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-W587451
    Cholic acid 3-O-glucuronide disodium
    		Agonist 98.82%
    Cholic acid 3-O-glucuronide (OCA-3-glucuronide) disodium is a farnesoid X receptor (FXR) agonist with an EC50 value of 91.5 μM. Cholic acid 3-O-glucuronide is promising for research of bile acid metabolism and detoxification.
    Cholic acid 3-O-glucuronide disodium
  • HY-12222R
    Obeticholic acid (Standard)
    		Agonist
    Obeticholic acid (Standard) is the analytical standard of Obeticholic acid. This product is intended for research and analytical applications. 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 (Standard)
  • HY-N1423S1
    Glycocholic acid-d5
    		Inhibitor 99.9%
    Glycocholic acid-d5 is the deuterium 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-d<sub>5</sub>
  • HY-101273
    BAR502
    		Agonist 99.53%
    BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
    BAR502
  • HY-103704
    LY2562175
    		Agonist 99.49%
    LY2562175 is a potent and selective FXR agonist, with an EC50 of 193 nM.
    LY2562175
  • HY-172122
    FXR/HSD17B13 modulator 1
    		Modulator
    FXR/HSD17B13 modulator 1 (compound 6) is a potent modulator of FXR/HSD17B13. FXR/HSD17B13 modulator 1 plays an important roel in metabolic dysfunction-associated steatohepatitis (MASH) research.
    FXR/HSD17B13 modulator 1
  • HY-P1624S1
    Teduglutide-Leu(13C6,15N) sodium
    Teduglutide-Leu(13C6,15N) (ALX-0600-Leu(13C6,15N)) sodium is the 13C- and 15N-labeled Teduglutide (HY-P1624). Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide 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 can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.
    Teduglutide-Leu(<sup>13</sup>C<sub>6</sub>,<sup>15</sup>N) sodium
  • HY-151959
    FXR agonist 4
    		Inhibitor 99.37%
    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-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 an orally active polymeric phosphate binder and bile acid sequestrant. Sevelamer binds dietary phosphate in the gastrointestinal tract, reducing phosphate absorption and serum phosphorus levels, and reduces urinary phosphate excretion. Sevelamer binds polyanion bile acids, increases bile acid faecal excretion, and reduces total cholesterol and LDL cholesterol levels. Sevelamer can be used for the research of hyperphosphataemia, hyperparathyroidism, chronic renal failure, kidney disease, and type 2 diabetes.
    Sevelamer
  • HY-15371G
    Forskolin (GMP)
    		Activator
    Forskolin (Coleonol) (GMP) is a potent adenylate cyclase activator with an IC50 of 41 nM and an EC50 of 0.5 μM for type I adenylyl cyclase. Forskolin (GMP) is also an inducer of intracellular cAMP formation. Forskolin (GMP) induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin (GMP) exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin (GMP) also induces autophagy.
    Forskolin (GMP)
  • 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-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-N17383
    Ligusticum cycloprolactam
    		Inhibitor
    Ligusticum cycloprolactam is a potent, orally active, and CNS-penetrant TLR4/NF-κB inhibitor, exhibiting anti-inflammatory and neuroprotective activity. Ligusticum cycloprolactam reduces FPR1 expression, inhibits NLRP3 inflammasome, TLR4/NF-κB, hepatic MAPK and TGF-β signaling, and selectively activates hepatic FXR. Ligusticum cycloprolactam attenuates pro-inflammatory mediator production, enhances anti-inflammatory cytokine secretion, regulates renal uric acid transporters, and preserves intestinal microbiota composition. Ligusticum cycloprolactam can be used for the research of ischemic stroke, hyperuricemic nephropathy, neuroinflammation, and metabolic dysfunction-associated fatty liver disease.
    Ligusticum cycloprolactam
Cat. No. Product Name / Synonyms Application Reactivity