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merck millipore,默克密理博,HTS073M,ChemiScreen™ Recombinant Human β2 Adrenoceptor
产品名称:ChemiScreen™ Recombinant Human β2 Adrenoceptor
产品型号:HTS073M
Human beta 2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
merck millipore,默克密理博,HTS073M,ChemiScreen™ Recombinant Human β2 Adrenoceptor
- 产品介绍
重要规格表
应用说明 品种 宿主细胞 蛋白靶 Radioligand binding assay, and GTPγS binding. Human Chem-2 beta 2 描述 产品目录编号 HTS073M 品牌系列 Chemicon®
商名 - Chemicon
- ChemiScreen
描述 ChemiScreen™ Recombinant Human β2 Adrenoceptor 概述 Human β2 adrenoceptor 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 -adrenergic receptors (Bylund et al., 1994). The β -adrenergic receptors, primarily the β2 subtype, mediate relaxation of smooth muscle in many tissues, and β 2-selective agonists are the preferred drugs for stimulating bronchodilation in the treatment of asthma and chronic obstructive pulmonary disease (Sears and Lotvall, 2005). Activation of the β-adrenergic receptors, primarily the β1 subtype and to a lesser extent the β2 subtype, acutely increases heart rate, cardiac output, and cardiac automaticity, and chronically increases cardiac myocyte apoptosis. As a result, β -adrenergic receptor antagonists (β blockers) are effective in the treatment of congestive heart failure and arrhythmia (Feldman et al., 2005). Chemicon's β2 adrenoceptor 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 antagonists of β2 adrenoceptor interactions with (-)Iodocyanopindolol (ICYP). The membrane preparations exhibit a Kd of 0.51 nM for [125I]-(-)ICYP. With 5 µg/well β2 Adrenoceptor Membrane Prep and 0.5 nM [125I]-(-)ICYP, a greater than 40-fold signal-to-background ratio was obtained. 产品信息 演示 One package contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 40-fold signal:background with 125I-labeled (-)Iodocyanopindolol at 0.5 nM. Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives. Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80oC. 应用 应用 Human beta 2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding. 应用说明 Radioligand binding assay, and GTPγS binding. 生物信息 品种 Human 品种反应性 Human Entrez基因编号 - NM_005160.3
Entrez基因汇总 The beta-adrenergic receptor kinase specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G protein-coupled receptors. Overall, the beta adrenergic receptor kinase 2 has 85% amino acid similarity with beta adrenergic receptor kinase 1, with the protein kinase catalytic domain having 95% similarity. These data suggest the existence of a family of receptor kinases which may serve broadly to regulate receptor function. 基因符号 - EC 2.7.11.15
- ADRBK2
- BARK2
- GRK3
- Beta-ARK-2
GPCR类别 A 宿主细胞 Chem-2 蛋白靶 beta 2 靶子系列 Adrenergic UniProt编号 - P35626
UniProt汇总 FUNCTION: SwissProt: P35626 # Specifically phosphorylates the agonist-occupied form of the beta-adrenergic and closely related receptors.
SIZE: 688 amino acids; 79710 Da
SIMILARITY: SwissProt: P35626 ## Belongs to the protein kinase superfamily. AGC Ser/Thr protein kinase family. GPRK subfamily. & Contains 1 AGC-kinase C-terminal domain. & Contains 1 PH domain. & Contains 1 protein kinase domain. & Contains 1 RGS domain.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, a GF/C 96-well filter plate is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM HEPES, pH 7.4. 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, filtered and stored at 4°C
Radioligand: [125I]-(-) Iodocyanopindolol (Perkin Elmer # NEX189)
Wash Buffer: 50 mM Hepes, pH 7.4, 500 mM NaCl, filtered and stored at 4°C.产品使用声明 质量保证 Signal:background and specific binding values obtained in a competition binding assay with varying amounts of β2 adrenoceptor membrane prep.
10 µg/well 5 µg/well Signal:Background 95 103 Specific Binding (cpm) 51393 58517
SPECIFICATIONS: 1 unit = 5 µg membrane preparation
Bmax: 8.5 pmol/mg
Kd: 0.51 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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