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HTS034M

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ChemiSCREEN NTR1 Membrane Preparation

Human NTR1 / NTS1 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.

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About This Item

Codice UNSPSC:
41106514
eCl@ss:
32161000
NACRES:
NA.84

Origine biologica

human

Livello qualitativo

Ricombinante

expressed in Chem-2 cells

Produttore/marchio commerciale

ChemiScreen
Chemicon®

Concentrazione

0.5 mg/mL

tecniche

ligand binding assay: suitable (GTPγS)
radioligand binding assay (RLBA): suitable

N° accesso NCBI

N° accesso UniProt

Condizioni di spedizione

dry ice

Descrizione generale

Human NTR1
Neurotensin is a 13 amino acid peptide that induces hypothermia and mediates analgesia when administered centrally, and also mediates the behavioral effects of antipsychotic drugs in rodents (Kinkead and Nemeroff, 2004). In addition, several intestinal functions, such as contractility and inflammation, are mediated by neurotensin (Castagliuolo et al., 1999). The actions of neurotensin are mediated by two GPCRs, NTR1 (or NTS1) and NTR2 (or NTS2). NTR1 knockout mice are resistant to the hypothermic, analgesic and contractile effects of neurotensin, indicating that NTR1 is the primary mediator of these effects (Pettibone et al., 2002). Small molecule antagonists, including SR48692 and SR142948A, that are partially selective for NTR1 also interfere with the biological effects of neurotensin (Labbé-Jullié et al., 1998).

Chemicon′s NTR1 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 neurotensin/NTR1 interactions. The membrane preparations exhibit a Kd of 1.5 nM for [125I]-neurotensin. With 2.5 μg/well NTR1 Membrane Prep and 0.5 nM [125I]-neurotensin, a greater than 7-fold signal-to-background ratio is obtained.

Applicazioni

Radioligand binding assay, and GTPgammaS binding.

Azioni biochim/fisiol

GPCR Class: A
Protein Target: NTR1 / NTS1
Target Sub-Family: Neurotensin

Qualità

Signal:background and specific binding values obtained in a competition binding assay with NTR1 membrane prep:
5 µg/well
Signal:Background 47
Specific Binding (cpm) 17556


SPECIFICATIONS: 1 unit = 5 µg
Bmax: 12.9 pmol/mg
Kd: 1.5 nM

Specifiche

Inucbation Conditions
Binding buffer: 50mM HEPES, 5mM MgCl2, 1mM CaCl2, 0.2% BSA, pH to 7.4 and filter.
Radioligand: [125I] Neurotensin (PerkinElmer#: NEX198)
One vial 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 125I-labeled neurotensin at 0.5 nM.

Stato fisico

PACKAGING: Packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSAPackaging method: Membranes protein were adjusted to 0.5 mg/ml in 1 ml packaging buffer, rapidly frozen, and stored at -80oC.

Stoccaggio e stabilità

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.

Note legali

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

Esclusione di responsabilità

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.

Codice della classe di stoccaggio

12 - Non Combustible Liquids

Classe di pericolosità dell'acqua (WGK)

WGK 2

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


Certificati d'analisi (COA)

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I Castagliuolo et al.
The Journal of clinical investigation, 103(6), 843-849 (1999-03-17)
The neuropeptide neurotensin mediates several intestinal functions, including chloride secretion, motility, and cellular growth. However, whether this peptide participates in intestinal inflammation is not known. Toxin A, an enterotoxin from Clostridium difficile, mediates pseudomembranous colitis in humans. In animal models
Douglas J Pettibone et al.
The Journal of pharmacology and experimental therapeutics, 300(1), 305-313 (2001-12-26)
Mice deficient in the neurotensin (NT)-1 receptor (NTR1) were developed to characterize the NT receptor subtypes that mediate various in vivo responses to NT. F2 generation (C57BL6/Sv129J) NTR1 knockout (-/-) mice were viable, and showed normal growth and overt behavior.
Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist
Labbe-Jullie, C, et al
The Journal of Biological Chemistry, 273, 16351-16357 (1998)
Neurotensin, schizophrenia, and antipsychotic drug action
Kinkead, Becky and Nemeroff, Charles B
International Review of Neurobiology, 59, 327-349 (2004)

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