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Pregnane X Receptors

Pregnane X receptor (PXR) agonists activate a nuclear receptor that senses foreign compounds. PXR was reported in 1998 as an orphan nuclear receptor activated by pregnane steroids. In the same year, human PXR was shown to respond to compounds that induce cytochrome P450 3A4 (CYP3A4) and cause drug interactions. Ligand-bound PXR pairs with retinoid X receptor (RXR) and raises the expression of drug-metabolizing enzymes and transporters in liver and intestine. Rifampin and SR-12813 activate human PXR, while pregnenolone 16α-carbonitrile is the classic rodent agonist. Other listed activators include (3S,5S)-Atorvastatin, SJPYT-328, isobutylparaben and the bile acid precursor 7α-Hydroxy-4-cholesten-3-one.

3 Items

  • Pregnenolone 16α-carbonitrile
    Cat. No.
    A69677
    CAS No.
    1434-54-4

    Pregnenolone 16α-carbonitrile

    Pregnenolone 16α-carbonitrile is a potent activator of the pregnane X receptor (PXR), primarily utilized in rodent models. As a synthetic steroid, it effectively induces the expression of cytochrome P450 3A, playing a crucial role in drug metabolism. This compound has also been shown to enhance resistance to various stressors, making it valuable for research in pharmacology and toxicology.

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    5 mg
    $40.00
    25 mg
    $45.00
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  • (3S,5S)-Atorvastatin sodium salt
    Cat. No.
    A69930
    CAS No.
    1428118-38-0

    (3S,5S)-Atorvastatin sodium salt

    (3S,5S)-Atorvastatin sodium salt functions as a pregnane X receptor (PXR) activator. As the inactive enantiomer of Atorvastatin, it is primarily utilized in research to explore the regulatory mechanisms of drug metabolism and transport. Its application in studies related to cholesterol metabolism and lipid regulation makes it a valuable reagent in pharmaceutical and biochemical research.

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  • Cholic acid-Glu
    Cat. No.
    A85384
    CAS No.
    95051-21-1

    Cholic acid-Glu

    Cholic acid-Glu is a derivative of cholic acid that functions as a PXR (Pregnane X Receptor) activator. It has been shown to increase PXR activation, leading to a significant upregulation of the downstream target gene Cyp3a11 in small intestinal organoid tissue. This compound is particularly relevant for research on inflammatory bowel diseases, such as Crohn’s disease, due to its altered levels in affected individuals.

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