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Metabolism

ATP Citrate Lyase

(11)

Acetyl-CoA Carboxylase

Amino Acids and Derivatives

Angiotensin-converting Enzyme (ACE)

Endogenous Metabolite

Glutathione Peroxidase

(36)

HIF/HIF Prolyl-Hydroxylase

Indoleamine 2,3-Dioxygenase (IDO)

(33)

Isocitrate Dehydrogenase (IDH)

Mitochondrial Metabolism

(85)

N-Acetylglucosaminyltransferase

Procollagen C Proteinase

(1)

Prolyl Endopeptidase (PREP)

Reactive Oxygen Species

Serine/threonin kinase

(47)

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 HomeSignaling PathwaysMetabolismFXR

GW 4064

T2233278779-30-9

GW 4064 is an effective farnesoid X receptor (FXR) agonist (EC50 =65 nM).

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Obeticholic Acid

T1789459789-99-2

Obeticholic Acid (6-ECDCA, INT-747) is a high-affinity, semisynthetic, bile acid-derived FXR agonist with an EC50 of 99 nM and is able to upregulate IκB-α, KLF-2, and KLF-4 expression. Obeticholic Acid (6-ECDCA, INT-747) also shows potential for treating hepatic steatosis, inflammation, and fibrosis while increasing insulin sensitivity.

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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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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).

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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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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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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.

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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.

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LY2562175

T158061103500-20-4

LY2562175 is an effective and selective FXR agonist (EC50: 193 nM).

$106

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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).

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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.

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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.

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Cilofexor

T74361418274-28-8

Cilofexor inhibits binding of a synthetic peptide, Cilofexor is a farnesoid X receptor (FXR) agonist.

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Hyodeoxycholic acid

T296883-49-8

Hyodeoxycholic acid (NSC 60672) has been used in trials studying the treatment of Hypercholesterolemia.

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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.

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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,

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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.

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Androsterone

T526453-41-8

Androsterone, a metabolic product of testosterone, can activate Farnesoid X Receptor (FXR).

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Vonafexor

T84711192171-69-9

Vonafexor (EYP001) is a farnesoid X receptor (FXR, NR1H4) agonist, with anti-HBV effects

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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

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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.

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Nidufexor

T78861773489-72-7

Nidufexor is an agonist for the farnesoid X receptor (FXR).

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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.

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BAR502

TQ02521612191-86-2

BAR502 is a dual GPBAR1 and FXR agonist (IC50s: 0.4 μM and 2 μM).

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INT-767

T116611000403-03-1In house

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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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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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

35 days

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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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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, serves as a competitive and reversible FXR antagonist (IC50 = 40 μM) and demonstrates antiapoptotic effects by preventing bile acid-induced hepatocellular apoptosis and maintaining mitochondrial membrane potential [1][2].

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BAR-2227

T2006622409154-23-8

BAR-2227 (compound 3a) functions as an FXR agonist and a LIFR inhibitor. It is utilized in the study of liver fibrosis and inflammation.

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10-14 weeks

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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

35 days

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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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