Date published: 2025-10-3

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FXR Activators

The chemical class of FXR activators pertains to a group of compounds that interact with and modulate the activity of the farnesoid X receptor (FXR), a nuclear receptor found predominantly in the liver and intestine. FXR is a critical regulator of numerous physiological processes, including bile acid metabolism, lipid homeostasis, glucose regulation, and inflammation. FXR activators are characterized by their ability to bind to the ligand-binding domain of FXR, leading to conformational changes that facilitate receptor activation. This activation triggers a cascade of molecular events that influence the transcription of target genes involved in various metabolic pathways. Structurally, FXR activators can vary widely, encompassing diverse chemical moieties. Some FXR activators are steroidal in nature, sharing structural similarities with bile acids, the endogenous ligands of FXR. Others are non-steroidal and exhibit distinct chemical structures. These activators exert their effects by initiating the recruitment of co-activator proteins and the subsequent binding of the activated FXR to specific DNA sequences known as response elements in the promoters of target genes. This leads to the upregulation or downregulation of gene expression, resulting in altered metabolic pathways that contribute to overall homeostasis. FXR activators have gained considerable attention in research due to their potential to modulate key metabolic processes. Understanding the mechanisms by which these compounds activate FXR provides insights into the complex regulatory networks that govern metabolic homeostasis. Ongoing studies continue to elucidate the intricate interactions between FXR and its activators, shedding light on how these molecules could be harnessed to influence metabolic processes.

SEE ALSO...

Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

GW 4064

278779-30-9sc-218577
5 mg
$93.00
13
(1)

GW 4064 (CAS 278779-30-9) is a chemical compound that activates FXR, a nuclear receptor involved in regulating various physiological processes.

Thrombin from human plasma

9002-04-4sc-471713
100 U
$230.00
(0)

Thrombin can indirectly activate FX through feedback activation of FVII. Thrombin also activates other clotting factors, amplifying the coagulation cascade.

SR 12813

126411-39-0sc-204296
sc-204296A
10 mg
50 mg
$89.00
$338.00
(0)

SR 12813 (CAS 126411-39-0) is a compound that activates FXR, a nuclear receptor associated with the regulation of various physiological processes.

Fexaramine

574013-66-4sc-203580
sc-203580A
10 mg
50 mg
$398.00
$1380.00
1
(1)

Fexaramine (CAS 574013-66-4) is a chemical compound that activates FXR, a nuclear receptor involved in the modulation of diverse physiological processes.

GW 9662

22978-25-2sc-202641
5 mg
$68.00
30
(2)

GW4064 is a synthetic FXR agonist that was developed as a research tool to study FXR activation. It activates FXR in a manner similar to natural bile acids by binding to the receptor and promoting the transcription of target genes. GW4064 has been used in various experimental settings to explore FXR-mediated effects on metabolism and other physiological processes.

Chenodeoxycholic acid, free acid

474-25-9sc-278835
sc-278835A
1 g
5 g
$27.00
$115.00
(1)

CDCA is a primary bile acid that activates the farnesoid X receptor (FXR). When CDCA binds to FXR, it triggers the formation of FXR-RXR heterodimers, which then bind to specific DNA sequences in target gene promoters. This binding leads to the transcription of genes responsible for regulating bile acid synthesis, transport, and metabolism. This mechanism helps maintain the balance of bile acids in the body and supports the feedback regulation of bile acid levels.

Ursodeoxycholic acid

128-13-2sc-204935
sc-204935A
1 g
5 g
$51.00
$128.00
4
(0)

UDCA is a primary bile acid that has been shown to activate FXR. Similar to CDCA, UDCA binds to FXR and induces the formation of FXR-RXR heterodimers. This leads to the activation of genes involved in bile acid transport and detoxification. UDCA is often used therapeutically to treat certain liver disorders, and its FXR-mediated effects contribute to its beneficial effects on bile acid metabolism.