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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.
Signaling Pathways | Target | TargetMol
Cat. No. Product name CAS No. Purity Chemical Structure
T63042 NDB 1660153-08-1 98.94%
NDB
NDB is a selective and potent hFXRα antagonist that inhibits GW4064-stimulated FXR/RXR interactions and FXRα target gene expression in primary mouse hepatocytes....
T78910 ZLY28 98%
ZLY28
ZLY28 is a novel, first-in-class compound with specific intestinal restriction and oral activity, serving as a dual modulator of FXR and FABP1. Additionally, it ...
T81030 Tauro-β-muricholic acid 25696-60-0 98%
Tauro-β-muricholic acid
Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, acts as a competitive and reversible FXR antagonist (IC 50 = 40 μM) and exhibits antiapoptotic effe...
TN4628 Nelumol A 77836-86-3 98%
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....
T11426 Gly-β-MCA 66225-78-3 98%
Gly-β-MCA
Gly-β-MCA is an orally bioactive, enteroselective and potent inhibitor of the farnesoid X receptor (FXR), a bile acid, used in the study of obesity and diabetes....
T15818 LY367385 198419-91-9 98%
LY367385
LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM ...
T13093 Tauro-β-muricholic acid sodium 145022-92-0 98%
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).
T2202 Lithocholic acid 434-13-9 99.98%
Lithocholic acid
Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It a...
T2233 GW 4064 278779-30-9 99.94%
GW 4064
GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).
TQ0252 BAR502 1612191-86-2 99.91%
BAR502
BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).
T1789 Obeticholic Acid 459789-99-2 99.88%
Obeticholic Acid
Obeticholic Acid (6-ECDCA) is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
T13092 Tauro-Obeticholic acid 863239-61-6 99.82%
Tauro-Obeticholic acid
Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).
T7886 Nidufexor 1773489-72-7 99.79%
Nidufexor
Nidufexor is an agonist for the farnesoid X receptor (FXR).
T15806 LY2562175 1103500-20-4 99.78%
LY2562175
LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).
T0847 Chenodeoxycholic acid 474-25-9 99.72%
Chenodeoxycholic acid
Chenodeoxycholic acid (CDCA) is a bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorpti...
T31587 DY268 1609564-75-1 99.43%
DY268
DY268 is a compound based on trisubstituted pyrazolamide without any FXR agonist activity and cytotoxicity and can be used as an effective FXR antagonist (IC50 =...
T6690 T0901317 293754-55-9 99.43%
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).
T4379 Tropifexor 1383816-29-2 99.3%
Tropifexor
Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
T2015 Fexaramine 574013-66-4 98.87%
Fexaramine
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity compared to natural compounds.
T2939 Forskolin 66575-29-9 98.83%
Forskolin
Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces auto...
NDB
T63042
NDB is a selective and potent hFXRα antagonist that inhibits GW4064-stimulated FXR/RXR interactions and FXRα target gene expression in primary mouse hepatocytes....
ZLY28
T78910
ZLY28 is a novel, first-in-class compound with specific intestinal restriction and oral activity, serving as a dual modulator of FXR and FABP1. Additionally, it ...
Tauro-β-muricholic acid
T81030
Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, acts as a competitive and reversible FXR antagonist (IC 50 = 40 μM) and exhibits antiapoptotic effe...
Nelumol A
TN4628
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....
Gly-β-MCA
T11426
Gly-β-MCA is an orally bioactive, enteroselective and potent inhibitor of the farnesoid X receptor (FXR), a bile acid, used in the study of obesity and diabetes....
LY367385
T15818
LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM ...
Tauro-β-muricholic acid sodium
T13093
Tauro-β-muricholic Acid sodium is a endogenous metabolite, is a competitive and reversible antagonist of farnesoid X receptor (FXR)(IC50 of 40 μM).
Lithocholic acid
T2202
Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It a...
GW 4064
T2233
GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).
BAR502
TQ0252
BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).
Obeticholic Acid
T1789
Obeticholic Acid (6-ECDCA) is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
Tauro-Obeticholic acid
T13092
Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).
Nidufexor
T7886
Nidufexor is an agonist for the farnesoid X receptor (FXR).
LY2562175
T15806
LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).
Chenodeoxycholic acid
T0847
Chenodeoxycholic acid (CDCA) is a bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorpti...
DY268
T31587
DY268 is a compound based on trisubstituted pyrazolamide without any FXR agonist activity and cytotoxicity and can be used as an effective FXR antagonist (IC50 =...
T0901317
T6690
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).
Tropifexor
T4379
Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
Fexaramine
T2015
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity compared to natural compounds.
Forskolin
T2939
Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces auto...
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