Recombinant Human Endothelin-1 receptor(EDNRA)

Code CSB-CF007403HU
Size US$3555Purchase it in Cusabio online store
(only available for customers from the US)
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  • (Tris-Glycine gel) Discontinuous SDS-PAGE (reduced) with 5% enrichment gel and 15% separation gel.

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Product Details

Purity Greater than 90% as determined by SDS-PAGE.
Target Names EDNRA
Uniprot No. P25101
Research Area Signal Transduction
Alternative Names Ednra; EDNRA_HUMAN; Endothelin 1 receptor precursor; Endothelin 1 specific receptor; Endothelin A receptor; Endothelin ET A receptor; Endothelin receptor ET1 specific type; Endothelin receptor subtype A; Endothelin receptor type A; Endothelin-1 receptor; ET A; ET-A; ETA; ETA R; ETA-R; ETAR; ETRA; G protein coupled receptor; hET AR; hET-AR; MFDA
Species Homo sapiens (Human)
Source in vitro E.coli expression system
Expression Region 21–427aa
Target Protein Sequence DNPERYSTNLSNHVDDFTTFRGTELSFLVTTHQPTNLVLPSNGSMHNYCPQQTKITSAFKYINTVISCTIFIVGMVGNATLLRIIYQNKCMRNGPNALIASLALGDLIYVVIDLPINVFKLLAGRWPFDHNDFGVFLCKLFPFLQKSSVGITVLNLCALSVDRYRAVASWSRVQGIGIPLVTAIEIVSIWILSFILAIPEAIGFVMVPFEYRGEQHKTCMLNATSKFMEFYQDVKDWWLFGFYFCMPLVCTAIFYTLMTCEMLNRRNGSLRIALSEHLKQRREVAKTVFCLVVIFALCWFPLHLSRILKKTVYNEMDKNRCELLSFLLLMDYIGINLATMNSCINPIALYFVSKKFKNCFQSCLCCCCYQSKSLMTSVPMNGTSIQWKNHDQNNHNTDRSSHKDSMN
Note: The complete sequence including tag sequence, target protein sequence and linker sequence could be provided upon request.
Mol. Weight 49.9kDa
Protein Length Full Length of Mature Protein
Tag Info C-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 endothelin-1. Mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of binding affinities for ET-A is
Gene References into Functions
  1. No link between EDNRA rs5335 and large artery stroke risk in a Ukrainian population was found. PMID: 29849817
  2. miR200c regulates the proliferation, apoptosis and invasion of gastric carcinoma cells through the downregulation of EDNRA expression. PMID: 29286062
  3. Presence of SST5, CXCR4 and ETA on tumor cells and of SST3, CXCR4 and ETA on microvessels gradually increased from grade II to grade IV tumors. PMID: 29696364
  4. There is no association between the C+70G polymorphism of the EDNRA gene and the development of ischemic atherothrombotic stroke. PMID: 29064794
  5. endothelin-A receptor-activated ABCB1 expression has a role in nintedanib resistance in FGFR1-driven small cell lung cancer PMID: 27367030
  6. Endothelin-1 possesses an anti-apoptotic effect in vascular endothelial cells and this effect is mediated, to a great extent, via the activation of EDNRB, with a minor contribution via activation of EDNRA. PMID: 28732172
  7. ETA and ETB receptors are present in human haemorrhoids with ETB receptors predominating PMID: 28095606
  8. ETAR stimulation acted via downstream G-protein Galphaq/11 and Rho GTPase to suppress the Hippo pathway, thus leading to YAP/TAZ activation, which was required for ETAR-induced tumorigenesis. Overall, these results indicate a critical role of the YAP/TAZ axis in ETAR signaling PMID: 28249901
  9. Data show that endothelin A receptor drives invadopodia function by direct interaction of beta-arrestin-1 (beta-arr1) with Rho guanine nucleotide exchange factor (GEF) 11 protein (PDZ-RhoGEF). PMID: 26522724
  10. In control arteries, ETAR was expressed by vascular smooth muscle cells in the media whereas ETBR was hardly detected. In giant cell arteritis, both ETAR and ETBR receptors were expressed by alphaSMA-positive cells at the intima-media border. Endothelial cells and inflammatory cells also expressed both ET receptors. PMID: 28606962
  11. Data suggest that TNFalpha (tumor necrosis factor-alpha) induces proliferation of airway smooth muscle cells via ET1 (endothelin-1), GM-CSF (granulocyte-macrophage colony-stimulating factor), and IL6 (interleukin 6) signaling; ET1 induces cell proliferation via ETAR (endothelin receptor type A); ETBR (endothelin receptor type B) is up-regulated by TNFalpha and appears to mediate ET1 effects on cell proliferation. PMID: 27422754
  12. presence of ET-1 receptors in the chronic thrombus in proximal CTEPH suggests ET-1 could act not only on the distal vasculopathy in the unobstructed vessels but may also stimulate smooth muscle cell proliferation within chronic clot PMID: 26874031
  13. Data show that auriculo-condylar syndrome (ACS)-associated mutations in G protein subunit alpha i3 (GNAI3) produce dominant-negative Galpha(i3) mutant proteins that couple to endothelin type A receptor (ET(A)R). PMID: 27072656
  14. Patients with lung fibrosis and patients with high modified Rodnan skin score showed a reduced endothelin 1 Type A receptor (ETAR)/ETBR ratio. PMID: 26773103
  15. High ETAR expression is associated with ovarian carcinoma. PMID: 26675258
  16. Data show that macitentan interferes with the profibrotic action of transforming growth factor-beta (TGF-beta), blocking the endothelin receptor type A (ET-1 receptor) portion of the ET-1/TGF-beta receptor complex. PMID: 26357964
  17. Ednra, encoding Endothelin receptor A (ETA)-the target of Endothelin 1 (ET-1)-was significantly increased in Systemic Capillary Leak Syndrome blood-outgrowth endothelial cells compared to healthy controls. PMID: 26176954
  18. Genebased analyses revealed associations of the EDNRA gene with longitudinal Blood Pressure phenotypes, associations with essential hypertension, Blood Pressure salt sensitivity, preeclampsia, or preclinical stages of atherosclerosis. PMID: 25424718
  19. Endothelin receptor A was detected in all patients with squamous cell carcinoma and psoriasis, with a higher frequency and grade of expression than controls and basal cell carcinoma. PMID: 25946671
  20. The aim was to quantify the density of ETA and ETB receptors in cardiopulmonary tissue from pulmonary arterial hypertension patients and the monocrotaline (MCT) rat. PMID: 24582810
  21. findings suggest a role for agonistic autoantibodies-induced activation of immune cells mediated by the AT1R and the ETAR in the pathogenesis or even the onset of systemic sclerosis PMID: 24612997
  22. Polymorphisms of EDNRA have been associated with the development of group I pulmonary hypertension, dilated cardiomyopathy and essential hypertension PMID: 24570333
  23. Mutations in the endothelin receptor type A cause mandibulofacial dysostosis with alopecia. PMID: 25772936
  24. significant single nucleotide polymorphism associations with birth weight near coding regions for two genes involved in oxygen sensing and vascular control, PRKAA1 and EDNRA, respectively, were identified. PMID: 25225183
  25. no significant association between EDNRA (C+70G, G-231A) allele and Hashimoto's thyroiditis in Turkish population; this polymorphism relates to decreased risk for early disease onset PMID: 24815860
  26. Data show that upon endothelin-1 (ET-1) stimulation, ET type A receptor (ETAR) is recycled back to plasma membrane, whereas ET type B receptor (ETAR) is targeted to lysosome for degradation. PMID: 25381251
  27. Suggest a functional link between endothelin receptor autoantibody formation and down-regulated midkine serum levels, that may be relevant in the pathogenesis of clinically relevant peripheral artery occlusive disease. PMID: 25056169
  28. genetic association study in population in India: Data suggest that (in addition to mutations in cystic fibrosis transmembrane conductance regulator) an SNP in EDNRA (rs5335) is associated with congenital absence of vas deferens in population studied. PMID: 24958810
  29. our findings reveal the existence of a novel mechanism by which ETAR/beta-arr1 signaling is integrated with the Wnt/beta-catenin pathway to sustain chemoresistance in epithelial ovarian cancer, and they offer a solid rationale for clinical evaluation PMID: 25377471
  30. no association between Graves' disease and genetic polymorphism PMID: 24291390
  31. EDNRA mRNA expression was increased in reflux esophagitis and Barrett's esophagus compared to controls. PMID: 23384184
  32. ETAR and CXCR4 expression levels are potential prognostic biomarkers in nasopharyngeal carcinoma patients. PMID: 23987636
  33. Mutation of EDNRA is involved in ACTH-independent macronodular adrenal hyperplasia. PMID: 23754170
  34. We used this sample of 250 surgical patients to describe the distribution of ET-1, ETA and ETB polymorphisms in the aneurysmal subarachnoid hemorrhage population. PMID: 22997346
  35. ETAR overexpression promoted colon cancer liver metastases. PMID: 23818293
  36. Report serum levels ETAR autoantibodies in peripheral arterial disease. PMID: 24627317
  37. the positive correlation between ET-1 and ETAR in lesional compared with perilesional normal epidermis suggest an important role of this receptor in vitiligo. PMID: 23683481
  38. Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation. PMID: 24064210
  39. The presence ETr-A and ETr-B in rheumatic mitral valves suggests its interaction with the system of c endothelins, particularly ETr-B detected in a greater proportion, which could explain the lack of expression of endothelin in rheumatic mitral valve. PMID: 23515723
  40. Genetic deletion of a nephron-specific endothelin A receptor causes very modest fluid retention that does not alter arterial pressure, nor doea it play a major role in regulating sodium excretion or systemic hemodynamics. PMID: 23217151
  41. The mRNA expressions of endothelin A and B receptors and endothelin-1 are significantly increased in failed Fontan patients. PMID: 21356562
  42. A significant difference existed between migraineurs & controls with AA genotype vs. AG+GG. Pooled relative risk with fixed effect was 4.04. This meta-analysis suggests a significant association between EDNRA -231G>A polymorphism and migraine. PMID: 23058564
  43. Right ventricular hypertrophy myocardial endothelin type A receptor level is increased compared to nonhypertrophied right ventricular endothelin receptor level. PMID: 23233754
  44. Findings suggest a potential link between specific genotypes in the ednra gene and susceptibility to pulmonary arterial hypertension. PMID: 21773759
  45. Both endothelin A and B receptors were reduced in pulmonary arterial hypertension, particularly type B, and type B signaling through protein kinases was markedly reduced in vascular smooth cells with a mutation in bone morphogenetic protein receptor 2. PMID: 22688668
  46. endothelin A receptor and epidermal growth factor receptor signaling converge on beta-catenin to promote ovarian cancer metastasis PMID: 22480520
  47. ETB receptors predominated in normal human liver and displayed the highest ratio (ETB:ETA 63:47) compared with other peripheral tissues; liver ETB expression was upregulated in cirrhosis (ETB:ETA 83:17) PMID: 22365955
  48. Expressed recombinant ET(A) as a fusion protein with phi6 p9 envelope protein. The purified protein showed specific binding to ET-1 and the alpha subunit of G(q) protein. PMID: 22561246
  49. SNP, rs6842241, near EDNRA at chromosome 4q31.22 (combined P-value = 9.58 x 10(-9); odds ratio = 1.25), was found to be significantly associated with intracranial aneurysm PMID: 22286173
  50. Data show that optical imaging with a fluorescent ET(A)R tracer allows the noninvasive imaging of tumor-associated ET(A)R expression in vivo. PMID: 22510270
  51. four TRPC isoforms, TRPC3, TRPC5, TRPC6, and TRPC7, can function as endothelin type A receptor-operated Ca2+ channels. PMID: 22129540
  52. Results demonstrated significant association of IA with rs6841581 on chromosome 4q31.23, immediately 5' of the endothelin receptor type A with P = 2.2 x 10(-8) [odds ratio (OR) = 1.22, PPA = 0.986]. PMID: 22106312
  53. Single nucleotide polymorphisms in EDNRA gene is associated with breast cancer. PMID: 21424380
  54. ET1 induced calcium responses are only mediated by endothelin A receptors, possibly due to sub-threshold endothelin B receptor expression. PMID: 21515378
  55. Data show that blockade of ET(A)R-driven EMT can overcome chemoresistance and inhibit tumor progression, improving the outcome of EOC patients' treatment. PMID: 21220476
  56. Data show that EDNRA/H323H polymorphism is a novel and independent prognostic marker, which may help identify patient subgroups at high risk for poor disease outcome. PMID: 21487064
  57. the role of EDNRA -231 G>A and APOE HhaI polymorphism for a possible association with migraine PMID: 21453125
  58. Study of a novel enhanced green fluorescent protein (EGFP) reporter (Ednra) transgenic mouse line enables visualization of placode-derived inner ear sensory cell lineage. PMID: 20963824
  59. Our results show additional findings for a role of endothelin receptor type A as a susceptibility factor for migraine without aura PMID: 20964792
  60. Expression of ETA receptor in normal endometrium and decidua is regulated by homeobox protein A10 (HOXA10). PMID: 20371740
  61. Studies indicate that understanding the mechanisms of how cigarette smoke causes up-regulation of endothelin receptors in the vasculature and airways may provide new strategies for treatment of cigarette smoke-associated cardiovascular and lung diseases. PMID: 21057729
  62. Lack of ET(A)R expression may be an independent negative marker for recurrence-free survival in bladder cancer. PMID: 18945538
  63. Endothelin receptor type A polymorphism rs 5335 may be associated with congenital bilateral absence of vas deferens penetrance. PMID: 20100616
  64. The results suggested that during the luteal phase, ET(A) and ET(B) receptors participate in contractile effects of endothelins on isthmic segment of fallopian tubes, probably regulating the length of time the oocyte remains in the ampulla PMID: 20401344
  65. A significant association between EDNRA 3'-untranslated region (UTR) variant rs5335 and pulmonary function, was demonstrated. PMID: 20028935
  66. SNPs as susceptibility factors for obstructive sleep apnea syndrome PMID: 20083432
  67. Both ET(A)R and ET(B)R are present in lung carcinomas but at different levels, according to the histological type of tumor. PMID: 20043107
  68. these results suggest that the amount of Jab1 bound to ETR regulates the degradation rate of ET(A)R and ET(B)R by modulating ubiquitination of these receptors, leading to changes in ET(A)R and ET(B)R levels. PMID: 20034471
  69. Selective endothelin A-receptor blockade attenuates coronary microvascular dysfunction after coronary stenting in patients with type 2 diabetes. PMID: 19898645
  70. The endothelin system plays a role in the complex pathophysiology of idiopathic dilated cardiomyopathy. PMID: 11601839
  71. The vasoconstrictor effect of endothelin-1 in small resistance arteries of normotensive subjects and, in part, also in hypertensive patients is mediated by ET(A) receptors, while ET(B) receptors play a minor role, if any PMID: 11930911
  72. endothelin-1 increased diastolic distensibility of acutely loaded myocardium and this effect was mediated by endothelin (A) receptors and Na(+)/H(+) exchanger activation PMID: 12595285
  73. In autosomal-dominant polycystic kidney disease, neo-expression of ETA receptors has been found overlying glomeruli and cysts and markedly increased in medium-sized renal arteries. PMID: 12629276
  74. Data show that in a human Kaposi sarcoma cell line, blockade of endothelin receptors A and B blocked the endothelin-1-induced increase in secretion and activation of matrix-metalloproteinases. PMID: 12875994
  75. ET(A)R expression in breast cancer corrrelated with favorable prognosis. PMID: 14519635
  76. It is clear from the present data for lung fibroblasts that for both stimulated and unstimulated states of ETA receptors, there exist multiple covalent forms differing in the number and location of sites of posttranslational modifications. PMID: 14636059
  77. Endothelin ETA receptor mRNA levels are significantly higher in arteries from patients with ischemic heart disease as compared to congestive heart failure and controls. PMID: 14729387
  78. ET-1 induces collagen matrix contraction through the ETA, but not the ETB, receptor PMID: 15047866
  79. Endothelin receptor type A was significantly down-regulated in papillary renal tumor specimens PMID: 15139053
  80. endothelin A receptor regulates cell migration through the Cdc42-dependent c-Jun N-terminal kinase pathway and is mediated by Nck1 PMID: 15187089
  81. Recycling of ET(A) receptor is mediated by a motif with the structural characteristics of an internal PDZ ligand. This structural motif may represent a more general principle of endocytic sorting of G protein-coupled receptors. PMID: 15713850
  82. Examine therapeutic targeting of the endothelin-A receptor in human ovarian carcinoma. Report that efficacy of cytotoxic agents is markedly enhanced by co-administration with atrasentan. PMID: 15838262
  83. Compared kidney endothelin-A and endothelin-B receptor distribution visualized by radioligand binding versus immunocytochemical localization using subtype selective antisera. PMID: 15838285
  84. Results suggest that [F]-SB209670 binds rapidly and primarily to endothelin-A receptors in the heart. PMID: 15838315
  85. Report pharmacological characterization of YM598, a selective endothelin-A receptor antagonist. PMID: 15838329
  86. Targeting the endothelin-A receptor, but not the endothelin-B receptor, may be a valid tool in the therapy of cervical carcinoma. PMID: 15838364
  87. Report the effects of the selective ET(A) receptor antagonist, sitaxsentan sodium, in a patient population with pulmonary arterial hypertension that meets traditional inclusion criteria of previous pulmonary arterial hypertension trials PMID: 15838366
  88. Endothelin-A receptor antagonism promotes decreased vasodilation but has no differential effect on coronary artery compliance in hypertensive patients. PMID: 15838367
  89. The polymorphism of EDNRA/C+70G may be related to NTG (normal tension glaucoma) risk factors. PMID: 15988412
  90. in human lung fibroblasts ET-1 exerts a profibrogenic action via an ET(A) receptor-dependent, MAPK-mediated induction of IL-11 release and cell proliferation PMID: 16149067
  91. Observations strongly suggest that the expression of ETA receptor is enhanced in neointimal smooth muscle cells at early stages after percutaneous coronary intervention injury in human coronary arteries. PMID: 16531800
  92. Reverse transcriptase-polymerase chain reaction analysis revealed mRNA the ETA receptor subtype in the human trigeminal ganglion. Immunocytochemistry revealed numerous cell bodies containing ETA proteins. PMID: 16816835
  93. endothelin receptor type A(ETR-A) is selectively up-regulated in placental tissue of delayed miscarriages as compared to normal pregnancies PMID: 16879994
  94. Associations between endothelin receptors A and B in aystemic ssclerosis subsets supports the role of endothelin and its receptors in the pathogenesis of this disease. PMID: 16947775
  95. ET receptors in pigment cells of vertebrate species were identified by RT-PCR assays, and the differential expression of the various subtypes in each species was compared by quantitative PCR. PMID: 16962346
  96. Polymorphism of EDNRA:c.*1222C > T was significantly associated with normal tension glaucoma. AA genotype of EDNRA:c.-231G > A polymorphism was associated with lower baseline intraocular pressure than in GG+GA genotype group. PMID: 16971893
  97. Endothelin receptor A has a role in progression of prostate cancer PMID: 16984730
  98. association of genetic variation with aortic pressure in patients with dilated cardiomyopathy PMID: 17198909
  99. No association between the -231 G > A polymorphism in the EDNRA gene and preeclampsia as well as any correlation with the main clinical features of the disorder were found. PMID: 17437213
  100. Hypoxia-induced breast carcinoma invasiveness was reduced by ETRA antagonist atrasentan. PMID: 17468950

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Involvement in disease Mandibulofacial dysostosis with alopecia (MFDA)
Subcellular Location Cell membrane, Multi-pass membrane protein
Protein Families G-protein coupled receptor 1 family, Endothelin receptor subfamily, EDNRA sub-subfamily
Tissue Specificity Isoform 1, isoform 3 and isoform 4 are expressed in a variety of tissues, with highest levels in the aorta and cerebellum, followed by lung, atrium and cerebral cortex, lower levels in the placenta, kidney, adrenal gland, duodenum, colon, ventricle and li
Database Links

HGNC: 3179

OMIM: 131243

KEGG: hsa:1909

STRING: 9606.ENSP00000315011

UniGene: Hs.183713

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