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-151959
    FXR agonist 4
    		Inhibitor
    FXR agonist 4 (compound 10a) is an agonist of farnesoid X receptor (FXR) with an EC50 value of 1.05 μM. FXR agonist 4 effectively improves hyperlipidemia, hepatic steatosis, insulin resistance and hepatic inflammation in DIO mice. FXR agonist 4 can be used for the research of non-alcoholic fatty liver disease (NAFLD).
    FXR agonist 4
  • 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.
    V023-9340
  • 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-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.
    FXR antagonist 2 hydrochloride
  • 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.
    Obeticholic acid-d<sub>5</sub>
  • HY-172422
    Danifexor
    		Agonist
    Danifexor is the agonist for farnesoid X receptor.
    Danifexor
  • 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-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-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-142159
    FXR/TGR5 agonist 1
    		Agonist
    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
  • 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
Cat. No. Product Name / Synonyms Application Reactivity