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Metabolism FXR

FXR

The bile acid receptor (BAR), also known as farnesoid X receptor (FXR) or NR1H4 (nuclear receptor subfamily 1, group H, member 4) is a nuclear receptor that is encoded by the NR1H4 gene in humans.FXR is expressed at high levels in the liver and intestine. Chenodeoxycholic acid and other bile acids are natural ligands for FXR. Similar to other nuclear receptors, when activated, FXR translocates to the cell nucleus, forms a dimer (in this case a heterodimer with RXR) and binds to hormone response elements on DNA, which up- or down-regulates the expression of certain genes.
Cat No. product name
T11426 Gly-β-MCA Gly-β-MCA, a bile acid, is a sable, intestine-selective, and oral bioactive farnesoid X receptor (FXR) inhibitor.
T11428 Glyco-Obeticholic acid Glyco-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an agonist of the farnesoid X receptor (FXR).
T12583L (-)-PX20606 trans isomer (-)-PX20606 trans isomer is an agonist of FXR (EC50s: 18 and 29 nM for FXR in FRET and M1H assay, respectively).
T13092 Tauro-Obeticholic acid Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).
T13093 Tauro-β-muricholic acid sodium Tauro-β-muricholic Acid sodium is a endogenous metabolite, is a competitive and reversible antagonist of farnesoid X receptor (FXR)(IC50 of 40 μM).
T15818 LY367385 LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μ...
T1789 Obeticholic Acid Obeticholic acid is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
T2015 Fexaramine Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity compared to natural compounds.
T2202 Lithocholic acid Lithocholic acid is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubil...
T2233 GW 4064 GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).
T2968 Hyodeoxycholic acid Hyodeoxycholic Acid has been used in trials studying the treatment of Hypercholesterolemia.
T4379 Tropifexor Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
T5264 Androsterone Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
T6053 Turofexorate Isopropyl Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM
T6344 Sevelamer HCl Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
T6690 T0901317 T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).
T7436 Cilofexor Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.
T7886 Nidufexor Nidufexor is an agonist for the farnesoid X receptor (FXR).
T8471 Vonafexor Vonafexor is a farnesoid X receptor (FXR, NR1H4) agonist, with anti-HBV effects
T8895 Altenusin Altenusin is a natural nonsteroidal fungal metabolite, as a novel selective agonist of FXR with an EC50 value of 3.2 ± 0.2 μM.
TN4628 Nelumol A Nelumol A, and nelumal A show a potency comparable to the endogenous ligand, they may as a valuable potential novel lead compound in the search for FXR agonists...
TQ0252 BAR502 BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).
Gly-β-MCA
T11426CAS 66225-78-3
Gly-β-MCA, a bile acid, is a sable, intestine-selective, and oral bioactive farnesoid X receptor (FXR) inhibitor.
Glyco-Obeticholic acid
T11428CAS 863239-60-5
Glyco-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an agonist of the farnesoid X receptor (FXR).
(-)-PX20606 trans isomer
T12583LCAS 1268244-88-7
(-)-PX20606 trans isomer is an agonist of FXR (EC50s: 18 and 29 nM for FXR in FRET and M1H assay, respectively).
Tauro-Obeticholic acid
T13092CAS 863239-61-6
Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).
Tauro-β-muricholic acid sodium
T13093CAS 145022-92-0
Tauro-β-muricholic Acid sodium is a endogenous metabolite, is a competitive and reversible antagonist of farnesoid X receptor (FXR)(IC50 of 40 μM).
LY367385
T15818CAS 198419-91-9
LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μ...
Obeticholic Acid
T1789CAS 459789-99-2
Obeticholic acid is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
Fexaramine
T2015CAS 574013-66-4
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity compared to natural compounds.
Lithocholic acid
T2202CAS 434-13-9
Lithocholic acid is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubil...
GW 4064
T2233CAS 278779-30-9
GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).
Hyodeoxycholic acid
T2968CAS 83-49-8
Hyodeoxycholic Acid has been used in trials studying the treatment of Hypercholesterolemia.
Tropifexor
T4379CAS 1383816-29-2
Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
Androsterone
T5264CAS 53-41-8
Androsterone is a metabolic product of testosterone and can activate Farnesoid X Receptor (FXR).
Turofexorate Isopropyl
T6053CAS 629664-81-9
Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM
Sevelamer HCl
T6344CAS 152751-57-0
Sevelamer HCl is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
T0901317
T6690CAS 293754-55-9
T0901317 is a potent and selective agonist for both LXR and FXR, with EC50 of ~50 nM and 5 μM, respectively; it inhibits nuclear factor/κB (NF/κB).
Cilofexor
T7436CAS 1418274-28-8
Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.
Nidufexor
T7886CAS 1773489-72-7
Nidufexor is an agonist for the farnesoid X receptor (FXR).
Vonafexor
T8471CAS 1192171-69-9
Vonafexor is a farnesoid X receptor (FXR, NR1H4) agonist, with anti-HBV effects
Altenusin
T8895CAS 31186-12-6
Altenusin is a natural nonsteroidal fungal metabolite, as a novel selective agonist of FXR with an EC50 value of 3.2 ± 0.2 μM.
Nelumol A
TN4628CAS 77836-86-3
Nelumol A, and nelumal A show a potency comparable to the endogenous ligand, they may as a valuable potential novel lead compound in the search for FXR agonists...
BAR502
TQ0252CAS 1612191-86-2
BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).