Recombinant Human Nuclear receptor subfamily 1 group I member 2 (NR1I2)

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Code CSB-EP016048HU
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  • (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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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 including tag sequence, target protein sequence and linker sequence could be provided upon request.
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, pH 8.0.
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 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 Basically, we can dispatch the products out in 3-7 working days after receiving your orders. Delivery time may differ from different purchasing way or location, please kindly consult your local distributors for specific delivery time.
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.

Target Data

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
  1. EGF suppresses specifically CAR signaling mainly through transcriptional regulation and drives the xenobiotic response toward a pregnane X receptor (PXR)-mediated mechanism. PMID: 29269410
  2. 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
  3. An overview of NR1I2 and NR1I3 pharmacogenetic studies in various therapeutic fields. PMID: 29199543
  4. The pregnane X receptor (PXR) and the nuclear receptor corepressor 2 (NCoR2) modulate cell growth in head and neck squamous cell carcinoma. PMID: 29470550
  5. High endogenous pregnane X receptor (PXR) level is associated with poor sorafenib therapy outcome. PMID: 29369785
  6. 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
  7. 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
  8. NR1I2 has a role in promoting stem cell-mediated colon cancer relapse PMID: 27448961
  9. Dual ligands of CAR/PXR show distinct gene regulation patterns by regulating cross-talk between CAR and PXR. PMID: 27197997
  10. High PXR expression is associated with multidrug resistance in breast cancer. PMID: 26934120
  11. PXR, CYP3A4, and VIL1 expression was decreased only in the actively inflamed small intestinal tissue in children with Crohn's disease. PMID: 27013401
  12. 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
  13. 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
  14. Mulberroside A significantly suppressed PXR-mediated P-gp luciferase activity induced by rifampicin (Rif). PMID: 27918128
  15. This data indicates that 14-3-3sigma contributes to P-gp overexpression through interaction with PXR with rifampin and paclitaxel treatment. PMID: 28077325
  16. 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
  17. Genetic variations in PXR affect induction of Bupropion hydroxylation by sodium ferulate. PMID: 23840296
  18. 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
  19. 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
  20. 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
  21. 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
  22. 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
  23. Extracellular granzyme K mediates endothelial activation through the cleavage of PAR-1. PMID: 26936634
  24. Pregnane X receptor interacts with liver X receptor to regulate expression of SMPDL3A in primary hepatocytes. PMID: 28414139
  25. 66034T/C polymorphism of the human pregnane X receptor (hPXR) is potential risk factor for drug-resistant epilepsy. PMID: 27836114
  26. 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
  27. miR-30c-1-3p was shown to alter the expression of CYP3A4, a prototypical target gene of PXR. PMID: 27085140
  28. The nuclear receptor PXR regulates hepatic energy metabolism. (Review) PMID: 27041449
  29. Novel functions of PXR in cardiometabolic disease development have been described. (Review) PMID: 26924429
  30. 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
  31. Genome-wide comparison of the inducible transcriptomes of nuclear receptors CAR, PXR and PPARalpha in primary human hepatocytes has been presented. PMID: 26994748
  32. PXR regulates the intestinal epithelial barrier during inflammation by modulating cytokine-induced MLCK expression and JNK1/2 activation PMID: 27440420
  33. 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
  34. FGF21-PXR signaling pathway may be involved in decreased hepatic CYP3A4 metabolic activity in Nonalcoholic fatty liver disease. PMID: 27482056
  35. the -831C/T polymorphism has a direct effect on transcriptional regulation of PXR gene. PMID: 28198586
  36. 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
  37. 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
  38. The agonistic effects of two new flame retardants on PXR expression and activity are reported. PMID: 27506419
  39. Identify sixteen novel structurally different PXR activators capable of inducing CYP3A4 expression in HepG2 cells. PMID: 25455453
  40. suPAR is a useful surrogate biomarker for development of multiple organ dysfunction and severe sepsis after multiple traumas. PMID: 27121128
  41. 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
  42. EPAS-1 and PXR may cooperatively participate in development and especially MDR process of stomach cancer PMID: 26783937
  43. 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
  44. We found that ARRDC3 is required for ALIX ubiquitination induced by activation of PAR1 PMID: 26490116
  45. hPXR is regulated through its phosphorylation at threonine-408 by PKC, CHIP/chaperone-dependent stability check, and autophagic degradation pathway. PMID: 26534988
  46. we have identified novel PXR dependent pathways in human de novo lipogenesis, which may participate in hepatic steatosis and pathogenesis of steatohepatitis PMID: 25182422
  47. Role of NR1I2 polymorphisms in head and neck squamous cell carcinoma PMID: 26141049
  48. Our results revealed that PXR could be a determinant of stable warfarin doses. PMID: 25848132
  49. 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
  50. Genotyping of CYP3A4/MDR1/NR1I2 polymorphisms may be helpful for better guiding tacrolimus dosing in CYP3A5 nonexpressers. PMID: 26228923
  51. Data show that pregnane X receptor/retinoid X receptor PXR/RXR-[alpha], RXR-[beta], or RXR-[gamma] expression was noted in 9 (16.4%), 9 (16.4%), and 10 (18.2%) pancreatic adenocarcinoma cases, respectively. PMID: 26355550
  52. PSC is characterized by disease-specific impairment of SULT2A1 expression following PXR activation, a phenomenon which is not noted in PBC, and may account for the impaired hepatoprotection in PSC. PMID: 26504856
  53. data reveal that the SUMOylation and ubiquitylation of the PXR interface in a fundamental manner directs its biologic function in the liver in response to xenobiotic or inflammatory stress. PMID: 26063058
  54. Optical Isomers of Atorvastatin, Rosuvastatin and Fluvastatin Enantiospecifically Activate Pregnane X Receptor PXR and Induce CYP2A6, CYP2B6 and CYP3A4 in Human Hepatocytes. PMID: 26366873
  55. we found that the PAR1 IVS-14 A/T rs168753 polymorphism was associated with the development of COPD. PMID: 26535635
  56. PAR-1 activation in endothelial colony forming cells increases chemotactic gene expression and leukocyte recruitment at ischemic sites through a COX-2-dependent mechanism PMID: 26026674
  57. Our study led to the identification of phytochemicals, which showed interaction with at least one experimentally determined active site residue of PAR1, showed no violations to Lipinski's rule of five along with predicted high human absorption PMID: 25007158
  58. Aging and SXR mRNA significantly affect the expression of CYP3A4- and CYP3A5-specific mRNA as measured by their concentration in monocytes PMID: 25916520
  59. Stimulation of thrombin receptor PAR1 in the model induced cytoplasmic calcium oscillations, calcium uptake by mitochondria, opening of the permeability transition pore and collapse of the mitochondrial membrane potential PMID: 26391841
  60. findings establish a functional interconnection between ER stress and signaling of proinflammatory cytokines in the regulation of PXR expression PMID: 25616597
  61. Data suggest that transmembrane domains of G protein-coupled receptors PAR1 (proteinase-activated receptor 1), ADRB2 (beta-2 adrenergic receptor), and OPRM1 (opioid receptor mu 1) are highly ordered when embedded in bicelles/lipid bilayers. PMID: 25740347
  62. Expression of CYP3A4 is largely due to the activation of Pregnane X Receptor (PXR) and PXR rs7643645 polymorphism is associated with higher PSA level in prostate cancer. PMID: 24924803
  63. Pregnane X receptor alters cell morphology and induces cell migration through repression of HNF4alpha and induction of IGFBP1. PMID: 26232425
  64. Ser(350) of hPXR is crucial for formation of the hPXR-retinoid X receptor alpha heterodimer. PMID: 26119819
  65. It is suggested that the functions of PXR, CAR and AhR may be closely implicated in the pathogeneses of metabolic vascular diseases, such as hyperlipidemia, atherogenesis, and hypertension. PMID: 24859622
  66. Two PXR SNP genotypes and 2 haplotypes influenced the risk of HEPATOTOXICITY DURING ANTITUBERCULOSIS TREATMENT only in females. The PXR SNP showed a sex-specific impact that contributed to an increased HATT risk in females PMID: 26091473
  67. These data demonstrate that GelE from Enterococcus faecalis can regulate enteric epithelial permeability via PAR2. PMID: 25916983
  68. Findings suggest that catalytically inactive thrombin can bind to and modulate PAR1 function in vitro. PMID: 25934730
  69. We found EMT in gastric cancer cell lines that underwent alpha-thrombin-induced PAR1 activation. PMID: 25231630
  70. Suggest that PXR and CAR double humanized mice are more sensitive rifampcin induction of cytochrome P450 and UDP-glucuronosyltransferases. PMID: 25835148
  71. PXR is expressed in liver, acts through a DNA response element located in the CYP3A promoter, and is activated by a structurally diverse collection of drugs that induce CYP3A. Review. PMID: 25831443
  72. The pregnane X receptor (PXR) tightly regulates the expression of genes in the hepatic drug-clearance system and its undesired activation plays a role in drug-induced liver injury PMID: 25252616
  73. The rs3814058C>T polymorphism of PXR interacts with smoking on increasing lung cancer risk in Chinese smokers. PMID: 25268617
  74. Due to the observed differences in activation of polar bear and human PXRs, exposure of each species to environmental agents is likely to induce biotransformation differently in the two species. PMID: 25680588
  75. this study reports the first structure of PXR in complex with a biologics (Adnectin-1), suggesting that an Adnectin can substitute for SRC-1 co-activator peptide and potentially be used as a crystallization chaperone to obtain structures of PXR with compounds of interest. PMID: 25579995
  76. Results suggest that expression of Ets family members, in conjunction with Pax5, LEF-1 and c-Jun, lead to coordinated up-regulation of PXR gene transcription. PMID: 25265064
  77. This study concluded that diindolylmethane induces pregnane X receptor -regulated CYP3A4 and MDR1 gene expression. PMID: 25542144
  78. These results indicate that the expression of PAR1 and PAR2 in esophageal squamous cell carcinoma is increased but PAR4 is decreased. PMID: 25297082
  79. NLRP3 was identified as a transcriptional target of PXR. PMID: 25202020
  80. by increasing protein expression and interacting with PAR1, thrombin promotes human pulmonary fibroblasts proliferation. PMID: 24523227
  81. Bisphenol A increased atherosclerosis in ApoE-/- mice in a human PXR-dependent manner. PMID: 24755147
  82. Suggest a novel role for PXR signaling in the maintenance of intestinal homeostasis and may help to elucidate additional mechanisms through which PXR signaling is protective in inflammatory bowel disease. PMID: 24486481
  83. the progression of A549 cells is able to be inhibited by knockdown of PAR1 expression. Efficient delivery of the specific siRNA targeting PAR1 may be used for further study in clinical cancer therapy. PMID: 24604247
  84. High Protease-activated receptor-1 drives pancreatic cancer progression and chemoresistance. PMID: 24436106
  85. Results suggest that PXR*1B, in combination with HNF4alpha rs2071197, might be associated with the C/Dconcentration-to-dose ratios and the duration to reach the maintenance dose of carbamazepine therapy. PMID: 24384557
  86. The polymorphisms investigated in PPARA (rs1800206), RXRA (rs11381416), and NR1I2 (rs1523130) did not influence the lipid-lowering efficacy and safety of statin and our results show the possible influence of NR1I3 genetic variant on the safety of statin. PMID: 24232815
  87. It could be speculated that, due to its dual role as a xenosensor and a regulator of energy metabolism, PXR, in concert with a mixture of PXR agonists in the environment, contributes to the present-day type 2 diabetes epidemic. PMID: 24166671
  88. Data suggest that post-transcriptional and post-translational modifications of PXR are critical in regulation of xenobiotic-metabolizing cytochrome P450 enzymes, mainly in hepatic tissue. [REVIEW] PMID: 24329114
  89. Persistent PAR1 signaling due to the absence of membrane PHB and decreased PAR1 degradation caused by the upregulation of intracellular PHB in cancer cells may render them highly invasive. PMID: 24732013
  90. In the promoter region of SXR. PMID: 24088131
  91. Post-translational regulation of pregnane X receptor via phosphorylation is by ubiquitination by DYRK2 and UBR5. PMID: 24438055
  92. Role of PPAR, LXR, and PXR in epidermal homeostasis and inflammation. PMID: 24315978
  93. Role of pregnane X receptor in obesity and glucose homeostasis PMID: 24362030
  94. Each tested drugs were determined and compared in AhR-, GR- and PXR-gene reporter cell lines. PMID: 24316275
  95. For the first time, direct evidence is provided that PXR is phosphorylated at specific residues, suggesting that further investigation is warranted to fully understand the regulation of PXR by phosphorylation. PMID: 24184507
  96. A total of 101 renal transplant recipients receiving cyclosporine were genotyped for CYP3A4(*)1G, CYP3A5(*)3, ABCB1 C1236T, G2677T/A, C3435T, NFKB1 -94 ins/del ATTG, and NR1I2 polymorphisms. PMID: 23503472
  97. Activation of PXR in hepatocytes is mediated through serum- and glucocorticoid-regulated kinase (SGK)2. PMID: 24204015
  98. Neutrophil elastase and proteinase-3 trigger G protein-biased signaling through proteinase-activated receptor-1 (PAR1). PMID: 24052258
  99. PAR1 and PAR4 require allosteric changes induced via receptor cleavage by alpha-thrombin to mediate heterodimer formation PMID: 24097976
  100. Developed a protocol using the nonradioactive electrophoretic mobility shift assay to study interactions between human pregnane X receptor with promoter CYP3A4 response element DNA sequences. PMID: 23977680

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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

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