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Metabolism

ATP Citrate Lyase

(11)

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(29)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(30)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(76)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(46)

Stearoyl-CoA Desaturase (SCD)

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.

Filter Signaling PathwaysMetabolismFXR

Forskolin
T293966575-29-9
Forskolin (Coleonol) is a natural product, an adenylate cyclase activator (EC50=0.5 μM). Forskolin increases cAMP levels, activates PXR and FXR, and induces autophagy. Forskolin produces positive inotropic effects in the heart, and has platelet anticoagulant and antihypertensive effects.
- $36
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Obeticholic Acid
T1789459789-99-2
Obeticholic Acid (6-ECDCA) is a Farnesoid X Receptor Agonist. The mechanism of action of obeticholic acid is as a Farnesoid X Receptor Agonist.
- $41
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Lithocholic acid
T2202434-13-9
Lithocholic acid (3α-Hydroxy-5β-cholanic acid) is a bile acid formed from chenodeoxycholate by bacterial action, usually conjugated with glycine or taurine. It acts as a detergent to solubilize fats for absorption and is itself absorbed. It is used as cholagogue and choleretic.
- $46
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Androsterone
T526453-41-8
Androsterone, a metabolic product of testosterone, can activate Farnesoid X Receptor (FXR).
- $46
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GSK2324
T274601020567-30-9In house
GSK2324 is a potent FXR agonist for the treatment of NAFLD by controlling hepatic lipids through reduced uptake and selective reduction of fatty acid synthesis.
- $342
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Altenusin
T889531186-12-6In house
Altenusin is a natural nonsteroidal fungal metabolite, as a novel selective agonist of FXR with an EC50 value of 3.2 ± 0.2 μM.
- $389
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Ursodeoxycholic acid sodium
T290782898-95-5In house
Ursodeoxycholic acid sodium (Sodium Ursodeoxycholate) is a naturally occurring secondary bile acid with anti-inflammatory and cytoprotective activities. Ursodeoxycholic acid sodium acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors,
- $118
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T0901317
T6690293754-55-9
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).
- $32
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Fexaramine
T2015574013-66-4
Fexaramine is a small molecule farnesoid X receptor (FXR) agonist with 100-fold increased affinity compared to natural compounds.
- $42
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GW 4064
T2233278779-30-9
GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).
- $46
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Hyodeoxycholic acid
T296883-49-8
Hyodeoxycholic acid (NSC 60672) has been used in trials studying the treatment of Hypercholesterolemia.
- $38
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Turofexorate Isopropyl
T6053629664-81-9
Turofexorate Isopropyl (XL335) is a potent, selective, and orally bioavailable FXR agonist with EC50 of 4 nM
- $39
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Chenodeoxycholic acid
T0847474-25-9
Chenodeoxycholic acid (CDCA) is a bile acid, usually conjugated with either glycine or taurine. It acts as a detergent to solubilize fats for intestinal absorption and is reabsorbed by the small intestine. It is used as cholagogue, a choleretic laxative, and to prevent or dissolve gallstones.
- $55
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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 is a pioneering anti-NASH agent, utilized in the study of nonalcoholic steatohepatitis (NASH) [1].
- $353
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Tauro-β-muricholic acid sodium
T13093145022-92-0
Tauro-β-muricholic Acid sodium is a endogenous metabolite, is a competitive and reversible antagonist of farnesoid X receptor (FXR)(IC50 of 40 μM).
- $180
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Tauro-β-muricholic acid
T8103025696-60-0
Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, acts as a competitive and reversible FXR antagonist (IC 50 = 40 μM) and exhibits antiapoptotic effects by inhibiting bile acid-induced hepatocellular apoptosis and preserving mitochondrial membrane potential [1] [2].
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Sevelamer hydrochloride
T6344152751-57-0
Sevelamer hydrochloride (Sevelamer HCl) is a phosphate binding drug used to treat hyperphosphatemia via binding to dietary phosphate and prevents its absorption.
- $50
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Chenodeoxycholic Acid sodium salt
T650702646-38-0
Chenodeoxycholic Acid sodium salt (CDCA sodium salt) is a bile acid in humans that activates the nuclear receptor FXR, rescues axonal degeneration of induced pluripotent stem cell-derived neurons in patients with spastic paraplegia type 5 and cerebral xanthomatosis, and can be used to study pancreatic necrosis.
- $31
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Osocimab
T771242056878-75-0
Osocimab (BAY 1213790) is a potent anti-FXIa antibody with a Ki value of 2.4 nM and an EC50 value of 0.2 nM.Osocimab may reduce thrombosis through FXI inhibition.Osocimab is often used as an XI factor inhibitor, has an inhibitory effect on thrombin generation, has an anticoagulant effect, and is used in the study of thromboembolic diseases. Thromboembolic Diseases
- $247
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INT-767
T116611000403-03-1
INT-767 is a potent farnesoid X receptor (FXR)/TGR5 dual agonist that prevents NASH and promotes visceral adipose brown lipogenesis and mitochondrial function for the study of non-alcoholic steatohepatitis.
- $399
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Nidufexor
T78861773489-72-7
Nidufexor is an agonist for the farnesoid X receptor (FXR).
- $51
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BAR502
TQ02521612191-86-2
BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).
- $107
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Nelumol A
TN462877836-86-3
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.
- $700
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LY2562175
T158061103500-20-4
LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).
- $163
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Tropifexor
T43791383816-29-2
Tropifexor (LJN452) is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
- $89
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Vonafexor
T84711192171-69-9
Vonafexor (EYP001) is a farnesoid X receptor (FXR, NR1H4) agonist, with anti-HBV effects
- $35
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LY367385
T15818198419-91-9
LY367385 is a highly effective and selective mGluR1a antagonist. LY367385 has neuroprotective, anticonvulsant, and antiepileptic effects. Compared with > 100 μM for mGlu5a, LY367385 has an IC50 of 8.8 μM for inhibits of quisqualate-induced phosphoinositide (PI) hydrolysis.
- $595
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Tauro-Obeticholic acid
T13092863239-61-6
Tauro-Obeticholic acid is an active Obeticholic acid metabolite. Obeticholic acid is an orally bioavailable agonist of farnesoid-X receptor (FXR).
- $119
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Guggulsterone
T557495975-55-6
Guggulsterone (Guggulsterone E&Z) E&Z is a 3-hydroxy steroid. It has a role as an androgen.
- $30
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Gly-β-MCA
T1142666225-78-3
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.
- $199
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Cilofexor
T74361418274-28-8
Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.
- $46
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Glyco-Obeticholic acid
T11428863239-60-5
Glyco-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an agonist of the farnesoid X receptor (FXR).
- $179
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DY268
T315871609564-75-1
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 = 7.5 nM).
- $34
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NDB
T630421660153-08-1
NDB is a selective and potent hFXRα antagonist that inhibits GW4064-stimulated FXR RXR interactions and FXRα target gene expression in primary mouse hepatocytes.NDB is used in the study of diabetes.
- $99
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