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 1 to 10 of 18 total

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Product NameCAS #Catalog #QUANTITYPriceCitationsRATING

Rifampicin

13292-46-1sc-200910
sc-200910A
sc-200910B
sc-200910C
1 g
5 g
100 g
250 g
$95.00
$322.00
$663.00
$1438.00
6
(1)

Known agonist of PXR; induces its activation and potentially its expression.

Hyperforin

11079-53-1sc-507549
250 µg
$420.00
(0)

Acts as a potent activator of PXR, leading to increased expression of target genes.

DHEA

53-43-0sc-202573
10 g
$109.00
3
(1)

DHEA functions as a potent ligand for the pregnane X receptor (PXR), influencing gene expression related to xenobiotic metabolism. Its structural conformation allows for effective binding, triggering distinct signaling cascades. The compound exhibits unique hydrophobic interactions, enhancing its stability in lipid environments. Furthermore, DHEA's metabolic pathways involve intricate enzymatic conversions, contributing to its diverse biological effects and regulatory mechanisms within cellular systems.

Pregnenolone

145-13-1sc-204860
sc-204860A
sc-204860B
sc-204860C
5 g
25 g
100 g
500 g
$85.00
$145.00
$340.00
$1100.00
(1)

Pregnenolone acts as a significant ligand for the pregnane X receptor (PXR), modulating transcriptional activity linked to various metabolic processes. Its unique steric configuration facilitates specific interactions with PXR, leading to the activation of downstream signaling pathways. The compound's lipophilic nature promotes its integration into cellular membranes, influencing membrane fluidity and receptor accessibility. Additionally, pregnenolone undergoes complex metabolic transformations, impacting its bioavailability and functional outcomes in cellular environments.

5,5-Diphenyl Hydantoin

57-41-0sc-210385
5 g
$70.00
(0)

Has been shown to activate PXR and subsequently influence the expression of PXR target genes.

Rifaximin

80621-81-4sc-205841B
sc-205841C
sc-205841
sc-205841A
sc-205841D
100 mg
250 mg
500 mg
1 g
5 g
$27.00
$41.00
$77.00
$103.00
$398.00
2
(1)

Rifaximin serves as a notable ligand for the pregnane X receptor (PXR), engaging in selective binding that influences gene expression related to xenobiotic metabolism. Its unique structural features enable it to stabilize the PXR conformation, enhancing receptor activation. The compound's hydrophobic characteristics facilitate its partitioning into lipid bilayers, affecting cellular uptake and distribution. Furthermore, rifaximin's metabolic pathways involve intricate enzymatic interactions, shaping its pharmacokinetic profile and biological effects.

Meclizine Dihydrochloride

1104-22-9sc-211779A
sc-211779
5 g
10 g
$66.00
$138.00
3
(1)

Meclizine Dihydrochloride acts as a potent modulator of the pregnane X receptor (PXR), exhibiting a distinct affinity that alters transcriptional activity linked to metabolic processes. Its unique molecular structure promotes specific interactions with PXR, leading to conformational changes that enhance receptor signaling. The compound's lipophilic nature aids in its integration into cellular membranes, influencing its bioavailability and interaction with various metabolic enzymes, thereby impacting its kinetic behavior in biological systems.

TCPOBOP

76150-91-9sc-203291
25 mg
$209.00
4
(1)

TCPOBOP serves as a selective agonist for the pregnane X receptor (PXR), characterized by its ability to induce significant conformational shifts in the receptor's structure. This compound engages in unique hydrogen bonding and hydrophobic interactions, facilitating enhanced receptor activation. Its distinct electronic properties influence the kinetics of ligand-receptor binding, promoting efficient transcriptional regulation of genes involved in xenobiotic metabolism and homeostasis.

Carbamazepine

298-46-4sc-202518
sc-202518A
1 g
5 g
$32.00
$70.00
5
(0)

Another antiepileptic agent that can activate PXR.

SR 12813

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

Synthetic compound known to be a potent PXR agonist.