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merck millipore,默克密理博,HTS104M,ChemiSCREEN™ Membrane Preparation Recombinant Human β1 Adrenoceptor Receptor
产品名称：ChemiSCREEN™ Membrane Preparation Recombinant Human β1 Adrenoceptor Receptor
产品型号：HTS104M
Human beta 1 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
merck millipore,默克密理博,HTS104M,ChemiSCREEN™ Membrane Preparation Recombinant Human β1 Adrenoceptor Receptor
- 产品介绍
- merck millipore,默克密理博,HTS104M,ChemiSCREEN™ Membrane Preparation Recombinant Human β1 Adrenoceptor 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 beta 1 描述 产品目录编号 HTS104M 商名 - Chemicon
- ChemiScreen
描述 ChemiSCREEN™ Membrane Preparation Recombinant Human β1 Adrenoceptor Receptor 概述 Full-length human ADRB1 cDNA encoding the β1 adrenoceptor Alternate Names - beta1
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 three members of the β-adrenergic receptor family, β1, β2 and β3, couple to Gs to increase cAMP upon activation. In the heart, the β1 receptor constitutes 70-80% of the β-adrenergic receptors. Activation of cardiac β-adrenergic receptors acutely increases heart rate, cardiac output, and cardiac automaticity, and chronically increases cardiac myocyte apoptosis. In failing hearts, the β1 subtype is downregulated and desensitized, probably as a result of increased catecholamine levels. As a result, β-adrenergic receptor antagonists (β blockers) are effective in the treatment of congestive heart failure and arrhythmia (Lohse et al., 2003). Millipore's β1 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 β1 adrenoceptor interactions. The membrane preparations exhibit a Kd of 2.6 nM for [125I]-(-) Iodocyanopindolol (ICYP). With 5 µg/well β1 Adrenoceptor Membrane Prep and 0.25 nM [125I]-(-)ICYP, a greater than 15-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 15-fold signal:background with 125I-labeled (-)Iodocyanopindolol at 0.25 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 beta 1 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_000684.2
Entrez基因汇总 The adrenergic receptors (subtypes alpha 1, alpha 2, beta 1, and beta 2) are a prototypic family of guanine nucleotide binding regulatory protein-coupled receptors that mediate the physiological effects of the hormone epinephrine and the neurotransmitter norepinephrine. Specific polymorphisms in this gene have been shown to affect the resting heart rate and can be involved in heart failure. 基因符号 - BETA1AR
- ADRB1
- ADRB1R
- RHR
- B1AR
GPCR类别 A 宿主细胞 Chem-1 蛋白靶 beta 1 靶子系列 Adrenergic UniProt编号 - P08588
UniProt汇总 FUNCTION: SwissProt: P08588 # Beta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity.
SIZE: 477 amino acids; 51323 Da
SUBUNIT: Interacts with GOPC and DLG4.
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein. Note=Localized at the plasma membrane. Found in the Golgi upon GOPC overexpression.
DOMAIN: SwissProt: P08588 The PDZ domain-binding motif mediates competitive interactions with GOPC and DLG4 and plays a role in subcellular location of the receptor.
PTM: Homologous desensitization of the receptor is mediated by its phosphorylation by beta-adrenergic receptor kinase.
SIMILARITY: 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. 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, 500mM NaCl, filtered and stored at 4°C.产品使用声明 质量保证 5 µg/well 10 µg/well Signal:Background 28.5 34.6 Specific Binding (cpm) 27002 28467
SPECIFICATIONS: 1 unit = 5 μg membrane preparation
Bmax: 47.9 pmol/mg
Kd: ~2.6 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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