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FXR

Farnesoid X receptor (FXR) agonists and antagonists act on a nuclear receptor that senses bile acids. In 1999 three groups identified bile acids such as chenodeoxycholic acid as endogenous FXR ligands. FXR is expressed mainly in liver, intestine and kidney, where it controls bile acid synthesis, transport and enterohepatic circulation. Activated FXR induces small heterodimer partner, which represses cholesterol 7α-hydroxylase, the rate-limiting enzyme of bile acid synthesis. FXR ligands are used to study bile acid, lipid and glucose metabolism and liver fibrosis models. Steroidal agonists include obeticholic acid, a semisynthetic bile acid analog. GW4064, cilofexor and tropifexor are nonsteroidal agonists, while DY 268 serves as an FXR antagonist.

3 Items

  • Chenodeoxycholic acid 3-glucuronide
    Cat. No.
    A74872
    CAS No.
    58814-71-4

    Chenodeoxycholic acid 3-glucuronide

    Chenodeoxycholic acid 3-glucuronide is an active metabolite of Chenodeoxycholic acid that serves as a selective Farnesoid X receptor (FXR) activator, exhibiting an EC50 of 8 μM in in vitro assays. This compound effectively modulates FXR signaling pathways, which are crucial for bile acid homeostasis and lipid metabolism. Research applications include studying metabolic disorders, liver physiology, and the potential therapeutic effects of FXR activation in various disease models.

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    1 mg
    $80.00
    5 mg
    $200.00
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  • 5β-Cholane
    Cat. No.
    A74916
    CAS No.
    80373-86-0

    5β-Cholane

    5β-Cholane is a potent activator of the farnesoid X receptor (FXR). It plays a critical role in regulating bile acid homeostasis and lipid metabolism, making it a valuable tool for investigating cholesterol and lipid-related disorders. Researchers can utilize 5β-Cholane to better understand the molecular mechanisms underlying metabolic diseases and to explore therapeutic interventions targeting FXR.

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  • FXR agonist 9
    Cat. No.
    A74919
    CAS No.
    2982502-32-7

    FXR agonist 9

    FXR agonist 9 is a selective partial agonist of the farnesoid X receptor (FXR) with an EC50 of 0.09 µM, exhibiting 75.13% maximum efficacy. This compound has demonstrated the ability to improve pathological features associated with metabolic dysfunction and steatohepatitis in mouse models induced by a high-fat diet and carbon tetrachloride. FXR agonist 9 is valuable for research into metabolic disorders and liver diseases.

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