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主要文件

HTS115M

Sigma-Aldrich

ChemiSCREEN Membrane Preparation Recombinant Human M2 Muscarinic Acetylcholine Receptor

Human M2 GPCR membrane prepation for Radioligand binding Assays.

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S922331-50MG
¥165.79

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S922331-50MG
¥165.79

About This Item

UNSPSC代码:
41106514
eCl@ss:
32161000
NACRES:
NA.41

¥165.79


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生物来源

human

质量水平

重组

expressed in Chem-1 cells

制造商/商品名称

ChemiScreen
Chemicon®

技术

radioligand binding assay (RLBA): suitable

UniProt登记号

运输

dry ice

基因信息

human ... CHRM2(1129)

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107021PHR121990872
Acetone for analysis EMSURE® ACS,ISO,Reag. Ph Eur

100014

Acetone

Acetone for analysis EMPARTA® ACS

107021

Acetone

Acetone Pharmaceutical Secondary Standard; Certified Reference Material

PHR1219

Acetone

Acetone analytical standard

90872

Acetone

grade

ACS reagent, for extraction, for analytical purposes, reagent grade

grade

ACS reagent, for analytical purposes, for extraction, reagent grade

grade

certified reference material, pharmaceutical secondary standard

grade

analytical standard

assay

≥99.8% (GC)

assay

≥99.5% (GC)

assay

-

assay

≥99.5% (GC)

Quality Level

300

Quality Level

200

Quality Level

300

Quality Level

100

application(s)

environmental
food and beverages
industrial qc
pharmaceutical
sample preparation

application(s)

environmental
food and beverages
industrial qc
pharmaceutical
sample preparation

application(s)

pharmaceutical (small molecule)

application(s)

cleaning products
cosmetics
environmental
flavors and fragrances
food and beverages
personal care

form

liquid

form

liquid

form

liquid

form

liquid

vapor density

2 (vs air)

vapor density

2 (vs air)

vapor density

2 (vs air)

vapor density

2 (vs air)

一般描述

Full-length human CHRM2 cDNA encoding M2
The muscarinic acetylcholine receptor (mAChR) family consists of five GPCRs that mediate some of the neurotransmission functions of acetylcholine in the CNS and the periphery. The M1, M3 and M5 receptors couple to Gq to mobilize intracellular calcium, whereas the M2 and M4 receptors couple to Gi/o to inhibit cAMP production (Caulfield and Birdsall, 1998). In urinary bladder trachea and stomach, M2 augments the function of M3 in promoting contractility, and activation of M2 serves to counteract relaxation induced by increased cAMP levels (Ehlert et al., 2005; Wess, 2004). In addition, the ability of mAChR agonists to decrease heart rate appears to be mediated primarily by M2. Agonists of mAChRs induce tremor, hypothermia, corticosterone release, and analgesia; each of these functions is mediated at least in part by M2 (Wess, 2004). Chemicon′s M2 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 M2 interactions with its ligands. The membrane preparations exhibit a Kd of 0.24 nM for [3H]-Scopolamine methyl chloride (NMS). With 10 µg/well M2 Membrane Prep and 0.5 nM [3H]-NMS, greater than 3-fold signal-to-background ratio was obtained.

生化/生理作用

Protein Target: M2

质量

Table 1. Signal:background and specific binding values obtained in a competition binding assay with M2 membrane prep and unlabeled Atropine.
10 µg/well
Signal:Background 3.2
Specific Binding (cpm) 606.8
SPECIFICATIONS: 1 unit = 10 µg
Bmax for [3H]-NMS binding: 0.5 pmol/mg protein
Kd for [3H]-NMS binding: ~0.24 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, an FC 96-well harvest plate (Millipore cat. # MAHF C1H) is coated with 0.33% polyethyleneimine for 30 min, then washed with 4mM Na2HPO4, 1mM KH2PO4, pH7.4. 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 and Wash buffer: 4mM Na2HPO4, 1mM KH2PO4, pH7.4, filtered and stored at 4&degC Radioligand: [3H] NMS (Perkin Elmer#:NEX-636 ) One package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 3-fold signal:background with 3H-labeled NMS at 0.5 nM

外形

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

法律信息

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

储存分类代码

12 - Non Combustible Liquids

WGK

WGK 2


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    Frederick J Ehlert et al.
    The Journal of pharmacology and experimental therapeutics, 313(1), 368-378 (2004-12-21)
    We investigated the contractile role of M2 muscarinic receptors in mouse urinary bladder. When measured in the absence of other agents, contractions elicited to the muscarinic agonist oxotremorine-M exhibited properties consistent with that expected for an M3 response in urinary
    International Union of Pharmacology. XVII. Classification of muscarinic acetylcholine receptors.
    M P Caulfield et al.
    Pharmacological reviews, 50(2), 279-290 (1998-07-02)
    Muscarinic acetylcholine receptor knockout mice: novel phenotypes and clinical implications.
    Wess, Jurgen
    Annual Review of Pharmacology and Toxicology, 44, 423-450 (2004)

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