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Key Documents

SRP2158

Sigma-Aldrich

Pregnane X Receptor human

recombinant, expressed in insect cells, ≥80% (SDS-PAGE)

Synonym(s):

BXR, ONR1, PAR, PAR1, PAR2, PARq, PRR, PXR

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About This Item

UNSPSC Code:
12352200
NACRES:
NA.26

biological source

human

recombinant

expressed in insect cells

Assay

≥80% (SDS-PAGE)

form

frozen liquid

mol wt

~51.6 kDa

packaging

pkg of 5 μg

storage condition

avoid repeated freeze/thaw cycles

concentration

650 μg/mL

color

clear colorless

NCBI accession no.

NM_003889

UniProt accession no.

O75469

shipped in

dry ice

storage temp.

−70°C

Gene Information

human ... NR1I2(8856)

Biochem/physiol Actions

The nuclear pregnane X receptor (PXR; NR1I2) is an important component of the body′s adaptive defense mechanism against toxic substances including foreign chemicals (xenobiotics). PXR is activated by a large number of endogenous and exogenous chemicals including steroids, antibiotics, antimycotics, bile acids, and the herbal antidepressant St. John′s wort. PXR is known to regulate the expression of several additional genes encoding proteins involved in xenobiotic metabolism, including multidrug resistance protein 1 (MDR1), multidrug resistance-associated protein 2 (MRP2), and organic anion transporter polypeptide 2. Elucidation of the three-dimensional structure of the PXR ligand binding domain revealed that it has a large, spherical ligand binding cavity that allows it to interact with a wide range of hydrophobic chemicals. Thus, unlike other nuclear receptors that interact selectively with their physiological ligands, PXR serves as a generalized sensor of hydrophobic toxins. PXR binds as a heterodimer with the 9-cis retinoic acid receptor (NR2B) to DNA response elements in the regulatory regions of cytochrome P450 3A monooxygenase genes and a number of other genes involved in the metabolism and elimination of xenobiotics from the body. Although PXR evolved to protect the body, its activation by a variety of prescription drugs represents the molecular basis for an important class of harmful drug-drug interactions. Thus, assays that detect PXR activity will be useful in developing safer prescription drugs.

Physical form

Clear and colorless frozen liquid solution

Preparation Note

Use a manual defrost freezer and avoid repeated freeze-thaw cycles. While working, please keep sample on ice.

Storage Class Code

12 - Non Combustible Liquids

WGK

WGK 1

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Regulatory Listings

Regulatory Listings are mainly provided for chemical products. Only limited information can be provided here for non-chemical products. No entry means none of the components are listed. It is the user’s obligation to ensure the safe and legal use of the product.

EU REACH Annex XVII (Restriction List)

CAS No.

EU REACH Annex XIV (Authorisation List)

CAS No.

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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P Honkakoski et al.
The Biochemical journal, 347(Pt 2), 321-337 (2000-04-06)
Members of the nuclear-receptor superfamily mediate crucial physiological functions by regulating the synthesis of their target genes. Nuclear receptors are usually activated by ligand binding. Cytochrome P450 (CYP) isoforms often catalyse both formation and degradation of these ligands. CYPs also
D J Waxman
Archives of biochemistry and biophysics, 369(1), 11-23 (1999-08-27)
The biochemistry of foreign compound metabolism and the roles played by individual cytochrome P450 (CYP) enzymes in drug metabolism and in the toxification and detoxification of xenochemicals prevalent in the environment are important areas of molecular pharmacology and toxicology that
G Bertilsson et al.
Proceedings of the National Academy of Sciences of the United States of America, 95(21), 12208-12213 (1998-10-15)
Nuclear receptors regulate metabolic pathways in response to changes in the environment by appropriate alterations in gene expression of key metabolic enzymes. Here, a computational search approach based on iteratively built hidden Markov models of nuclear receptors was used to
Andreas Elentner et al.
Experimental dermatology, 24(11), 835-840 (2015-05-28)
Skin is in daily contact with potentially harmful molecules from the environment such as cigarette smoke, automobile emissions, industrial soot and groundwater. Pregnane X receptor (PXR) is a transcription factor expressed in liver and intestine that is activated by xenobiotic

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