merck millipore,默克密理博,HTS096M,ChemiSCREEN™ Human α2A Adrenergic Receptor Membrane Preparation

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merck millipore,默克密理博,HTS096M,ChemiSCREEN™ Human α2A Adrenergic Receptor Membrane Preparation
产品名称：ChemiSCREEN™ Human α2A Adrenergic Receptor Membrane Preparation
产品型号：HTS096M
Human alpha2A GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

merck millipore,默克密理博,HTS096M,ChemiSCREEN™ Human α2A Adrenergic Receptor Membrane Preparation

产品介绍

merck millipore,默克密理博,HTS096M,ChemiSCREEN™ Human α2A Adrenergic Receptor Membrane Preparation

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	alpha2A

描述
产品目录编号	HTS096M
品牌系列	Chemicon®
商名	Chemicon ChemiScreen
描述	ChemiSCREEN™ Human α_2A Adrenergic Receptor Membrane Preparation
概述	Full-length human ADRA2A transcript variant 1 cDNA encoding α_2A
Alternate Names	alpha2A
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 α_2A, α_2B, and α_2C, couple primarily to Gi to inhibit cAMP production, and play an important role in regulation of cardiovascular and CNS function. Experiments with α_2A-selective agonists and mice lacking α_2A demonstrate that activation of α_2A results in hypotension, sedation, analgesia, and hypothermia (Kable et al., 2000). Chemicon's α_2A 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 α_2A. The membrane preparations exhibit a Kd of 5.4 nM for [³H]-MK-912. With 5 nM [³H]-MK-912, 5 µg/well α_2A Membrane Prep typically yields greater than 20-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 MK-912 at 5 nM Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.

应用
应用	Human alpha2A 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_000681.2
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. Studies in mouse revealed that both the alpha2A and alpha2C subtypes were required for normal presynaptic control of transmitter release from sympathetic nerves in the heart and from central noradrenergic neurons; the alpha2A subtype inhibited transmitter release at high stimulation frequencies, whereas the alpha2C subtype modulated neurotransmission at lower levels of nerve activity. This gene encodes alpha2A subtype and it contains no introns in either its coding or untranslated sequences.
基因符号	ADRAR ADRA2A ZNF32 ADRA2R ALPHA2AAR Alpha-2AAR ADRA2 OTTHUMP00000058849
GPCR类别	A
宿主细胞	Chem-1
蛋白靶	alpha2A
靶子系列	Adrenergic
UniProt编号	P08913
UniProt汇总	FUNCTION: SwissProt: P08913 # 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 oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol. SIZE: 450 amino acids; 48957 Da SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein. SIMILARITY: SwissProt: P08913 ## 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] MK-912 (Perkin Elmer#: NET-1059) 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 α_2A membrane prep and unlabeled rauwolscine.

	10 µg/well	5 µg/well
Signal:Background	28.97	34.14
Specific Binding (cpm)	11777	9147

SPECIFICATIONS: 1 unit = 5 µg
Bmax for [3H] MK-912 binding: 71.4 pmol/mg protein
Kd for [3H] MK-912 binding: ~5.4 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

merck millipore,默克密理博,HTS096M,ChemiSCREEN™ Human α2A Adrenergic Receptor Membrane Preparation

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