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merck millipore,默克密理博,HTS087M,ChemiScreen™ Recombinant HumanMembrane Preparation α1A Adrenergic Receptor
产品名称：ChemiScreen™ Recombinant HumanMembrane Preparation α1A Adrenergic Receptor
产品型号：HTS087M
Human alpha1A GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
merck millipore,默克密理博,HTS087M,ChemiScreen™ Recombinant HumanMembrane Preparation α1A Adrenergic Receptor
- 产品介绍
- merck millipore,默克密理博,HTS087M,ChemiScreen™ Recombinant HumanMembrane Preparation α1A Adrenergic Receptor
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-1 alpha1A 描述 产品目录编号 HTS087M 品牌系列 Chemicon®
商名 - Chemicon
- ChemiScreen
描述 ChemiScreen™ Recombinant HumanMembrane Preparation
α1A Adrenergic Receptor概述 Human α1A 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 three members of the α1 subclass of adrenoceptors, α1A, α1B and α1D, couple to Gq, and promote contraction of vascular and urinary tract smooth muscle, relaxation of intestinal smooth muscle, increased contractile force in the heart, and glycogenolysis and gluconeogenesis in the liver. The different subtypes have overlapping distributions and variably contribute to these effects depending on species and tissue; the α1A subtype plays a prominent role in urogenital smooth muscle contraction and renal artery contraction (Hrometz et al., 1999; Ruffolo and Hieble, 1999). Activation of α1 adrenoceptors also influences cell proliferation; α1A inhibits cell growth by arresting progression at the G1/S transition (Shibata et al., 2003). Chemicon's α1A 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 α1A interactions with prazosin. The membrane preparations exhibit a Kd of 1.34 nM for [3H]-prazosin. With 5 µg/well α1A Membrane Prep and 1 nM [3H]-prazosin, a greater than 7-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 7-fold signal:background with 3H-labeled prazosin at 1 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 -80°C. 应用 应用 Human alpha1A 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 Entrez基因编号 - NM_033304.2
- NM_000680.2
- NM_033302.2
- NM_033303.3
Entrez基因汇总 Alpha-1-adrenergic receptors (alpha-1-ARs) are members of the G protein-coupled receptor superfamily. They activate mitogenic responses and regulate growth and proliferation of many cells. There are 3 alpha-1-AR subtypes: alpha-1A, -1B and -1D, all of which signal through the Gq/11 family of G-proteins and different subtypes show different patterns of activation. This gene encodes alpha-1A-adrenergic receptor. Alternative splicing of this gene generates four transcript variants, which encode four different isoforms with distinct C-termini but having similar ligand binding properties. 基因符号 - ADRA1D
- ADRA1A
- ADRA1C
- ADRA1L1
- ALPHA1AAR
GPCR类别 A 宿主细胞 Chem-1 蛋白靶 alpha1A 靶子系列 Adrenergic UniProt编号 - P35348
UniProt汇总 FUNCTION: SwissProt: P35348 # This alpha-adrenergic receptor mediates its action by association with G proteins that activate a phosphatidylinositol- calcium second messenger system. Its effect is mediated by G(q) and G(11) proteins.
SIZE: 466 amino acids; 51487 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Heart, brain, liver and prostate, but not in kidney, lung, adrenal, aorta and pituitary. Isoform 4 is the most abundant isoform expressed in the prostate with high levels also detected in liver and heart.
PTM: Carboxyl-terminal Ser or Thr residues may be phosphorylated (By similarity).
SIMILARITY: SwissProt: P35348 ## 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, a GF/C 96-well filter plate 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] prazosin (Perkin Elmer # NET823)
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 SPECIFICATIONS: Signal:background and specific binding values obtained in a competition binding assay with varying amounts of α1A membrane prep.
10 µg/well 5 µg/well Signal:Background 10.7 9.6 Specific Binding (cpm) 3244 2530
1 unit = 5 µg membrane preparation
Bmax: 11.02 pmol/mg
Kd: 1.34 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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