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  4. Recombinant Human P2Y purinoceptor 12 (P2RY12)

Recombinant Human P2Y purinoceptor 12 (P2RY12)

  • 货号：
    CSB-CF861997HU
  • 规格：
    ￥9720
  • 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：
  • Uniprot No.：
  • 别名：
    P2RY12; HORK3; P2Y purinoceptor 12; P2Y12; ADP-glucose receptor; ADPG-R; P2T(AC; P2Y(AC; P2Y(cyc; P2Y12 platelet ADP receptor; P2Y(ADP; SP1999
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    Full Length
  • 来源：
    in vitro E.coli expression system
  • 分子量：
    42.2 kDa
  • 表达区域：
    1-342aa
  • 氨基酸序列
    MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFIIFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITIDRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKSEFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFIIIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFFLCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
    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
  • 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：
    Lyophilized from Tris/PBS-based buffer, 6% Trehalose, pH 8.0
  • 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：
    Receptor for ADP and ATP coupled to G-proteins that inhibit the adenylyl cyclase second messenger system. Not activated by UDP and UTP. Required for normal platelet aggregation and blood coagulation.
  • 基因功能参考文献：
    1. Downregulation of the P2Y12 receptor in the superior cervical ganglia after myocardial ischemia may improve cardiac function by alleviating the sympathoexcitatory reflex PMID: 28949406
    2. TRAP-6 induced platelet activation leads to an elevation of purinergic receptor P2Y12 expression. PMID: 29902630
    3. upon platelet activation with ADP, the number of GP IIb-IIIa and P2Y12 receptors increases, which may serve as evidence of these proteins being synthesized in the activated platelets PMID: 27028818
    4. In patients with type 2 diabetes, the presence of chronic kidney disease is associated with hyperreactive platelets and a dysfunctional status of the P2Y12 receptor signalling pathway. PMID: 27786340
    5. We documented a different effect of CYP2C19 and P2Y12 receptor polymorphisms on platelet reactivity and cardiovascular outcome in coronary artery disease patients after percutaneous coronary intervention on clopidogrel treatment. Importantly, increased platelet reactivity adversely affects the cardiovascular outcome independently of the studied polymorphisms. PMID: 28329746
    6. Findings offer insight into positive regulation of Akt signaling through P2Y12 phosphorylation as well as MAPK signaling in platelets by ASK1. PMID: 28753204
    7. Genomic association study identified deleterious rare variants in P2RY12 in patients with ischemic stroke. PMID: 29232918
    8. Expression of platelet hsa-miR-223 increased and P2RY12 mRNA reduced in type 2 diabetic patients following ET non-significantly. PMID: 29526844
    9. The meta-analysis shows a potential of association between P2RY12 gene polymorphisms and higher risks of composite ischemic events for coronary artery disease patients treated with clopidogrel. [review] PMID: 29510176
    10. CLEC-2 and P2Y12 are required for CpG ODN-induced platelet activation and thrombosis, and might be targeted to prevent adverse events in patients at risk. PMID: 28296036
    11. miR-223, miR-26b, miR-126 and miR-140 are expressed at a lower level in platelets and megakaryocytes in type 2 diabetics causing up-regulation of P2RY12 and SELP mRNAs that may contribute to adverse platelet function. PMID: 27975100
    12. The DHA - naringenin hybrid presented triple antiplatelet activity simultaneously targeting PAR-1, P2Y12 and COX-1 platelet activation pathways PMID: 28844979
    13. The results suggest that P2Y12 is a useful marker for the identification of human microglia throughout the lifespan. Moreover, P2Y12 expression might help to discriminate activated microglia and infiltrating myeloid cells from quiescent microglia in the human CNS. PMID: 27862351
    14. P2RY12, the gene related to thrombogenesis was differentially expressed between the left atrium and right atrium in Sinus rhythm and Atrial fibrillation. Therefore, the changes in the expression of these genes were likely involved in the pathophysiology of AF-related thrombus formation. PMID: 27494721
    15. Abnormalities of P2Y12 receptor include congenital deficiencies or high activity in diseases like diabetes mellitus and chronic kidney disease, exposing such patients to a prothrombotic condition. (Review) PMID: 27628007
    16. Data suggest that PAR4 and P2Y12 heterodimer internalization/endocytosis is required for beta-arrestin-2 recruitment to endosomes and up-regulation of Akt signaling; activation of PAR4 but not of P2Y12 drives internalization of the PAR4-P2Y12 heterodimer. (PAR4 = protease-activated receptor 4; P2Y12 = purinergic receptor P2Y, G-protein coupled, 12 protein; Akt = proto-oncogene protein c-akt) PMID: 28652403
    17. Studies indicate that purinergic receptor P2Y12 (P2Y12 receptor) gene C34T and G52T polymorphism might be a risk factor for the poor response to the platelet in patients on clopidogrel therapy. PMID: 28791856
    18. studies describe 2 novel modes of action of ticagrelor, inhibition of platelet ENT1 and inverse agonism at the P2Y12R that contribute to its effective inhibition of platelet activation. PMID: 27694321
    19. apart from the established association of the CYP2C19 *2 and *3 LOF alleles with high on-treatment platelet reactivity (HTPR), haplotypes of P2RY12 rs6798347, rs6787801, rs6801273, and rs6785930 rather than rs2046934 (T744C) that related to pharmacodynamics of clopidogrel in patients with ACS were independently associated with HTPR PMID: 28070995
    20. The present report illustrates an update of dysfunctional platelet P2Y12R mutations diagnosed with congenital lifelong bleeding problems. [review] PMID: 27487748
    21. aim of this study was to evaluate the effects of platelet receptor gene (P2Y12, P2Y1) and glycoprotein gene (GPIIIa) polymorphisms, as well as their interactions, on antiplatelet drug responsiveness and clinical outcomes in patients with acute MIS PMID: 28091702
    22. The Conundrum of Platelet P2Y12 Inhibition in ST-Segment Elevation Myocardial Infarction. PMID: 27795489
    23. P2Y12R gene rs2046934 C>T and rs3732759 A>G polymorphisms might be associated with the risk of coronary artery disease and the efficacy of clopidogrel treatment for CAD. PMID: 27566695
    24. No association was found in genotype frequencies of P2Y12 and responsiveness to clopidogrel in coronary heart disease patients of Han ethnicity. PMID: 27488401
    25. P2Y12 inhibitor monotherapy and dual antiplatelet therapy inhibit hemostatic system activation to a comparable extent in healthy volunteers. PMID: 26663880
    26. In the presence of loss of function C34T polymorphism of P2Y12 receptor, smoking is associated with increased adverse cardiovascular outcome in coronary artery disease patients. PMID: 26950170
    27. These data strongly suggest that P2Y12 may represent an important pharmacological target for the treatment of patients with allergic bronchial asthma. [review] PMID: 25579761
    28. Report appropriate P2Y12 inhibitor regimen to prevent increased bleeding risk and maintain antiplatelet efficacy in East Asian patients with acute coronary syndrome. in Korean patients PMID: 26354056
    29. Baseline platelet aggregation was increased in carriers of the common alleles of P2Y12 SNPs rs1907637, rs2046934, and rs6809699 and rs6787801 TC heterozygotes. PMID: 26083990
    30. The ratio of ADP- to TRAP-induced platelet aggregation quantifies P2Y12-dependent platelet inhibition independently of the platelet count in contrast to conventional ADP-induced aggregation. PMID: 26885820
    31. Synergistic inhibition of both P2Y1 and P2Y12 adenosine diphosphate receptors by GLS-409 immediately attenuates platelet-mediated thrombosis and effectively blocks agonist-stimulated platelet aggregation irrespective of concomitant aspirin therapy. PMID: 26743169
    32. PON1, P2Y12 and COX1 polymorphisms were associated with poorer vascular outcomes in patients with extracranial or intracranial stents. PMID: 26870959
    33. In non-ST elevation acute coronary syndrome patients undergoing PCI a loading dose of ticagrelor or prasugrel given during the procedure provides optimal P2Y12-ADP receptor blockade in 2 h and maximal inhibition within 4 h. PMID: 26311415
    34. While there is increasing evidence for the cancer-protective effect of aspirin, this study suggests P2Y12 inhibition may also play a role. PMID: 26353776
    35. Establish a reliable antiplatelet profile of SAR216471, and support its potential use in clinical practice as an alternative to currently available P2Y12 receptor antagonists. PMID: 25064036
    36. 2 functional single nucleotide polymorphisms of PON1 gene (rs662 and rs854560) and 3 variants of the P2RY12 gene (rs2046934, rs6798347, rs6801273) in samples pooled from average Hungarian Roma and Hungarian population samples, were investigated. PMID: 25297118
    37. coexisting polymorphisms of CYP3A5*3 and 2C19*2, but not P2Y12*1, play an important role in the variability of clopidogrel's curative effect PMID: 25730082
    38. ADP stimulation of P2Y12 led to cAMP decrease that, in turn, caused changes in phospholipase C phosphorylation by protein kinase A, increase in cytoplasmic calcium level and, consequently, PS+ platelet formation PMID: 26391841
    39. Leukotriene E4 may play some important roles in allergic mucus secretion partially via activation of P2Y12 receptor PMID: 25838093
    40. the distribution of the ABCB1, CYP3A5, CYP2C19, and P2RY12 gene polymorphisms distinguishes to the Mexican Mestizos population from other ethnic groups. PMID: 25106522
    41. Experiments reveal a surmountable and competitive mode of antagonism of ticagrelor at P2Y12 -receptors activated by either the natural agonist ADP or the synthetic agonist 2-methylthio-ADP. PMID: 25186974
    42. This is the first study to demonstrate that the genetic polymorphisms of P2RY12 can affect platelet and eosinophil activation in patients with aspirin-exacerbated respiratory disease after aspirin exposure. PMID: 25778862
    43. this is the first study to report that PJ34 could act via a competitive P2Y(12) antagonism. PMID: 25329809
    44. Our findings suggest that the regulation of gpiibiiia and P2Y12 levels could be clinically useful to activate platelets to reach hemostasis. PMID: 25247182
    45. The findings of this study suggest a potential association between P2Y12-receptor H2/H2 carriers and reduced platelet function mediated by TRAP in healthy volunteers. PMID: 24510678
    46. study reports robust involvement of P2Y12R in inflammatory pain: anti-hyperalgesic effect of P2Y12R antagonism could be mediated by the inhibition of both central and peripheral cytokine production and involves alpha7-receptor mediated efferent pathwaysefferent pathways PMID: 24971933
    47. Two patients with bleeding diathesis had dysfunctional platelet P2Y12 receptor for ADP, attributable to homozygous His187Gln mutation. PMID: 25428217
    48. thrombin activates the mTORC1 pathway in human platelets through PKC-mediated ADP secretion and subsequent activation of P2Y(12), in a manner largely independent of the canonical PI3 kinase/Akt pathway PMID: 24612393
    49. analysis of a P2Y12 receptor mutation and a function-reducing polymorphism in protease-activated receptor 1 in a patient with chronic bleeding [case report] PMID: 24612435
    50. The evidence from our study indicates that P2Y12 methylation may bring new hints to elaborate the pathogenesis of CR. PMID: 24745016

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  • 相关疾病：
    Bleeding disorder, platelet-type 8 (BDPLT8)
  • 亚细胞定位：
    Cell membrane; Multi-pass membrane protein.
  • 蛋白家族：
    G-protein coupled receptor 1 family
  • 组织特异性：
    Highly expressed in the platelets, lower levels in the brain. Lowest levels in the lung, appendix, pituitary and adrenal gland. Expressed in the spinal cord and in the fetal brain.
  • 数据库链接：

    HGNC: 18124

    OMIM: 600515

    KEGG: hsa:64805

    STRING: 9606.ENSP00000307259

    UniGene: Hs.591281