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  4. Recombinant Human Cytochrome P450 2C8 (CYP2C8)

Recombinant Human Cytochrome P450 2C8 (CYP2C8)

  • 货号：
    CSB-EP006418HU
  • 规格：
    ￥1836
  • 图片：
    • (Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel.
  • 其他：

产品详情

  • 纯度：
    Greater than 85% as determined by SDS-PAGE.
  • 基因名：
    CYP2C8
  • Uniprot No.：
  • 别名：
    CP2C8_HUMAN; CPC8; CYP2C8; CYPIIC8; Cytochrome P450 2C8; Cytochrome P450 family 2 subfamily C polypeptide 8; Cytochrome P450 form 1; Cytochrome P450 IIC2; Cytochrome P450 MP-12; Cytochrome P450 MP-20; Cytochrome P450 subfamily IIC (mephenytoin 4 hydroxylase) polypeptide 8; Flavoprotein linked monooxygenase; Microsomal monooxygenase; MP 12/MP 20; P450 form 1; P450 IIC2; P450 MP 12/MP 20; S mephenytoin 4 hydroxylase; S-mephenytoin 4-hydroxylase; Xenobiotic monooxygenase
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full Length of Mature Protein
  • 来源：
    E.coli
  • 分子量：
    60.1 kDa
  • 表达区域：
    27-490aa
  • 氨基酸序列
    RKLPPGPTPLPIIGNMLQIDVKDICKSFTNFSKVYGPVFTVYFGMNPIVVFHGYEAVKEALIDNGEEFSGRGNSPISQRITKGLGIISSNGKRWKEIRRFSLTTLRNFGMGKRSIEDRVQEEAHCLVEELRKTKASPCDPTFILGCAPCNVICSVVFQKRFDYKDQNFLTLMKRFNENFRILNSPWIQVCNNFPLLIDCFPGTHNKVLKNVALTRSYIREKVKEHQASLDVNNPRDFIDCFLIKMEQEKDNQKSEFNIENLVGTVADLFVAGTETTSTTLRYGLLLLLKHPEVTAKVQEEIDHVIGRHRSPCMQDRSHMPYTDAVVHEIQRYSDLVPTGVPHAVTTDTKFRNYLIPKGTTIMALLTSVLHDDKEFPNPNIFDPGHFLDKNGNFKKSDYFMPFSAGKRICAGEGLARMELFLFLTTILQNFNLKSVDDLKNLNTTAVTKGIVSLPPSYQICFIPV
    Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
  • 蛋白标签：
    N-terminal 10xHis-tagged and C-terminal Myc-tagged
  • 产品提供形式：
    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.
  • 缓冲液：
    Tris-based buffer，50% glycerol
  • 储存条件：
    Store at -20°C/-80°C upon receipt, aliquoting is necessary for mutiple use. Avoid repeated freeze-thaw cycles.
  • 保质期：
    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.
  • 货期：
    Basically, we can dispatch the products out in 1-3 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.
    Note: All of our proteins are default shipped with normal blue ice packs, if you request to ship with dry ice, please communicate with us in advance and extra fees will be charged.
  • 注意事项：
    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.

产品评价

靶点详情

  • 功能：
    A cytochrome P450 monooxygenase involved in the metabolism of various endogenous substrates, including fatty acids, steroid hormones and vitamins. Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Primarily catalyzes the epoxidation of double bonds of polyunsaturated fatty acids (PUFA) with a preference for the last double bond. Catalyzes the hydroxylation of carbon-hydrogen bonds. Metabolizes all trans-retinoic acid toward its 4-hydroxylated form. Displays 16-alpha hydroxylase activity toward estrogen steroid hormones, 17beta-estradiol (E2) and estrone (E1). Plays a role in the oxidative metabolism of xenobiotics. It is the principal enzyme responsible for the metabolism of the anti-cancer drug paclitaxel (taxol).
  • 基因功能参考文献：
    1. In the villous trophoblast, CYP2C8 was the most abundant protein. Its expression is higher than the CYP2C9 and CYP2J2 in the cytotrophoblast in the embryonic stage of development and remains higher in syncytiotrophoblast of term placenta. PMID: 29908721
    2. The present study confirms the variable distribution of CYP2C8 (*2 and *3) and CYP2C9 (*2 and *3) allelic polymorphisms among South Indian diabetic populations. PMID: 28686288
    3. We found that SNPs rs7909236 and rs1934953 of the CYP2C8 gene were significantly associated with increased risk of essential hypertension. PMID: 28513222
    4. Clopidogrel increases the exposure to pioglitazone by inhibiting its CYP2C8-mediated biotransformation. PMID: 27260150
    5. Using an integrated pathway-based approach, we identified polymorphisms in ABCC6, ABCB1 and CYP2C8 associated with overall survival. These associations were replicated in a large independent cohort, highlighting the importance of pharmacokinetic genes as prognostic markers in Ewing sarcoma PMID: 27287205
    6. review summarizes glucuronides as CYP2C8 ligands and the active-site structural features of CYP2C8 that allow potential binding to glucuronides PMID: 28653847
    7. Preliminary results demonstrate SNPs in CYP2C8 represent potential genetic markers of coronary heart disease susceptibility. PMID: 28687336
    8. Inhibition of CYP2C8 activity adds to the protective effects of omega-3 LCPUFA on pathological retinal neovascularization and choroidal neovascularization. PMID: 27417579
    9. CYP2C8*3 carriers had an increased risk of peripheral neuropathy PMID: 27736846
    10. CYP2C8 Variants are associated with Ischemic Stroke. PMID: 27087514
    11. CYP2C8*3 is a gain-of-function polymorphism for imatinib N-demethylation, which appears to be mainly mediated by CYP2C8 and not CYP3A4 in vitro in human liver microsomes PMID: 26161459
    12. CYP2C8 genetic polymorphisms may influence outcome of taxane therapy in Roma and Hungarian populations. PMID: 26507668
    13. CYP2C8-derived epoxyeicosatrienoic acids prevented TNF-alpha-induced HUVECs apoptosis via inhibition of oxidative stress associated with the Nrf2 signaling. PMID: 26489615
    14. Interaction among CYP2C8, EPHX2, and CYP4A11 Gene Variants Significantly Increases the Risk for Ischemic Stroke. PMID: 25947240
    15. These comprehensive findings could inform for further genotype-phenotype studies on interindividual differences in CYP2C8-mediated drug metabolism PMID: 26427316
    16. Significant gene-sex interaction for CYP2C8*3 with twofold increase in the relative risk of essential hypertension and a similar tendency for CYP2J2*7 associated with coronary artery disease without myocardial infarction in Bulgarian males. PMID: 26404779
    17. We did not observe any association of CYP2C8*2, CYP2C8*3, CYP2C9*2 and CYP2C9*3 with myocardial infarction PMID: 25560582
    18. CYP2C8 polymorphisms affected neither R- nor S-ibuprofen PMID: 26122864
    19. the CYP2C8*3 allele has no major impact on paclitaxel metabolism in vitro or of paclitaxel-induced neuropathy PMID: 26115084
    20. Single nucleotide polymorphisms of CYP2C8,CYP2E1 and CYP4B1 are associated with susceptibility to gout in ethnic Han males population. PMID: 26252103
    21. Report impact of CYP2C8-HapC allele on paclitaxel/carboplatin-induced myelosuppression in patients with ovarian cancer. PMID: 21702053
    22. The present study shows that elevated EET levels in BC tissues are associated with upregulation of CYP2C8, 2C9, and 2J2, and downregulation of sEH, and are also associated with aggressive cell behavior in BC patients. PMID: 25406731
    23. Results show that CYP2C8 rs17110453 and EPHX2 rs751141 two-locus interaction confers a significantly higher risk for ischemic stroke. PMID: 25839935
    24. The sudy investigates the impact of OATP1B1 and CYP2C8 genotype and source of in vitro data on the prediction of drug-drug interaction risk for repaglinide. PMID: 24623479
    25. Patients with CYP2C8*2C and EPHX2 404del variants had worse long-term outcomes while those with EPHX2 287Gln, CYP2J2*7, and CYP2C9 g.816G variants had favorable outcomes. PMID: 25388680
    26. The CYP2C8 gene may be useful in the prevention and treatment of vascular inflammatory diseases. PMID: 25017038
    27. This study suggests that mitochondrially targeted variant 3 CYP2C8 may contribute to oxidative stress in various tissues. PMID: 25160618
    28. one intronic SNP in ABCG1 (rs492338) surpassed the exploratory significance threshold for an association with paclitaxel-induced neuropathy in the Caucasian cohort (p = 0.0008) but not in the non-Caucasian replication group PMID: 24706167
    29. Significant correlations with chemotherapy resistance were observed for CYP2C8*3 and CYP2C9*2 polymorphisms in patients with chronic lymphoproliferative diseases. PMID: 24288737
    30. And those of the genes CYP2C8, CYP3A5 and DPYD associated with toxicity. PMID: 24088129
    31. Based on overexpression of human CYP2C8 in mice, CYP2C8 appears to be part of a novel lipid metabolic pathway influencing retinal neovascularization. PMID: 24458713
    32. The increased risk of paclitaxel-induced neuropathy in patients who carry the CYP2C8*3 variant is replicated in African Americans and whites. PMID: 23413280
    33. We showed that CYP2C8*3 was associated with lower plasma levels of rosiglitazone and hence a reduced therapeutic response but also a lower risk of developing oedema during treatment with rosiglitazone. PMID: 23426382
    34. CYP2C8*3 is associated with decreased pioglitazone plasma exposure in vivo and significantly influences the pharmacokinetic magnitude of the gemfibrozil-pioglitazone drug-drug interaction PMID: 22625877
    35. Report impact of CYP2C8 polymorphisms on rosiglitazone pharmacokinetics and drug interactions. PMID: 23307233
    36. The study described polymorphisms of CYP2C8 in Chinese minorities for the first time, showing significant ethnic differences in the distribution of CYP2C8 among the Han, the Uighur, Hui, and Mongolian Chinese populations. PMID: 23336573
    37. The results indicated that AA and AG genotypes of CYP2C8 (rs1934951) might be predictors for multiple myeloma patients at high risk to develop bisphosphonate-related oxteonecrosis of the jaw. PMID: 23171856
    38. significant positive correlation between CYP2C8 rs 1934951 polymorphism and localization of ONJ. Applying PCA to clinical and biochemical factors sharply separates different variables significantly related to pathological process PMID: 22339777
    39. The translation efficiency (protein/mRNA ratio) for CYP2C8 was inversely correlated with the expression of miR-103 and miR-107. PMID: 22723340
    40. Allele frequencies of functionally important CYP2C8 variants in the Czech population are similar to that of other Caucasian populations. PMID: 22313047
    41. CYP2C8 rs11572080, 416G-A and rs10509681, 1196A-G carriers are more likely to achieve complete clinical response to neoadjuvant paclitaxel in the treatment of breast cancer. PMID: 22527101
    42. Co-administration of febuxostat had no effect on rosiglitazone or N-desmethylrosiglitazone pharmacokinetics, suggesting that febuxostat can be given safely with drugs metabolized through CYP2C8. PMID: 22242967
    43. Report impact of population diversity on the distribution of CYP2C8 polymorphisms among Brazilians. PMID: 21173785
    44. The putative binding site of diosmetin coincided with the CYP2C8 substrate binding site. PMID: 21791871
    45. Data suggest that sipoglitazar is metabolized first by UGT to form an unstable acyl glucuronide, and this acyl glucuronide is then deethylated by CYP2C8. PMID: 22028317
    46. CYP2C8 is the dominant enzyme in the biotransformation of montelukast in humans, accounting for about 80% of its metabolism. CYP3A4 only mediates the formation of the minor metabolite M5a/b, and is not important in the elimination of montelukast. PMID: 21838784
    47. The gemfibrozil-repaglinide interaction could be mainly explained by gemfibrozil 1-O-beta-glucuronide concentration-dependent, mechanism-based inhibition of CYP2C8. PMID: 21778352
    48. HRM analysis is a fast, reliable, accurate and cost-effective screening method for gene mutations, even very similar cDNA sequences with 83% identities, compared with CYP2C8 and CYP2C9 PMID: 22027337
    49. In vitro phenotyping indicated that montelukast is an appropriate probe for CYP2C8 inhibition studies. PMID: 21697463
    50. monocytes and macrophages express the epoxygenases CYP2J2 and CYP2C8 PMID: 22028915

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  • 亚细胞定位：
    Endoplasmic reticulum membrane; Peripheral membrane protein. Microsome membrane; Peripheral membrane protein.
  • 蛋白家族：
    Cytochrome P450 family
  • 数据库链接：

    HGNC: 2622

    OMIM: 601129

    KEGG: hsa:1558

    STRING: 9606.ENSP00000360317

    UniGene: Hs.709188