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merck millipore,默克密理博,HTS157M,ChemiSCREEN™ Human α2B Adrenergic Receptor Membrane Preparation
产品名称：ChemiSCREEN™ Human α2B Adrenergic Receptor Membrane Preparation
产品型号：HTS157M
Human alpha2B GPCR membrane prepation for Radioligand binding Assays.
merck millipore,默克密理博,HTS157M,ChemiSCREEN™ Human α2B Adrenergic Receptor Membrane Preparation
- 产品介绍
重要规格表
品种 宿主细胞 蛋白靶 Human Chem-1 alpha2B 描述 产品目录编号 HTS157M 品牌系列 Chemicon®
商名 - Chemicon
- ChemiScreen
描述 ChemiSCREEN™ Human α2B Adrenergic Receptor Membrane Preparation 概述 Full-length human ADRA2B transcript cDNA encoding α2B. Alternate Names - alpha2B
背景信息 The endogenous catecholamines epinephrine and norepinephrine have profound effects on smooth muscle activity, cardiac function, carbohydrate and fat metabolism, hormone secretion, neurotransmitter release, and central nervous system actions. These activities are mediated by GPCRs belonging to two subfamilies, the α- and β-adrenoceptors (Bylund et al., 1994). The α2 adrenergic receptor subfamily members, consisting of α2A, α2B, and α2C, couple primarily to Gi to inhibit cAMP production, and play an important role in regulation of cardiovascular and CNS function. Experiments with α2A-selective agonists and mice lacking α2A demonstrate that activation of α2A results in hypotension, sedation, analgesia, and hypothermia (Kable et al., 2000). Chemicon's α2B membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of agonists and antagonists at α2B. The membrane preparations exhibit a Kd of 11.5 nM for [3H]-Rauwolscine. With 15 nM [3H]-Rauwolscine, 5 µg/well α2B Membrane Prep typically yields greater than 30-fold signal-to-background ratio. 产品信息 演示 One package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 20-fold signal:background with 3H-labeled Rauwolscine at 15 nM
Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
应用 应用 Human alpha2B GPCR membrane prepation for Radioligand binding Assays. 生物信息 品种 Human 品种反应性 Human Entrez基因编号 - NM_000682.5
Entrez基因汇总 Alpha-2-adrenergic receptors are members of the G protein-coupled receptor superfamily. They include 3 highly homologous subtypes: alpha2A, alpha2B, and alpha2C. These receptors have a critical role in regulating neurotransmitter release from sympathetic nerves and from adrenergic neurons in the central nervous system. This gene encodes the alpha2B subtype, which was observed to associate with eIF-2B, a guanine nucleotide exchange protein that functions in regulation of translation. A polymorphic variant of the alpha2B subtype, which lacks 3 glutamic acids from a glutamic acid repeat element, was identified to have decreased G protein-coupled receptor kinase-mediated phosphorylation and desensitization; this polymorphic form is also associated with reduced basal metabolic rate in obese subjects and may therefore contribute to the pathogenesis of obesity. This gene contains no introns in either its coding or untranslated sequences. 基因符号 - ADRARL1
- ADRA2B
- ADRA2L1
- ALPHA2BAR
- ADRA2RL1
GPCR类别 A 宿主细胞 Chem-1 蛋白靶 alpha2B 靶子系列 Adrenergic UniProt编号 - P18089
UniProt汇总 FUNCTION: SwissProt: P18089 # Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is clonidine > norepinephrine > epinephrine = oxymetazoline > dopamine > p-tyramine = phenylephrine > serotonin > p-synephrine / p-octopamine. For antagonists, the rank order is yohimbine > chlorpromazine > phentolamine > mianserine > spiperone > prazosin > alprenolol > propanolol > pindolol.
SIZE: 450 amino acids; 49954 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
SIMILARITY: SwissProt: P18089 ## Belongs to the G-protein coupled receptor 1 family.孵化条件 Membranes are mixed with radioactive ligand and unlabeled competitor (see Figures 1 and 2 for concentrations tested) in binding buffer in a nonbinding 96-well plate, and incubated for 1-2 h. Prior to filtration, an FC 96-well harvest plate (Millipore cat. # MAHF C1H) is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM HEPES, pH 7.4, 0.5% BSA. Binding reaction is transferred to the filter plate, and washed 3 times (1 mL per well per wash) with Wash Buffer. The plate is dried and counted.
Binding buffer: 50 mM Hepes, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.2% BSA, filtered and stored at 4°C
Radioligand: [3H]-Rauwolscine (Perkin Elmer#: NET-722)
Wash Buffer: 50 mM Hepes, pH 7.4, 500mM NaCl , 0.1% BSA, filtered and stored at 4°C.产品使用声明 质量保证 Table 1. Signal:background and specific binding values obtained in a competition binding assay with α2B membrane prep and unlabeled rauwolscine. 5 µg/well Signal:Background 64.7 Specific Binding (cpm) 14646
SPECIFICATIONS: 1 unit = 5 µg
Bmax for [3H]-rauwolscine binding: 154 pmol/mg protein
Kd for [3H]-rauwolscine binding: ~11.5 nM使用声明 - Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
储存和货运信息 存储条件 Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw. 包装信息 数量 200 units
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