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

FXR Antagonist

FXR Antagonists (15):

Cat. No. Product Name Effect Purity
  • 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.
  • HY-B0172
    Lithocholic acid
    		Antagonist 99.99%
    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-107738
    Guggulsterone
    		Antagonist 99.95%
    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-110066
    (Z)-Guggulsterone
    		Antagonist 99.30%
    (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-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-135103
    Tauro-β-muricholic acid sodium
    		Antagonist 98.60%
    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-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-133890A
    Tauro-α-muricholic acid sodium
    		Antagonist
    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-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-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-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].
  • 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.
  • HY-76847A
    Chenodeoxycholic acid sodium
    		Antagonist
    Chenodeoxycholic acid sodium is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.
  • 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-163072
    FXR antagonist 3
    		Antagonist
    FXR antagonist 3 (V02-8) is an intestine-specific farnesoid X receptor (FXR) antagonist, with an IC50 of 0.89 μM.