Recombinant Human P2Y purinoceptor 12(P2RY12)

Code CSB-CF861997HU
Size US$3452
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Product Details

Target Names P2RY12
Uniprot No. Q9H244
Alternative Names ADP glucose receptor ; ADP-glucose receptor; ADPG R; ADPG-R; ADPGR ; BDPLT8; G protein coupled receptor SP1999; Gi coupled ADP receptor HORK 3; Gi coupled ADP receptor HORK3; HORK 3; HORK3; P2RY 12; P2RY12; P2T(AC); P2Y 12; P2Y purinoceptor 12; P2Y(12)R; P2Y(AC); P2Y(ADP); P2Y(cyc); P2Y12; P2Y12 platelet ADP receptor; P2Y12_HUMAN; Platelet ADP receptor ; Purinergic receptor P2RY12; Purinergic receptor P2Y G protein coupled 12; Purinergic receptor P2Y12; Putative G protein coupled receptor ; SP 1999; SP1999
Species Homo sapiens (Human)
Source in vitro E.coli expression system
Expression Region 1-342
Target Protein Sequence MQAVDNLTSAPGNTSLCTRDYKITQVLFPLLYTVLFFVGLITNGLAMRIFFQIRSKSNFI IFLKNTVISDLLMILTFPFKILSDAKLGTGPLRTFVCQVTSVIFYFTMYISISFLGLITI DRYQKTTRPFKTSNPKNLLGAKILSVVIWAFMFLLSLPNMILTNRQPRDKNVKKCSFLKS EFGLVWHEIVNYICQVIFWINFLIVIVCYTLITKELYRSYVRTRGVGKVPRKKVNVKVFI IIAVFFICFVPFHFARIPYTLSQTRDVFDCTAENTLFYVKESTLWLTSLNACLDPFIYFF LCKSFRNSLISMLKCPNSATSLSQDNRKKEQDGGDPNEETPM
Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
Protein Length full length protein
Tag Info N-terminal 10xHis-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 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 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.
Gene References into Functions
  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
  51. In patients on maintenance prasugrel therapy exposed to a reloading dose (30 or 60 mg) of prasugrel, in vitro cangrelor is associated with further platelet P2Y12 receptor inhibitory effects. PMID: 24630878
  52. Data indicate that SAR216471 is a potent, highly selective, and reversible P2Y purinoceptor 12 (P2Y12) receptor antagonist and by far the most potent inhibitor of ADP-induced platelet aggregation among the P2Y12 antagonists. PMID: 25075638
  53. Among patients with stable coronary artery disease, smokers have more P2Y12 receptor binding than nonsmokers and have a higher degree of clopidogrel-mediated platelet inhibition. PMID: 24357254
  54. P2Y1 and P2Y12 genes were polymorphic in a Korean population; 3 intronic P2Y12 polymorphisms (i-139C>T, i-744T>C, i-801insA) were in complete linkage disequilibrium but not with the c.52C>T polymorphism; platelet aggregation in response to ADP associated with c.52C>T polymorphism but not with the 3 intronic polymorphisms or the P2Y1 c.1622A>T polymorphism PMID: 23849096
  55. PAR4-P2Y12 association supports arrestin-mediated sustained signaling to Akt. PMID: 24723492
  56. 2.6 A resolution crystal structure of human P2Y12R in complex with a non-nucleotide reversible antagonist, AZD1283 PMID: 24670650
  57. structures of P2Y12R in complex with agonist 2-methylthio-adenosine-5'-diphosphate (2MeSADP, analogue of endogenous agonist ADP) at 2.5 A resolution, and corresponding ATP derivative 2-methylthio-adenosine-5'-triphosphate (2MeSATP) at 3.1 A resolution PMID: 24784220
  58. Platelet ADP and AA receptor inhibition is a prominent early feature of coagulopathy in traumatic brain injury in humans and rats and is linked to the severity of brain injury in patients with isolated head trauma. PMID: 24747445
  59. The data demonstrate nucleoside triphosphates in general act as P2Y12 receptor antagonists and antagonise ADP-, collagen-, and epinephrine-induced platelet aggregation. PMID: 24071464
  60. In our cohort, a pre-procedure P2Y12 reaction units value was the strongest independent predictor of all and major perioperative thromboembolic and hemorrhagic complications after Pipeline Embolization Device PMID: 23314576
  61. Bradykinin induces ATP release from human subcutaneous fibroblasts via connexin and pannexin-1-containing hemichannels leading to calcium mobilization through the cooperation of B2 and P2Y12 receptors. PMID: 24047499
  62. the study revealed no association between the risk of clopidogrel resistance and the presence of polymorphic variants of platelet receptor genes P2RY12 and GpIIIa. PMID: 24437181
  63. Data indicate that the ADP(PGE1) method is a reliable test for monitoring P2Y12 receptor inhibition by platelet aggregation. PMID: 23844259
  64. analysis of endosomal sorting of a novel P2Y12 purinoreceptor mutant PMID: 23387322
  65. Coexisting polymorphisms of of CYP2C19 and P2Y12 affected clopidogrel responsiveness and clinical outcome more than single polymorphism in Chinese patients with acute coronary syndrome undergoing percutaneous coronary intervention. PMID: 23506580
  66. Platelet P2Y12 function also appears to be inversely correlated with JAK2V617F allele burden. This compromised P2Y12 function may be a novel mechanism for the bleeding tendency associated with extreme thrombocytosis in MPN. PMID: 23751441
  67. This review aims to provide an overview on the state of the art P2Y12 receptor directed inhibition in ACS patients with a focus on patients undergoing a coronary stenting procedure. [review] PMID: 23299202
  68. study elicited an association between the T744C polymorphism of the P2Y12 ADP receptor gene and platelet reactivity PMID: 23751603
  69. In this review, we provide a brief but comprehensive report on P2Y(12), its role on platelet thrombus formation, and the targeting of this receptor as an intervention for cardiovascular disease PMID: 23054651
  70. Epac agonist 8-pCPT-2'-O-Me-cAMP affects P2Y12 receptors in blood platelets PMID: 23850619
  71. Characterized the expression of P2Y12 receptor in breast cancer cell lines and evaluate its role in enhancing the cytotoxic effects of cisplatin. Observed a significant upregulation in P2Y12 expression in 4T1 breast cancer cell line with cisplatin. PMID: 23568163
  72. RT-PCR analysis of total RNA extracted from human nasal turbinate, primary cultured human nasal epithelial cells and nasal vascular endothelial cells demonstrated the expression of P2Y12 receptor mRNA. PMID: 23612493
  73. Clopidogrel resistance was not associated with ADP receptor P2Y1 and P2Y12 gene polymorphisms. PMID: 22721490
  74. Our results suggest that 18C > T polymorphism of the P2RY12 gene may be an independent predictor of pharmacological response to clopidogrel. PMID: 23940995
  75. Demonstrate that P2Y(12) activation protects platelets from apoptosis via PI3k-dependent Bak/Bax inactivation. PMID: 23140172
  76. The platelet P2Y12 receptor contributes to granule secretion through Ephrin A4 receptor. PMID: 22273509
  77. A novel pathway is described for testosterone regulation of P2Y12 expression in a megakaryocytic DAMI cell line. PMID: 22746349
  78. Data indicate that single nucleotide polymorphisms (SNPs) in P2RY1 and P2RY12 are associated with on-aspirin platelet reactivity in patients with coronary artery disease (CAD). PMID: 22574824
  79. These studies indicate putative roles of the P2Y(12) receptor in inflammatory states and diseases of the brain, lung, and blood vessels--{REVIEW} PMID: 22528678
  80. reactivity, as assessed by post-treatment P2Y12 mediated reactivity, is heightened after thrombolytic therapy during STEMI management. PMID: 22704077
  81. Data describe a novel function of ARF6 in the internalization of P2Y purinoceptors and demonstrate the integral importance of this small GTPase upon platelet ADP receptor function. PMID: 22916275
  82. in acute coronary syndrome diabetes mellitus patients undergoing PCI, the extent of P2Y12 inhibition by clopidogrel is not related to glycaemic control but is related to body weight and inflammatory status as assessed by the WBC PMID: 22740070
  83. Combined blockade of P2Y12, P2Y1 and PI3-kinase p110beta fully prevents platelet and leukocyte activation during hypothermic extracorporeal circulation. PMID: 22701645
  84. T744C P2RY12 polymorphism did not significantly affect the risk of VTE in the Korean population. PMID: 22275393
  85. In patients undergoing nonurgent percutaneous coronary intervention intravenous/oral P2Y12 inhibitor elinogrel did not significantly increase thrombolysis in myocardial infarction or bleeding. PMID: 22647518
  86. increased fractalkine levels are associated with decreased endogenous platelet inhibition and impaired response to P2Y12 inhibition with clopidogrel. PMID: 22652599
  87. Findings suggest a novel model by which arrestin can serve as an adaptor to promote NHERF1 interaction with a GPCR to facilitate effective NHERF1-dependent receptor internalization. PMID: 22610101
  88. Increased residual platelet reactivity assessed by VerifyNow P2Y12 assay is related to post-discharge CV events in subjects with AMI. Prognostic significance is attenuated in patients with stable coronary disease after PCI. PMID: 22440490
  89. The P2RY12 variants were associated with lung function in a large family-based asthma cohort. House dust mite exposure caused significant gene-by-environment effects PMID: 22010907
  90. P2Y(12)-receptor gene variation has an effect on outcome of clopidogrel-treated patients undergoing elective coronary stent implantation PMID: 22159428
  91. SELP Pro715 allele is linked to low levels of sP-selectin, and both are associated with decreased P2Y12 ADP receptor reactivity in patients on clopidogrel therapy PMID: 21497813
  92. This study confirmed significant inter-ethnic differences in CYP3A5 and P2Y12 frequencies between Iranians and other ethnic groups. PMID: 21153923
  93. functional interaction of A2A and P2Y12 receptors on P2Y1 receptor PMID: 22079667
  94. P2Y(12)R function is compromised after deletion or mutation of the 4 amino acids at the extreme C-terminus of this receptor (ETPM), a putative postsynaptic density 95/disc large/zonula occludens-1 (PDZ)-binding motif. PMID: 21937696
  95. In diabetes mellitus patients undergoing percutaneous coronary intervention, impaired inhibition of P2Y12 by clopidogrel is an independent predictor of cardiac death. PMID: 21524751
  96. The P2Y12 receptor, activated by ADP, plays a central role in platelet activation and thrombus formation. Thus, the P2Y12 receptor has been an effective target for antithrombotic drugs. (Review) PMID: 21231822
  97. P2Y12 single-nucleotide polymorphisms and haplotypes revealed a significant association between P2Y12 haplotype, denoted H3, and an increase in the ADP-induced platelet aggregation response relative to that for the reference haplotype H1. PMID: 21216445
  98. central role played by P2Y in platelet thrombus formation (review) PMID: 20966167
  99. vasodilator-stimulated phosphoprotein is phosphorylated in patients with genetic defects of the platelet P2Y(12) receptor for ADP PMID: 20695985
  100. clopidogrel active metabolite formation potentiation by rifampicin leads to greater P2Y12 receptor blockade and inhibition of platelet aggregation after clopidogrel PMID: 20492465

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Involvement in disease Bleeding disorder, platelet-type 8 (BDPLT8)
Subcellular Location Cell membrane, Multi-pass membrane protein
Protein Families G-protein coupled receptor 1 family
Tissue Specificity 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.
Database Links

HGNC: 18124

OMIM: 600515

KEGG: hsa:64805

STRING: 9606.ENSP00000307259

UniGene: Hs.591281

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