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merck millipore,默克密理博,HTS119M,ChemiSCREEN™ Membrane Preparation Recombinant Human GABAB1b/GABAB2 Receptor
产品名称：ChemiSCREEN™ Membrane Preparation Recombinant Human GABAB1b/GABAB2 Receptor
产品型号：HTS119M
Human GABAB1b GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
merck millipore,默克密理博,HTS119M,ChemiSCREEN™ Membrane Preparation Recombinant Human GABAB1b/GABAB2 Receptor
- 产品介绍
- merck millipore,默克密理博,HTS119M,ChemiSCREEN™ Membrane Preparation Recombinant Human GABAB1b/GABAB2 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 GABAB1b 描述 产品目录编号 HTS119M 商名 - Chemicon
- ChemiScreen
描述 ChemiSCREEN™ Membrane Preparation Recombinant Human GABAB1b/GABAB2 Receptor 概述 Full-length human GABBR1b and GPR51 cDNAs encoding GABAB1b/GABAB2 Alternate Names - GABA<sub>B</sub>
背景信息 The neurotransmitter γ-aminobutyric acid (GABA) exerts its effects through an ion channel, GABAA, and a GPCR, GABAB. Functional GABAB is a heterodimer composed of the GABAB1 and GABAB2 subunits, which share 35% sequence identity and belong to the class 3 family of GPCRs. The GABAB1 subunit, which exists as splice variants GABAB1a and GABAB1b, binds directly to GABA and is required for agonist activation. The GABAB2 and GABAB1 subunits associate by formation of a coiled coil by their C-terminal tails; this association masks an ER retention sequence in GABAB1 to permit export from the ER and trafficking to the cell surface. In addition to its chaperone function, GABAB2 is the component that couples to Gi to reduce intracellular cAMP. Agonists of GABAB, such as baclofen, are used clinically for treatment of muscle spasticity, migraine headache and musculoskeletal pain (Bowery et al., 2002). Chemicon's GABAB1b 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 GABAB1b receptor interactions with its ligand. The membrane preparations exhibit a Kd of 1.15nM for [3H]-CGP 54626A. With 5.0 ug/well GABAB1b Membrane Prep and 7.5nM [3H]-CGP 54626A, a greater than 5-fold signal-to-background ratio was obtained. 产品信息 演示 Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
Packaging method: Membranes protein was adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.应用 应用 Human GABAB1b 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_021905.1
- NM_001470.1
- NM_021903.1
- NM_021904.1
Entrez基因汇总 Gamma-aminobutyric acid (GABA) is the main inhibitory neurotransmitter in the mammalian central nervous system. GABA exerts its effects through ionotropic [GABA(A/C)] receptors, to produce fast synaptic inhibition, and metabotropic [GABA(B)] receptors, to produce slow, prolonged inhibitory signals. The GABA(B) receptor consists of a heterodimer of two related 7-transmembrane receptors, GABA(B) receptor 1 and GABA(B) receptor 2. The GABA(B) receptor 1 gene is mapped to chromosome 6p21.3 within the HLA class I region close to the HLA-F gene. Susceptibility loci for multiple sclerosis, epilepsy, and schizophrenia have also been mapped in this region. Alternative splicing of this gene generates 4 transcript variants. 基因符号 - GPRC3A
- GABBR1
- dJ271M21.1.1
- GABBR1-3
- GABAB(1e)
- hGB1a
- GABABR1
- dJ271M21.1.2
- Gb1
- GABA-B-R1
GPCR类别 C 宿主细胞 Chem-1 蛋白靶 GABAB1b 靶子系列 GABAB UniProt编号 - Q9UBS5
UniProt汇总 FUNCTION: SwissProt: Q9UBS5 # Isoform 1E function may be to regulate the availability of functional GABA-B-R1A/GABA-B-R2 heterodimers by competing for GABA-B-R2 dimerization. This could explain the observation that certain small molecule ligands exhibit differential affinity for central versus peripheral sites.
COFACTOR: Calcium. Required for high affinity binding to GABA.
SIZE: 961 amino acids; 108320 Da
SUBUNIT: Heterodimer of GABA-B-R1 and GABA-B-R2. Neither of which is effective on its own and homodimeric assembly does not seem to happen. Isoform 1E (without C-terminal intracellular domain) is unable to dimerize via a coiled-coil interaction with GABA-B-R2. Interacts with the leucine zipper of the C-terminal bZIP domain of ATF4 via its C-terminal region.
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein. Note=Colocalizes with ATF4 in hippocampal neuron dendritic membranes (By similarity). Moreover coexpression of GABA-B-R1 and GABA-B-R2 appears to be a prerequisite for maturation and transport of GABA-B-R1 to the plasma membrane. & Isoform 1E: Secreted (Probable).
TISSUE SPECIFICITY: Highly expressed in brain and weakly in heart, small intestine and uterus. Mostly expressed in granular cell and molecular layer for isoform 1A and in Purkinje cells form isoform 1B. Isoform 1E is predominantly expressed in peripheral tissues as kidney, lung, trachea, colon, small intestine, stomach, bone marrow, thymus and mammary gland.
DOMAIN: SwissProt: Q9UBS5 Alpha-helical parts of the C-terminal intracellular region mediate heterodimeric interaction with GABA-B receptor 2. The linker region between the transmembrane domain 3 (TM3) and the transmembrane domain 4 (TM4) probably play a role in the specificity for G-protein coupling.
SIMILARITY: Belongs to the G-protein coupled receptor 3 family. GABA-B receptor subfamily. & Contains 2 Sushi (CCP/SCR) domains.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 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: 1X Hanks' Balanced Salt Solution (HBSS): GIBCO Cat. No. 14175
Radioligand: [3H]-CGP 54626A (American Radiolabeled Chemicals Inc., ART 517)
Wash Buffer: 1X Hanks' Balanced Salt Solution (HBSS): GIBCO Cat. No. 14175
One package contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 5-fold signal:background with 3H-labeled CGP 54626A at 7.5nM.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 5ug/well of GABAB1b Receptor membrane prep. 5 µg/well Signal:Background 6.4 Specific Binding (cpm) 2879
SPECIFICATIONS: 1 unit = 5.0 µg membrane preparation
Bmax: 8.49 pmol/mg
Kd: 1.15 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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