Product Details

Purity

Greater than 90% as determined by SDS-PAGE.

Target Names

NR1I2

Uniprot No.

O75469

Research Area

Signal Transduction

Alternative Names

BXR; Nr1i2; NR1I2_HUMAN; Nuclear receptor subfamily 1 group I member 2; ONR 1; ONR1; Orphan nuclear receptor PAR 1; Orphan nuclear receptor PAR1; Orphan nuclear receptor PXR; OTTHUMP00000215173; OTTHUMP00000215174; OTTHUMP00000215175; PAR 1; PAR 2; PAR; PAR q; PAR1; PAR2; PARq; pregnane X nuclear receptor variant 2; Pregnane X receptor; PRR; PXR; SAR; Steroid and xenobiotic receptor; SXR

Species

Homo sapiens (Human)

Source

E.coli

Expression Region

1-434aa

Target Protein Sequence

MEVRPKESWNHADFVHCEDTESVPGKPSVNADEEVGGPQICRVCGDKATGYHFNVMTCEGCKGFFRRAMKRNARLRCPFRKGACEITRKTRRQCQACRLRKCLESGMKKEMIMSDEAVEERRALIKRKKSERTGTQPLGVQGLTEEQRMMIRELMDAQMKTFDTTFSHFKNFRLPGVLSSGCELPESLQAPSREEAAKWSQVRKDLCSLKVSLQLRGEDGSVWNYKPPADSGGKEIFSLLPHMADMSTYMFKGIISFAKVISYFRDLPIEDQISLLKGAAFELCQLRFNTVFNAETGTWECGRLSYCLEDTAGGFQQLLLEPMLKFHYMLKKLQLHEEEYVLMQAISLFSPDRPGVLQHRVVDQLQEQFAITLKSYIECNRPQPAHRFLFLKIMAMLTELRSINAQHTQRLLRIQDIHPFATPLMQELFGITGS
Note: The complete sequence may include tag sequence, target protein sequence, linker sequence and extra sequence that is translated with the protein sequence for the purpose(s) of secretion, stability, solubility, etc.
If the exact amino acid sequence of this recombinant protein is critical to your application, please explicitly request the full and complete sequence of this protein before ordering.

Mol. Weight

69.8kDa

Protein Length

Full Length

Tag Info

N-terminal 10xHis-SUMO-tagged and C-terminal Myc-tagged

Form

Liquid or Lyophilized powder
Note: We will preferentially ship the format that we have in stock, however, if you have any special requirement for the format, please remark your requirement when placing the order, we will prepare according to your demand.

Buffer

If the delivery form is liquid, the default storage buffer is Tris/PBS-based buffer, 5%-50% glycerol.
Note: If you have any special requirement for the glycerol content, please remark when you place the order.
If the delivery form is lyophilized powder, the buffer before lyophilization is Tris/PBS-based buffer, 6% Trehalose.

Reconstitution

We recommend that this vial be briefly centrifuged prior to opening to bring the contents to the bottom. Please reconstitute protein in deionized sterile water to a concentration of 0.1-1.0 mg/mL.We recommend to add 5-50% of glycerol (final concentration) and aliquot for long-term storage at -20°C/-80°C. Our default final concentration of glycerol is 50%. Customers could use it as reference.

Troubleshooting and FAQs

Protein FAQs

Storage Condition

Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.

Shelf Life

The shelf life is related to many factors, storage state, buffer ingredients, storage temperature and the stability of the protein itself.
Generally, the shelf life of liquid form is 6 months at -20°C/-80°C. The shelf life of lyophilized form is 12 months at -20°C/-80°C.

Lead Time

3-7 business days

Notes

Repeated freezing and thawing is not recommended. Store working aliquots at 4°C for up to one week.

Datasheet & COA

Please contact us to get it.

Description

The recombinant Human NR1I2 was expressed with the amino acid range of 1-434. This NR1I2 protein is theoretically predicted to have a molecular weight of 69.8 kDa. This NR1I2 protein is produced using e.coli expression system. The NR1I2 coding gene included the N-terminal 10xHis-SUMO tag and C-terminal Myc tag, which simplifies the detection and purification processes of the recombinant NR1I2 protein in following stages of expression and purification.

Nuclear receptor subfamily 1 group I member 2 (NR1I2), also known as the pregnane X receptor (PXR), is a nuclear receptor involved in the regulation of various metabolic processes. NR1I2 acts as a ligand-activated transcription factor, responding to a diverse array of xenobiotics, including drugs and environmental substances. Upon activation, NR1I2 forms heterodimers with the retinoid X receptor (RXR) and binds to specific response elements in the DNA, leading to the regulation of target gene expression. Its primary role is in the detoxification and elimination of foreign compounds by modulating the expression of drug-metabolizing enzymes and transporters. Research on NR1I2 spans drug metabolism, pharmacology, and toxicology, exploring its impact on drug interactions and therapeutic responses.

Target Background

Function

Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes.

Gene References into Functions

EGF suppresses specifically CAR signaling mainly through transcriptional regulation and drives the xenobiotic response toward a pregnane X receptor (PXR)-mediated mechanism. PMID: 29269410
The bosutinib C0 in patients with the NR1I2 7635G/G or 8055T/T genotype was significantly lower than those in patients with the 7635A allele or 8055C allele. PMID: 29736778
An overview of NR1I2 and NR1I3 pharmacogenetic studies in various therapeutic fields. PMID: 29199543
The pregnane X receptor (PXR) and the nuclear receptor corepressor 2 (NCoR2) modulate cell growth in head and neck squamous cell carcinoma. PMID: 29470550
High endogenous pregnane X receptor (PXR) level is associated with poor sorafenib therapy outcome. PMID: 29369785
A total of six studies with 4248 cases and 3853 controls were included in this meta-analysis. Three PXR gene polymorphisms were evaluated: rs1523127, rs2276707, and rs6785049. Our analyses of rs1523127, rs2276707, and rs6785049 suggested that PXR gene polymorphism had no obvious influence on the risk of inflammatory bowel disease in Caucasians. PMID: 28742404
genotypes and haplotypes of PXR rs3814057, rs3814058 and rs6785049 have impact on the major adverse cardiovascular events in clopidogrel treated patients after percutaneous coronary intervention PMID: 29432831
NR1I2 has a role in promoting stem cell-mediated colon cancer relapse PMID: 27448961
Dual ligands of CAR/PXR show distinct gene regulation patterns by regulating cross-talk between CAR and PXR. PMID: 27197997
High PXR expression is associated with multidrug resistance in breast cancer. PMID: 26934120
PXR, CYP3A4, and VIL1 expression was decreased only in the actively inflamed small intestinal tissue in children with Crohn's disease. PMID: 27013401
NR1I2 g.7635A>G had a significant interaction with time, but the dose-adjusted tacrolimus concentration did not significantly differ over 5 years post-transplantation, except for the GG genotype of NR1I2 g.7635A>G. PMID: 28945481
Together, our results suggest that protection of the endothelial barrier by APC/TR47-mediated signaling pathways might be a valuable therapeutic approach to prevent metastasis PMID: 29196264
Mulberroside A significantly suppressed PXR-mediated P-gp luciferase activity induced by rifampicin (Rif). PMID: 27918128
This data indicates that 14-3-3sigma contributes to P-gp overexpression through interaction with PXR with rifampin and paclitaxel treatment. PMID: 28077325
Data suggest both PXR and CAR are expressed in testis/Sertoli cells; exposure of Sertoli cells (in vitro model of blood-testis barrier) to PXR or CAR ligands (including antiretroviral drugs) up-regulates expression of Pgp/ABCB1, BCRP, and MRP4. (PXR = pregnane X receptor; CAR = constitutive androstane receptor; Pgp/ABCB1 = P-glycoprotein ABCB1; BCRP = breast cancer resistance protein; MRP4 =multidrug resistance protein 4) PMID: 28970358
Genetic variations in PXR affect induction of Bupropion hydroxylation by sodium ferulate. PMID: 23840296
This study revealed for the first time the involvement of NR1I2 in the pharmacogenetics of irinotecan and suggest that it may help to predict the toxicity of low-dose irinotecan. PMID: 27116457
In intrahepatic cholestasis of pregnancy, gene silencing of miR-148a upregulated PXR expression which was inhibited by estradiol in liver cells. miR-148a may be involved in the estrogen induction in ICP via PXR signaling. MRP3 may be involved. PMID: 28575098
this study shows that PXR augments Mycobacterium tuberculosis survival inside the host macrophages by promoting the foamy macrophage formation and abrogating phagolysosomal fusion, inflammation, and apoptosis PMID: 27233963
This is the first time an association between NR1I2 polymorphism and time of progression to AIDS is reported and supports an apparent relationship between the gene in the immune response and identifies another genetic factor influencing AIDS progression. PMID: 28327790
MD simulations further revealed that the presence of small molecule at allosteric site disrupts the LBD dynamics and locks the LBD in a "tightly-contracted" conformation. The molecular details provided here could guide new structural studies to understand PXR activation and antagonism. PMID: 27515410
Extracellular granzyme K mediates endothelial activation through the cleavage of PAR-1. PMID: 26936634
Pregnane X receptor interacts with liver X receptor to regulate expression of SMPDL3A in primary hepatocytes. PMID: 28414139
66034T/C polymorphism of the human pregnane X receptor (hPXR) is potential risk factor for drug-resistant epilepsy. PMID: 27836114
The data suggest that some of the natural PXR variants may have adverse physiological consequences owing to its influence on the expression levels and functional output of drug-metabolizing enzymes and transporters. PMID: 26962022
miR-30c-1-3p was shown to alter the expression of CYP3A4, a prototypical target gene of PXR. PMID: 27085140
The nuclear receptor PXR regulates hepatic energy metabolism. (Review) PMID: 27041449
Novel functions of PXR in cardiometabolic disease development have been described. (Review) PMID: 26924429
Acetylation of lysine 109 modulates PXR DNA binding and transcriptional activity; PXR acetylation status and transcriptional activity are modulated by E1A binding protein (p300) and SIRT1. PMID: 26855179
Genome-wide comparison of the inducible transcriptomes of nuclear receptors CAR, PXR and PPARalpha in primary human hepatocytes has been presented. PMID: 26994748
PXR regulates the intestinal epithelial barrier during inflammation by modulating cytokine-induced MLCK expression and JNK1/2 activation PMID: 27440420
The polymorphism frequency of PXR11156A; C/11193 T; C and 8055C; T were 49.6 and 49.3%, and the rate of PXR (*) 1B haplotype was 48.8%. None of the pain scores, consumption of fentanyl 24 h post-operatively or enzyme activity of CYP3A4, showed differences among different genotypes. PMID: 27876007
FGF21-PXR signaling pathway may be involved in decreased hepatic CYP3A4 metabolic activity in Nonalcoholic fatty liver disease. PMID: 27482056
the -831C/T polymorphism has a direct effect on transcriptional regulation of PXR gene. PMID: 28198586
These findings demonstrated that rifaximin causes PXR-mediated inhibition of angiogenic factors in Caco-2 cell line and may be a promising anticancer tool. PMID: 27279570
rs3842689, 7635G>A (rs6785049), and 24381C>A (rs1523127) PXR polymorphisms have no obvious impact on FK506; furthermore, the PXR rs3842689 wild-type homozygous WW genotype is a risk factor of FK506 and results in gastrointestinal reactions. PMID: 27706725
The agonistic effects of two new flame retardants on PXR expression and activity are reported. PMID: 27506419
Identify sixteen novel structurally different PXR activators capable of inducing CYP3A4 expression in HepG2 cells. PMID: 25455453
suPAR is a useful surrogate biomarker for development of multiple organ dysfunction and severe sepsis after multiple traumas. PMID: 27121128
result suggests that in Indonesian patients with tuberculosis, the risk of having antituberculosis drug-induced liver injury was associated with TT genotype of the PXR gene PMID: 26417664
EPAS-1 and PXR may cooperatively participate in development and especially MDR process of stomach cancer PMID: 26783937
Reported is the distribution of allelic and genotypic frequencies of IL1A, IL4, NFKB1 and PAR1 variants in Native American, African, and European populations of Brazil and their association with predisposition to cancer. PMID: 26879815
We found that ARRDC3 is required for ALIX ubiquitination induced by activation of PAR1 PMID: 26490116
hPXR is regulated through its phosphorylation at threonine-408 by PKC, CHIP/chaperone-dependent stability check, and autophagic degradation pathway. PMID: 26534988
we have identified novel PXR dependent pathways in human de novo lipogenesis, which may participate in hepatic steatosis and pathogenesis of steatohepatitis PMID: 25182422
Role of NR1I2 polymorphisms in head and neck squamous cell carcinoma PMID: 26141049
Our results revealed that PXR could be a determinant of stable warfarin doses. PMID: 25848132
Carriers of two copies of the ATG haplotypes of NR1I2-rs1523130, rs3814055 and rs1523127 were less sensitive to thrombocytopenia than those harboring other haplotypes PMID: 26267044
Genotyping of CYP3A4/MDR1/NR1I2 polymorphisms may be helpful for better guiding tacrolimus dosing in CYP3A5 nonexpressers. PMID: 26228923

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Subcellular Location

Nucleus.

Protein Families

Nuclear hormone receptor family, NR1 subfamily

Tissue Specificity

Expressed in liver, colon and small intestine.

Database Links

HGNC: 7968

OMIM: 603065

KEGG: hsa:8856

STRING: 9606.ENSP00000336528

UniGene: Hs.7303

Code	CSB-EP016048HU
Abbreviation	Recombinant Human NR1I2 protein
MSDS	MSDS Datasheet
Size	$224
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Image	(Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel. Based on the SEQUEST from database of E.coli host and target protein, the LC-MS/MS Analysis result of CSB-EP016048HU could indicate that this peptide derived from E.coli-expressed Homo sapiens (Human) NR1I2. Based on the SEQUEST from database of E.coli host and target protein, the LC-MS/MS Analysis result of CSB-EP016048HU could indicate that this peptide derived from E.coli-expressed Homo sapiens (Human) NR1I2.
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Recombinant Human Nuclear receptor subfamily 1 group I member 2 (NR1I2)

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