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merck millipore,默克密理博,HTS037M,ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor
产品名称：ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor
产品型号：HTS037M
Human PAR2 GPCR membrane preparation for GTPγS Binding Assays.
merck millipore,默克密理博,HTS037M,ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor
- 产品介绍
- merck millipore,默克密理博,HTS037M,ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor
重要规格表
应用说明 品种 宿主细胞 蛋白靶 GTPγS Binding Assay. Human Chem-1 PAR2 描述 产品目录编号 HTS037M 品牌系列 Chemicon®
商名 - Chemicon
- ChemiScreen
描述 ChemiSCREEN™ Membrane Preparation Recombinant Human PAR2 Protease-Activated Receptor 概述 Human PAR2 背景信息 The protease-activated receptor family of GPCRs has a unique mechanism of activation, in which protease cleaves a prodomain to reveal a peptide sequence that functions as a tethered ligand to activate the receptor (Macfarlane et al., 2001). PAR2 is specifically activated by trypsin and mast cell tryptase, and can also be activated by free peptide analogs of the tethered ligand, such as SLIGRL and furoyl-LIGRLO (Coelho et al., 2003; Kawabata et al., 2004). PAR2 is expressed in endothelium, gastrointestinal epithelium, macrophages, eosinophils and nociceptive afferent neurons. Activation of PAR2 in these cells and tissues promotes vasodilation, inflammation, allergy, hyperalgesia and intestinal permeability. Therefore, PAR2 is regarded as an attractive therapeutic target for colitis, asthma, myocardial ischemia/reperfusion injury, and pain (Cocks et al., 1999; Hansen et al., 2005; Lindner et al., 2000; McLean et al., 2002; Vergnolle et al., 2001). Chemicon's PAR2 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 PAR2 interactions with its ligands. The membrane preparations exhibit an EC50 of 1.9 μM for furoyl-LIGRLO 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 with no preservatives.
Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80oC.
应用 应用 Human PAR2 GPCR membrane preparation for GTPγS Binding Assays. 应用说明 GTPγS Binding Assay. 生物信息 品种 Human Entrez基因编号 - AY336105
Entrez基因汇总 Coagulation factor II (thrombin) receptor-like 1 (F2RL1) is a member of the large family of 7-transmembrane-region receptors that couple to guanosine-nucleotide-binding proteins. F2RL1 is also a member of the protease-activated receptor family. It is activated by trypsin, but not by thrombin. It is activated by proteolytic cleavage of its extracellular amino terminus. The new amino terminus functions as a tethered ligand and activates the receptor. The F2RL1 gene contains two exons and is widely expressed in human tissues. The predicted protein sequence is 83% identical to the mouse receptor sequence. 基因符号 - PAR-2
- F2RL1
- PAR2
- GPR11
GPCR类别 A 宿主细胞 Chem-1 蛋白靶 PAR2 靶子系列 Protease-activated UniProt编号 - P55085
UniProt汇总 FUNCTION: SwissProt: P55085 # Receptor for trypsin and trypsin-like enzymes coupled to G proteins that stimulate phosphoinositide hydrolysis. May have a role in the regulation of vascular tone.
SIZE: 397 amino acids; 44126 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Widely expressed in tissues with especially high levels in pancreas, liver, kidney, small intestine, and colon. Moderate expression is detected in many organs, but none in brain or skeletal muscle.
PTM: A proteolytic cleavage generates a new N-terminus that functions as a tethered ligand.
SIMILARITY: SwissProt: P55085 ## Belongs to the G-protein coupled receptor 1 family.孵化条件 GTPγS ASSAY CONDITIONS: Membranes are permeabilized by addition of saponin to an equal concentration by mass, then mixed with [35S]-GTPγS (final concentration of 0.1 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 furoyl-LIGRLO is 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 an FB filter plate (Millipore MAHF B1H) 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. 产品使用声明 质量保证 1 unit = 5 μg
EC50 for furoyl-LIGRLO: ~1.9 μM in a GTPγS binding assay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 Store at –70°C. Product is stable for at least 6 months from the date of receipt when stored as directed. Do not freeze and thaw. 包装信息 数量 200 units
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