Date published: 2025-10-2

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PXR Activators

PXR activators are compounds that stimulate the activity or enhance the expression of the pregnane X receptor (PXR). PXR, also known as NR1I2 (nuclear receptor subfamily 1, group I, member 2), is a nuclear receptor that functions as a ligand-activated transcription factor. It is primarily expressed in the liver and intestines, and its main role is to sense the presence of foreign toxic substances and support the body's detoxification process by regulating genes involved in drug metabolism and transport. The ligand-binding domain of PXR has a notably flexible structure, allowing it to bind to a wide variety of endogenous and exogenous molecules, including prescription drugs, dietary supplements, and environmental contaminants. Upon ligand binding, PXR undergoes a conformational change that leads to its activation. The activated PXR forms a heterodimer with the retinoid X receptor (RXR) and then binds to specific DNA sequences, termed PXR response elements, to modulate the transcription of target genes. These target genes are often involved in drug metabolism and drug transport. PXR activators, by engaging with the receptor, can potentiate these regulatory effects, influencing the body's capacity to metabolize and excrete foreign compounds. The study of PXR activators provides insights into the body's adaptive mechanisms for responding to xenobiotic exposure. This understanding underscores the body's remarkable ability to recognize, process, and eliminate a myriad of diverse compounds, ensuring homeostasis and protection against toxic threats.

Items 11 to 18 of 18 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Hyperforin dicyclohexylammonium salt

238074-03-8sc-202178
sc-202178A
500 µg
1 mg
$137.00
$180.00
1
(2)

Hyperforin dicyclohexylammonium salt acts as a potent modulator of the pregnane X receptor (PXR), exhibiting unique binding dynamics that promote receptor dimerization. Its distinctive hydrophobic regions enhance molecular interactions, leading to altered receptor conformations. The compound's specific steric effects influence the rate of ligand binding and dissociation, thereby impacting downstream signaling pathways and gene expression related to metabolic processes.

2,2-Bis(4-hydroxyphenyl)butane

77-40-7sc-352249
sc-352249A
5 g
25 g
$145.00
$351.00
3
(0)

2,2-Bis(4-hydroxyphenyl)butane functions as a selective modulator of the pregnane X receptor (PXR), characterized by its ability to stabilize receptor-ligand complexes through hydrogen bonding and hydrophobic interactions. This compound exhibits unique conformational flexibility, allowing it to adapt to various binding sites on the receptor. Its kinetic profile reveals a distinct rate of activation, influencing transcriptional regulation of genes involved in xenobiotic metabolism and homeostasis.

Tris(2-butoxyethyl) phosphate

78-51-3sc-237373
100 g
$51.00
10
(0)

Tris(2-butoxyethyl) phosphate acts as a potent modulator of the pregnane X receptor (PXR), showcasing its ability to engage in specific electrostatic interactions that enhance receptor activation. Its unique branched structure promotes solubility and facilitates rapid diffusion across cellular membranes. The compound's distinct steric configuration allows for effective binding to PXR, influencing downstream signaling pathways related to detoxification processes and lipid metabolism.

GW 9662

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

GW 9662 is a selective antagonist of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting unique binding characteristics that disrupt receptor dimerization. Its hydrophobic regions enhance affinity for lipid bilayers, promoting cellular uptake. The compound's specific conformational changes upon binding alter the receptor's transcriptional activity, impacting gene expression related to metabolic regulation. Additionally, GW 9662's kinetic profile suggests a reversible interaction, allowing for nuanced modulation of PPARγ activity.

5-Pregnen-3β-ol-20-one-16α-carbonitrile

1434-54-4sc-227010
50 mg
$68.00
3
(1)

Potent rodent-specific PXR agonist.

Clotrimazole

23593-75-1sc-3583
sc-3583A
100 mg
1 g
$41.00
$56.00
6
(2)

Antifungal that has been shown to activate PXR in certain studies.

Citral

5392-40-5sc-252620
1 kg
$212.00
(1)

Has been shown to activate PXR and induce its target genes.

D,L-Sulforaphane

4478-93-7sc-207495A
sc-207495B
sc-207495C
sc-207495
sc-207495E
sc-207495D
5 mg
10 mg
25 mg
1 g
10 g
250 mg
$150.00
$286.00
$479.00
$1299.00
$8299.00
$915.00
22
(1)

Known to influence PXR activity, potentially leading to alterations in PXR expression.