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).

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).