastrointestinal diseases. Orally active.
  • HY-76847A
    Chenodeoxycholic acid sodium
    		Antagonist 98.0%
    Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • HY-N0910
    Notoginsenoside Ft1
    		Antagonist 98.0%
    NotoginsenosideFt1 is a saponin found in Panax notoginseng. Notoginsenoside Ft1 inhibits the PI3K/AKT/mTOR signaling pathway, activates the p38 MAPK and ERK1/2 signaling pathways, and increases the proportion of CD8+ T cells, thereby inducing apoptosis and lysosomal cell death in various cancer cells, and promoting angiogenesis. Notoginsenoside Ft1 causes vasodilation by activating glucocorticoid receptors (GR) and estrogen receptor beta (ERβ) in endothelial cells. Notoginsenoside Ft1 increases intracellular Ca2+ accumulation, reduces cAMP levels by activating a signaling network mediated through P2Y12 receptors, and promotes platelet aggregation, thereby exerting a procoagulant effect. Notoginsenoside Ft1 inhibits ferroptosis (ferroptosis) in renal tubular epithelial cells by activating the TGR5 receptor, thereby demonstrating a renal protective effect. Notoginsenoside Ft1 acts as a TGR5 agonist and an FXR antagonist to combat obesity and insulin resistance.
  • HY-N9933
    Tauro-β-muricholic acid
    		Antagonist 99.83%
    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.
  • HY-B0172R
    Lithocholic acid (Standard)
    		Antagonist
    Lithocholic acid (Standard) is the analytical standard of Lithocholic acid. This product is intended for research and analytical applications. Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.
  • HY-133890A
    Tauro-α-muricholic acid sodium
    		Antagonist 99.0%
    Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal.
  • HY-N7781
    (-)-(E)-Guggulsterone
    		Antagonist 99.27%
    (-)-(E)-Guggulsterone ((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.
  • HY-13771R
    Ursodeoxycholic acid (Standard)
    		Antagonist
    Ursodeoxycholic acid (Standard) is the analytical standard of Ursodeoxycholic acid. This product is intended for research and analytical applications. 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. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.
  • HY-151481
    FXR antagonist 1
    		Antagonist 98.01%
    FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies.
  • HY-138937
    NDB
    		Antagonist 98.94%
    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.
  • HY-163071
    V023-9340
    		Antagonist
    V023-9340 is a potent FXR inhibitor with IC50 of 4.27 μM that can be used in NASH (nonalcoholic steatohepatitis) research.
  • HY-148874A
    FXR antagonist 2 hydrochloride
    		Antagonist 99.96%
    FXR antagonist 2 (compound A-26) hydrochloride is a diarylamide derivative, as well as a moderate FXR antagonist. FXR antagonist 2 hydrochloride can be used in the study of hyperlipidemia and type 2 diabetes.
  • 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.
  • 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.