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

FXR Inhibitor

FXR Inhibitors (24):

Cat. No. Product Name Effect Purity
  • HY-N1423
    Glycocholic acid
    		Inhibitor 99.90%
    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).
  • HY-114392
    Gly-β-MCA
    		Inhibitor 99.95%
    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.
  • HY-121238
    Hyocholic acid
    		Inhibitor 99.46%
    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 .
  • HY-N1423A
    Glycocholic acid sodium
    		Inhibitor
    Glycocholic acid sodium 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 sodium inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid sodium modulates related bile acid receptor signaling. Glycocholic acid sodium suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid sodium can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
  • HY-N1423S
    Glycocholic acid-d4
    		Inhibitor 99.92%
    Glycocholic acid-d4 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).
  • HY-N1423R
    Glycocholic acid (Standard)
    		Inhibitor
    Glycocholic acid (Standard) is the analytical standard of Glycocholic acid (HY-N1423). This product is intended for research and analytical applications. Glycocholic acid is a bile acid with anticancer activity, targeting against pump resistance-related and non-pump resistance-related pathways.
  • HY-106539
    Colesevelam hydrochloride
    		Inhibitor 98.00%
    Colesevelam hydrochloride is an orally active bile acid sequestrant, lipid-lowering agent, and glycemic control agent. Colesevelam hydrochloride binds bile acids in the gastrointestinal tract to form nonabsorbable complexes, interrupts enterohepatic recirculation and increases fecal bile acid elimination. Colesevelam hydrochloride modulates FXR, TGR5, and Cyp7a1 activity and triggers cAMP signaling and GLP-1 release. Colesevelam hydrochloride alters hepatic lipid and glucose metabolism, suppresses hepatic glycogenolysis, reduces hepatic triglyceride and cholesterol levels, and increases LDL-C (low-density lipoprotein cholesterol) clearance. Colesevelam hydrochloride can be used for the research of type 2 diabetes mellitus, hypercholesterolemia, and alcohol-related liver disease.
  • HY-163436
    F44-A13
    		Inhibitor
    F44-A13 is an orally active and highly selective farnesoid X receptor (FXR) antagonist with an IC50 value of 1.1 μM. F44-A13 can optimize cholesterol metabolism and reduce its activity by inducing CYP7A1 expression. F44-A13 reduces levels of cholesterol, triglycerides, and low-density lipoprotein cholesterol (LDL-C) in mouse models. F44-A13 can be used in the study of metabolic diseases associated with lipid disorders.
  • HY-W013105
    Sodium glycocholate hydrate, 98%
    		Inhibitor 99.91%
    Sodium glycocholate hydrate, 98% is a bile acid derivative. Sodium glycocholate hydrate, 98% downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Sodium glycocholate hydrate, 98% inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Sodium glycocholate hydrate, 98% modulates related bile acid receptor signaling. Sodium glycocholate hydrate, 98% suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Sodium glycocholate hydrate, 98% can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
  • HY-13995B
    Sevelamer carbonate
    		Inhibitor
    Sevelamer carbonate is an orally active polymeric phosphate binder and bile acid sequestrant. Sevelamer carbonate binds dietary phosphate in the gastrointestinal tract, reducing phosphate absorption and serum phosphorus levels, and reduces urinary phosphate excretion. Sevelamer carbonate binds polyanion bile acids, increases bile acid faecal excretion, and reduces total cholesterol and LDL cholesterol levels. Sevelamer carbonate can be used for the research of hyperphosphataemia, hyperparathyroidism, chronic renal failure, kidney disease, and type 2 diabetes.
  • HY-13995A
    Sevelamer hydrochloride
    		Inhibitor 98.0%
    Sevelamer hydrochloride is an orally active polymeric phosphate binder and bile acid sequestrant. Sevelamer hydrochloride binds dietary phosphate in the gastrointestinal tract, reducing phosphate absorption and serum phosphorus levels, and reduces urinary phosphate excretion. Sevelamer hydrochloride binds polyanion bile acids, increases bile acid faecal excretion, and reduces total cholesterol and LDL cholesterol levels. Sevelamer hydrochloride can be used for the research of hyperphosphataemia, hyperparathyroidism, chronic renal failure, kidney disease, and type 2 diabetes.
  • HY-N1423B
    Glycocholic acid hydrate
    		Inhibitor
    Glycocholic acid hydrate is a bile acid derivative. Glycocholic acid hydrate downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid hydrate inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid hydrate modulates related bile acid receptor signaling. Glycocholic acid hydrate suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid hydrate can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).
  • 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).
  • 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).
  • 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.
  • 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.
  • 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).
  • 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].
  • HY-121238S1
    Hyocholic acid-d5
    		Inhibitor
    Hyocholic Acid-d5 is the deuterium labeled Hyocholic Acid.
  • 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].