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ChemiSCREEN Human 5-HT2C Receptor Membrane Preparation

品牌
Sigma-Aldrich
货号
HTS132M
规格纯度
Human 5-HT2C GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
参考价格
10533.9 *本价格含增值税费
促销
数量
-+
产品介绍:

产品说明

一般描述

5-Hydroxytryptamine (5-HT, also commonly known as serotonin) is synthesized in enterochromaffin cells in the intestine and in serotonergic nerve terminals. In the periphery, 5-HT mediates gastrointestinal motility, platelet aggregation, and contraction of blood vessels. Many functions of the central nervous system are influenced by 5-HT, including sleep, motor activity, sensory perception, arousal and appetite. A family of 12 GPCRs and one ion channel mediate the biological effects of 5-HT (Hoyer et al., 1994). 5-HT2C, which couples to Gq in most cells to stimulate intracellular calcium, is prominently expressed in brain and appears to modulate depression, anxiety and appetite (Miller, 2005; Serretti et al., 2004; Wood, 2003). The mRNA encoding 5-HT2C undergoes selective RNA editing that changes 4 amino acids in the second intracellular loop; these changes result in alteration of efficiency of coupling to G proteins. Alterations in editing of 5-HT2C have been detected in victims of suicidal depression and in mice treated with the SSRI, fluoxetine (Tohda et al., 2006). Millipore′′s 5-HT2C 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 5-HT2C interactions and its ligands. The membrane preparations exhibit a Kd of 5.9 nM for [3H]-mesulergine. With 6 nM [3H]- Mesulergine, 10 µg/well 5-HT2C Membrane Prep yields greater than 5 fold signal-to-background ratio.
Human 5-HT2C

应用

Radioligand binding assay and GTPγS binding.

生化/生理作用

Target Sub-Family: Serotonin
GPCR Class: A
Protein Target: 5-HT2C

质量

Signal:background and specific binding values obtained in a competition binding assay with varying amounts of 5-HT2C membrane prep:

10 µg/well
Signal:Background 7.8
Specific Binding (cpm) 2433


SPECIFICATIONS: 1 unit = 10 µg membrane preparation
Bmax: 15.66 pmol/mg
Kd: 5.9 nM

产品规格

Inucbation Conditions
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, a GF/C 96-well filter plate is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM HEPES, 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 Hepes, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, filtered and stored at 4°C
Radioligand: [3H]-Mesulergine (Amersham TRK 845)
Wash Buffer: 50 mM Hepes, pH 7.4, 500mM NaCl, filtered and stored at 4°C.

外形

Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives. Packaging method: Membrane protein was adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.

储存及稳定性

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.

法律信息

CHEMICON is a registered trademark of Merck KGaA, Darmstadt, Germany

免责声明

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.

基本信息

eCl@ss32161000
NACRESNA.84

产品性质

质量水平100
生物来源human
重组expressed in Chem-1 cells
manufacturer/tradenameChemiScreen
Chemicon®
technique(s)ligand binding assay: suitable (GTPγS)
radioligand binding assay (RLBA): suitable
NCBI登记号NM_000868.1
UniProt登记号P28335
运输dry ice
Gene Informationhuman ... HTR2C(3358)

安全信息

储存分类代码12 - Non Combustible Liquids
WGKWGK 2
闪点(F)Not applicable
闪点(C)Not applicable

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