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  4. Recombinant Human Hydroxycarboxylic acid receptor 2 (HCAR2)

Recombinant Human Hydroxycarboxylic acid receptor 2 (HCAR2)

  • 货号：
    CSB-CF840573HU
  • 规格：
  • 来源：
    in vitro E.coli expression system
  • 其他：

产品详情

  • 基因名：
  • Uniprot No.：
  • 别名：
    HCAR2; GPR109A; HCA2; HM74A; NIACR1; Hydroxycarboxylic acid receptor 2; G-protein coupled receptor 109A; G-protein coupled receptor HM74A; Niacin receptor 1; Nicotinic acid receptor
  • 种属：
    Homo sapiens (Human)
  • 蛋白长度：
    full length protein
  • 表达区域：
    1-363
  • 氨基酸序列
    MNRHHLQDHFLEIDKKNCCVFRDDFIVKVLPPVLGLEFIFGLLGNGLALWIFCFHLKSWK SSRIFLFNLAVADFLLIICLPFLMDNYVRRWDWKFGDIPCRLMLFMLAMNRQGSIIFLTV VAVDRYFRVVHPHHALNKISNRTAAIISCLLWGITIGLTVHLLKKKMPIQNGGANLCSSF SICHTFQWHEAMFLLEFFLPLGIILFCSARIIWSLRQRQMDRHAKIKRAITFIMVVAIVF VICFLPSVVVRIRIFWLLHTSGTQNCEVYRSVDLAFFITLSFTYMNSMLDPVVYYFSSPS FPNFFSTLINRCLQRKMTGEPDNNRSTSVELTGDPNKTRGAPEALMANSGEPWSPSYLGP TSP
    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：
    Acts as a high affinity receptor for both nicotinic acid (also known as niacin) and (D)-beta-hydroxybutyrate and mediates increased adiponectin secretion and decreased lipolysis through G(i)-protein-mediated inhibition of adenylyl cyclase. This pharmacological effect requires nicotinic acid doses that are much higher than those provided by a normal diet. Mediates nicotinic acid-induced apoptosis in mature neutrophils. Receptor activation by nicotinic acid results in reduced cAMP levels which may affect activity of cAMP-dependent protein kinase A and phosphorylation of target proteins, leading to neutrophil apoptosis. The rank order of potency for the displacement of nicotinic acid binding is 5-methyl pyrazole-3-carboxylic acid = pyridine-3-acetic acid > acifran > 5-methyl nicotinic acid = acipimox >> nicotinuric acid = nicotinamide.
  • 基因功能参考文献：
    1. GPR109A may inhibit inflammatory cytokine production, induced by palmitic acid, by MIN6 cells possibly via inhibiting the Akt/mTOR signaling pathway. PMID: 29263047
    2. These results demonstrate that GPR109A is functionally expressed in both human and murine islet beta-cells. PMID: 27570060
    3. new insights into the G protein coupling profiles of the HCA receptors and the function of the receptor's C terminus PMID: 26656756
    4. These results suggest that the PKC pathway and PDGFR/EGFR transactivation pathway play important roles in HCA2-mediated Akt activation. PMID: 25375133
    5. Results suggest that the atypical motif asparaging-cysteine-systeine Asn(17)-Cys(18)-Cys(19) is crucial for the normal surface trafficking and function of hydroxycarboxylic acid receptor 2 protein hGPR109A. PMID: 25690651
    6. niacin, at a relatively low concentration, preserves the ability of HMVEC to form tubes under conditions of saturated fatty acid excess, and may elicit this effect through activation of GPR109A PMID: 25463108
    7. GPR109A expression is upregulated in blood and substantia nigra in Parkinson disease patients. PMID: 25329911
    8. The results of this study suggested that GPR109A signaling is associated with T2DM, playing a role in regulation of the inflammatory cytokines. PMID: 25361930
    9. the promiscuous activity exerted by niacin via both GPR109A and GPER may open new avenues towards a better understanding of the mechanisms involved in its biological action exerted in different pathophysiological conditions, including malignant diseases. PMID: 24662263
    10. Although its functional role is still unknown, HCA2 may be potentially involved in the pathogenesis of various retinopathies and may offer a new therapeutic target. PMID: 24215154
    11. GPR109A is a tumor suppressor in mammary gland. PMID: 24371223
    12. These studies provide key insights into mechanisms by which GPR109A may influence cholesterol efflux in macrophages. PMID: 23770183
    13. despite NA's anti-inflammatory effect on human macrophages, it has no effect on foam cells in reverse cholesterol transport; due to GPR109A down-regulation PMID: 23658787
    14. Review of the role of GPR109A and its downstream effects in the context of atherosclerosis and vascular inflammation, along with insights into strategy for future drug development. [Review Article] PMID: 23526298
    15. A sequence from residues 329 to 343 in the C-terminal tail of HCA plays a crucial role in keeping HCA in an inactive conformation. PMID: 22962331
    16. Nicotnic acid displays a range of effects that are lipoprotein-independent and potentially antiatherogenic. These effects are mediated by GPR109A. PMID: 22267479
    17. upon binding to niacin GPR109A receptors initially activate G(i), leading to dissociation of the Gbetagamma subunit from activated G(i), and subsequently induce ERK1/2 activation via two distinct pathways. PMID: 21768093
    18. In contrast, in a squamous cell carcinoma derived cell line, both GPR109A and GPR109B show a more diffuse cellular localization and the receptors are nearly non-functional. PMID: 21655214
    19. niacin-mediated activation of GP109A in liver lowers ABCA1 expression leading to reduced hepatic cholesterol efflux to high density lipoprotein. PMID: 20655299
    20. Observational study of gene-disease association. (HuGE Navigator) PMID: 19913121
    21. Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator) PMID: 20628086
    22. The agonist-induced internalization of GPR109A receptors is regulated by GRK2 and arrestin3 in a pertussis toxin-sensitive manner and that internalized receptor recycling is independent of endosomal acidification. PMID: 20460384
    23. these results demonstrate that GPR109A and GPR109B dimerization is a constitutive process occurring early during biosynthesis. PMID: 20380810
    24. Data show that Mk-6892 was discovered as full and potent niacin receptor (GPR109A) agonist. PMID: 20184326
    25. HM74b has high similarity to HM74 is a receptor for nicotinic acid [HM74b] PMID: 12646212
    26. Our results provided direct evidence indicating that HM74A, but not HM74, was sufficient to mediate anti-lipolytic effect of niacin in adipose tissue. PMID: 16018973
    27. However, the synergistic effects of HM74A were not dramatically affected by co-treatment with both inhibitors, indicating the cross-talk occurred at the receptor level. PMID: 16674924
    28. neutrophils express functional GPR109A receptors,which might be involved in the regulation of neutrophil numbers PMID: 17932499
    29. Data show that the high-affinity niacin receptor HM74A is significantly down-regulated in the anterior cingulate cortex of individuals with schizophrenia. PMID: 18639743
    30. Data show that many phenolic acids, including those from the hydroxybenzoic and hydroxycinnamic acid classes, can bind and activate GPR109A (HM74a/PUMA-G), the receptor for the antidyslipidemic agent nicotinic acid. PMID: 19136666
    31. GPR109A receptor plays an important role in the dual regulation of adiponectin secretion and lipolysis PMID: 19141678
    32. Data show that the coordinated PPARgamma-mediated regulation of the GPR81, GPR109A and GPR109B presents a novel mechanism by which TZDs may reduce circulating free fatty acid levels and perhaps ameliorate insulin resistance in obese patients. PMID: 19633298
    33. Observational study of gene-disease association and gene-gene interaction. (HuGE Navigator) PMID: 19502010
    34. Observational study of gene-disease association. (HuGE Navigator) PMID: 18787507

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  • 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：
    Expression largely restricted to adipose tissue and spleen. Expressed on mature neutrophils but not on immature neutrophils or eosinophils.
  • 数据库链接：

    HGNC: 24827

    OMIM: 609163

    KEGG: hsa:338442

    STRING: 9606.ENSP00000375066

    UniGene: Hs.524812