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merck millipore,默克密理博,HTS061M,ChemiSCREEN™ Membrane Preparation Recombinant Human CysLT1 Cysteinyl Leukotriene Receptor
产品名称:ChemiSCREEN™ Membrane Preparation Recombinant Human CysLT1 Cysteinyl Leukotriene Receptor
产品型号:HTS061M
Human CysLT1 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
merck millipore,默克密理博,HTS061M,ChemiSCREEN™ Membrane Preparation Recombinant Human CysLT1 Cysteinyl Leukotriene Receptor
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- merck millipore,默克密理博,HTS061M,ChemiSCREEN™ Membrane Preparation Recombinant Human CysLT1 Cysteinyl Leukotriene 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 CysLT1 描述 产品目录编号 HTS061M 品牌系列 Chemicon®
商名 - Chemicon
- ChemiScreen
描述 ChemiSCREEN™ Membrane Preparation Recombinant Human CysLT1 Cysteinyl Leukotriene Receptor 概述 Full-length human CYSLTR1 cDNA 背景信息 The cysteinyl leukotrienes, leukotriene C4, leukotriene D4 and leukotriene E4, are arachidonic acid derivatives modified by glutathione, Cys-Gly or Cys. Activated mast cells release cysteinyl leukotrienes, which cause smooth muscle contraction, airway constriction, and vascular permeability. The biological effects of the cysteinyl leukotrienes are mediated by two GPCRs, CysLT1 and CysLT2. A CysLT1 selective antagonist, montelukast, is used clinically in the treatment of asthma (Brink et al., 2003; Evans, 2002). Chemicon's CysLT1 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 CysLT1 interactions and its ligands. The membrane preparations exhibit a Kd of 0.97nM for [33H]-Leukotriene D4 (LTD4). With 10.0ug/well CysLT1 membrane prep and 1.5 nM [33H]-Leukotriene D4, a greater than 3-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 3-fold signal:background with 3H-labeled LTD4 at 1.5 nM.
Liquid in packaging buffer: 50 mM Tris, pH 7.4, 10% glycerol with no preservatives.
Packaging method: Membranes protein was adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80oC.应用 应用 Human CysLT1 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_006639.2
Entrez基因汇总 The cysteinyl leukotrienes LTC4, LTD4, and LTE4 are important mediators of human bronchial asthma. Pharmacologic studies have determined that cysteinyl leukotrienes activate at least 2 receptors, the protein encoded by this gene and CYSLTR2. This encoded receptor is a member of the superfamily of G protein-coupled receptors. Activation of this receptor by LTD4 results in contraction and proliferation of smooth muscle, oedema, eosinophil migration and damage to the mucus layer in the lung. 基因符号 - CysLT1
- CYSLTR1
- CysLTR1
- CYSLTR
- CysLT(1)
- MGC46139
- HMTMF81
- CYSLT1
- CYSLT1R
- HG55
GPCR类别 A 宿主细胞 Chem-1 蛋白靶 CysLT1 靶子系列 Leukotriene UniProt编号 - Q9Y271
UniProt汇总 FUNCTION: SwissProt: Q9Y271 # Receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with and without asthma. Stimulation by LTD4 results in the contraction and proliferation of smooth muscle, edema, eosinophil migration and damage to the mucus layer in the lung. This response is mediated via a G-protein that activates a phosphatidylinositol-calcium second messenger system. The rank order of affinities for the leukotrienes is LTD4 > LTE4 = LTC4 > LTB4.
SIZE: 337 amino acids; 38541 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Widely expressed, with highest levels in spleen and peripheral blood leukocytes. Lower expression in several tissues, such as lung (mostly in smooth muscle bundles and alveolar macrophages), placenta, small intestine, pancreas, colon and heart.
SIMILARITY: SwissProt: Q9Y271 ## Belongs to the G-protein coupled receptor 1 family.
MISCELLANEOUS: Selective antagonists, such as montelukast (Singulair), zafirlukast (Accolate) and pranlukast (Onon), are used in the treatment of the asthma crisis.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 50 mM Tris, 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 Tris, pH7.4, 20 mM CaCl2, 25 mM MgCl2, 10 mM Glycine, 10 mM L-Cysteine, filtered and stored at 4°C
Radioligand: [3H] LTD4 (Perkin Elmer#: NET-101)
Wash Buffer: 50 mM Tris, pH 7.4, 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 varying amounts of CysLT1 Receptor membrane prep.
SPECIFICATIONS: 1 unit = 10 µg membrane preparation10 µg/well Signal:Background 4.62 Specific Binding (cpm) 1451.4
Bmax: 1.53 pmol/mg
Kd: 0.97 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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