FXR

FXR; NR1H4

FXR

Related Products

Farnesoid X receptor (FXR) is a ligand-activated transcription factor belonging to the nuclear receptor superfamily. FXR regulates the expression of various genes by binding to DNA either as a monomer or a heterodimer with the common partner for NRs, retinoid x receptor (RXR), to FXR response elements. Two known FXR genes exist, the FXRα and FXRβ.

FXR is mainly expressed in liver and small intestine, where it plays an important role in bile acid, lipid, and glucose metabolism. FXR affects several metabolic pathways through its specific target genes, regulating bile acid (BA) synthesis and homeostasis, glucose and lipid metabolism, also exhibiting a crucial role in intestinal bacterial growth and liver regeneration.

FXR Related Products (177)
Antibodies (2)

By Effects:	Inhibitors (24) Agonists (77) Control (1) Ligand (1) Antagonists (32) Activators (24) Modulators (6)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-15371

Forskolin	Activator	99.92%
Forskolin (Coleonol) is a potent adenylate cyclase activator with an IC₅₀ of 41 nM and an EC₅₀ of 0.5 μM for type I adenylyl cyclase. Forskolin is also an inducer of intracellular cAMP formation. Forskolin induces differentiation of various cell types and activates pregnane X receptor (PXR) and FXR. Forskolin exerts a inotropic effect on the heart, and has platelet antiaggregatory and antihypertensive actions. Forskolin also induces autophagy.

HY-B0172

Lithocholic acid	Antagonist	99.96%
Lithocholic acid is a toxic secondary bile acid that can promote intrahepatic cholestasis and promote tumorigenesis. Lithocholic acid is also a FXR antagonist and a PXR/SXR agonist.

HY-76847

Chenodeoxycholic Acid	Activator	99.93%
Chenodeoxycholic Acid is a hydrophobic primary bile acid that activates nuclear receptors (FXR) involved in cholesterol metabolism.

HY-13771

Ursodeoxycholic acid	Antagonist	99.94%
Ursodeoxycholic acid (Ursodeoxycholate) is a secondary bile acid issued from the transformation of (cheno)deoxycholic acid by intestinal bacteria, acting as a key regulator of the intestinal barrier integrity and essential for lipid metabolism. Ursodeoxycholic acid acts as signaling molecule, exerting its effects by interacting with bile acid activated receptors, including G-protein coupled bile acid receptor 5 (TGR5, GPCR19) and the farnesoid X receptor (FXR). Ursodeoxycholic acid can be used for the research of a variety of hepatic and gastrointestinal diseases. Ursodeoxycholic acid also reduces ACE2 expression and is beneficial for reducing SARS-CoV-2 infection. Orally active.

HY-12222

Obeticholic acid	Agonist	98.0%
Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC₅₀ of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.

HY-W587537

Deoxycholic acid 3-O-β-D-glucuronide disodium		99.59%
Deoxycholic Acid 3-O-beta-D-Glucuronide disodium salt is a bile acid receptor (FXR) agonist.

HY-W104814

sEH/FXR-IN-1	Ligand	≥98.0%
sEH/FXR-IN-1 (compound 9) is a soluble epoxide hydrolase (sEH) and FXR ligand.

HY-181876

F44-S101	Antagonist
F44-S101 is an orally active, potent, and selective gut-restricted FXR antagonist with an IC₅₀ of 0.48 μM and lipid-lowering activity. F44-S101 selectively antagonizes intestinal FXR, feedback-activates hepatic FXR, promotes cholesterol metabolism and reduces lipid accumulation. F44-S101 decreases total cholesterol, triglyceride and low-density lipoprotein cholesterol levels. F44-S101 can be used in studies related to hyperlipidemia.

HY-10626

T0901317	Agonist	99.85%
T0901317 is an orally active and highly selective LXR agonist with an EC₅₀ of 20 nM for LXRα. T0901317 activates FXR with an EC₅₀ of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with K_i values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.

HY-50108

GW 4064	Agonist	99.79%
GW 4064 is a potent FXR agonist with an EC₅₀ of 65 nM.

HY-N1423

Glycocholic acid	Inhibitor	99.90%
Glycocholic acid is a bile acid derivative. Glycocholic acid downregulates MDR1, Bcl-2, MRP1, MRP2 and FXR, upregulates Bax, p53, caspase-9, caspase-3, TGR5 and S1PR2. Glycocholic acid inhibits multidrug resistance and efflux pumps, induces mitochondrial apoptosis, and enhances chemosensitivity. Glycocholic acid modulates related bile acid receptor signaling. Glycocholic acid suppresses growth and conjugation of Enterobacteriaceae and increases their antibiotic susceptibility. Glycocholic acid can be used for the research of colon adenocarcinoma and cholangiocarcinoma (CCA).

HY-107738

Guggulsterone	Antagonist	99.83%
Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt. Guggulsterone, a farnesoid X receptor (FXR) antagonist, with IC₅₀s of 24.06 μM and 39.05 μM for (-)-(E)-Guggulsterone (HY-N7781) and (Z)-Guggulsterone (HY-110066), respectively.

HY-109083

Cilofexor	Agonist	99.82%
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC₅₀ of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.

HY-114392

Gly-β-MCA	Inhibitor	99.95%
Gly-β-MCA, a bile acid, is a potent, sable, intestine-selective and oral bioactive farnesoid X receptor (FXR) inhibitor that may be a candidate for the treatment of metabolic disorders.

HY-110267

DY268	Antagonist	99.48%
DY268 is a farnesoid X receptor (FXR) antagonist (IC₅₀=7.5 nM). It inhibits FXR transactivation in a cell-based assay with an IC₅₀ value of 468 nM. DY268 can be used in the study of drug-induced liver injury (DILI).

HY-P1624

Teduglutide	Activator	99.85%
Teduglutide (ALX-0600) is an analog of human glucagon like peptide-2 (GLP-2). Teduglutide can activate the expression of nuclear receptor subfamily 4 group a member 1 (NR4a1)/nur77 and intestinal FXR signaling in human hepatic stellate cells, thereby improving liver inflammation and fibrosis in mice with sclerosing cholangitis. Teduglutide can alleviate intestinal dysfunction in mice, improve lung injury, alleviate obesity related neuroinflammation and cell apoptosis.

HY-135103

Tauro-β-muricholic acid sodium	Antagonist	99.54%
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC₅₀ of 40 μM.

HY-10912

Fexaramine	Agonist	99.20%
Fexaramine is a potent and selective FXR agonist with an EC₅₀ of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.

HY-121238

Hyocholic acid	Inhibitor	99.46%
Hyocholic Acid is a bile acid found in pig. Hyocholic Acid can also be found in urine samples from patients with cholestasis. Hyocholic Acid promotes GLP-1 secretion via activating TGR5 and inhibiting FXR in enteroendocrine cells. Hyocholic Acid is known for its exceptional resistance to type 2 diabetes .

HY-107859

Tris(2-chloroethyl) phosphate
Tris(2-chloroethyl) phosphate (TCEP) is a widely used organic phosphorus flame retardant, mainly used as a plasticizer. Tris(2-chloroethyl) phosphate has orally active hepatotoxicity, inducing an increase in reactive oxygen species (ROS) and calcium ions (Ca²⁺) influx, a decrease in mitochondrial membrane potential (△Ψm), and causing DNA damage and cell apoptosis. Tris(2-chloroethyl) phosphate directly binds to FXR, inducing obesity and the formation of fatty liver in mice. Chloroethyl) phosphate activates the TLR4/NF-κB pathway, triggering liver inflammation.

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FXR

FXR

FXR Related Products (177)

Antibodies (2)

FXR Related Products (177):