merck millipore,默克密理愽
  • merck millipore,默克密理博,HTS201M,ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A Receptor

  • merck millipore,默克密理博,HTS201M,ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A Receptor

    产品名称：ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A Receptor
    产品型号：HTS201M
    Human GPR109A GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

    merck millipore,默克密理博,HTS201M,ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A Receptor

  • 产品介绍
  • merck millipore,默克密理博,HTS201M,ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A 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.HumanChem-4GPR109A
    描述
    产品目录编号 HTS201M
    商名
    • Chemicon
    • ChemiScreen
    描述 ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A Receptor
    概述 Full-length human GPR109A cDNA
    背景信息 Nicotinic acid (niacin), a vitamin of the B complex, is used clinically in high doses to decrease total plasma levels of cholesterol. Interestingly, the total cholesterol levels and low-density lipoprotein (LDL) concentrations decrease, while the high-density lipoprotein (HDL) concentrations increase with nicotinic acid treatment. The cholesterol-lowering effects of nicotinic acid result from inhibition of lipolysis in adipose tissue, which decreases plasma levels of free fatty acid (FFA) (Altschul et al., 1955; Carlson, 1963). In a study of nicotinic acid and myocardial infarction in the Coronary Drug Project (1966-1975), patients receiving 3 g/day nicotinic acid exhibited reduced rates of myocardial infarction (Coronary Drug Project Research Group, 1975). However, an unwanted effect of high doses of nicotinic acid is vasodilatation, occurring mainly in the upper body and face, known as flushing. Recently two receptors for nicotinic acid have been identified as class A G protein-coupled receptors that couple to Gi to inhibit accumulation of cAMP (Offermans, 2006). GPR109A (also known as HM74A in humans and PUMA-G in mice) is a high affinity receptor for nicotinic acid, whereas GPR109B (also known as HM74) is a low affinity receptor for nicotinic acid that is found in humans but not rodents (Wise et al., 2003). GPCR109A is found primarily in adipose tissue and immune cells. Millipore's GPR109A 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 GPR109A interactions with its ligands. The membrane preparations exhibit EC50s of 3.65 μM for nicotinic acid in a GTPγS binding assay.
    产品信息
    格式 Membranes
    演示 Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA no preservatives.
    Packaging method: Membranes protein were adjusted to 1 mg/ml in 1 ml packaging buffer, rapidly frozen, and stored at -80°C
    应用
    应用 Human GPR109A 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_177551.3
    基因符号
    • HM74b
    • GPR109A
    • HM74a
    • HM74A
    • PUMAG
    • Puma-g
    GPCR类别 A
    宿主细胞 Chem-4
    蛋白靶 GPR109A
    靶子系列 Nicotinic Acid
    UniProt编号
    • Q8TDS4
    UniProt汇总 FUNCTION: SwissProt: Q8TDS4 # Acts as a high affinity receptor for nicotinic acid and mediates its anti-lipolytic effect through a G(i)-protein-mediated inhibition of adenylyl cyclase. This pharmacological effect requires nicotinic acid doses that are much higher than those provided by a normal diet.
    SIZE: 363 amino acids; 41850 Da
    SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
    TISSUE SPECIFICITY: Expression largely restricted to adipose tissue and spleen.
    SIMILARITY: SwissProt: Q8TDS4 ## Belongs to the G-protein coupled receptor 1 family.
    MISCELLANEOUS: The rank order of potency for the displacement of nicotinic acid binding is 5-methyl pyrazole-3-carboxylic acid = pyridine-3-acetic acid > acifran > 5-methyl nicotinic acid = acipimox > nicotinuric acid = nicotinamide.
    孵化条件 ASSAY CONDITIONS: Membranes are permeabilized by addition of saponin to an equal concentration by mass, then mixed with [35S]-GTPγS (final concentration of 0.3 nM) in 20 mM HEPES, pH 7.4/100 mM NaCl/10 mM MgCl2/0.5 μM GDP in a nonbinding 96-well plate. Unlabeled nicotinic acid was added to the final concentration indicated in Figure 1 (final volume 100 μL), and incubated for 30 min at 30°C. The binding reaction is transferred to a GF/B filter plate (Millipore MAHF B1H) previously prewetted with water, and washed 3 times (1 mL per well per wash) with cold 10 mM sodium phosphate, pH 7.4. The plate is dried and counted.

    One vial contains enough membranes for at least 200 assays (units), where one unit is the amount of membrane that will yield greater than 1000 cpm specific nicotinic acid-stimulated [35S]-GTPγS binding.

    The GPR109A membrane preparation is expected to be functional in a radioligand binding assay; however, the end user will need to determine the optimal radiolabeled ligand for use with this product.
    产品使用声明
    质量保证 SPECIFICATIONS: 1 unit = 5 μg
    EC50 in GTPγS binding assay by Nicotinic Acid: ~ 3.65 μM
    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,HTS201M,ChemiSCREEN™ Membrane Preparation Recombinant Human GPR109A Receptor

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下一件merck millipore产品：merck millipore,默克密理博,05-919,Anti-T-Cell Receptor Antibody, clone C305


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