Accéder au contenu
Merck
Toutes les photos(2)

Key Documents

HTS034M

Sigma-Aldrich

ChemiSCREEN NTR1 Membrane Preparation

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

Se connecterpour consulter vos tarifs contractuels et ceux de votre entreprise/organisme


About This Item

Code UNSPSC :
41106514
eCl@ss :
32161000
Nomenclature NACRES :
NA.84

Source biologique

human

Niveau de qualité

Produit recombinant

expressed in Chem-2 cells

Fabricant/nom de marque

ChemiScreen
Chemicon®

Concentration

0.5 mg/mL

Technique(s)

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

Numéro d'accès NCBI

Numéro d'accès UniProt

Conditions d'expédition

dry ice

Description générale

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.

Application

Radioligand binding assay, and GTPgammaS binding.

Actions biochimiques/physiologiques

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

Qualité

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

Caractéristiques

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.

Forme physique

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.

Stockage et stabilité

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

Informations légales

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

Clause de non-responsabilité

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.

Code de la classe de stockage

12 - Non Combustible Liquids

Classe de danger pour l'eau (WGK)

WGK 2

Point d'éclair (°F)

Not applicable

Point d'éclair (°C)

Not applicable


Certificats d'analyse (COA)

Recherchez un Certificats d'analyse (COA) en saisissant le numéro de lot du produit. Les numéros de lot figurent sur l'étiquette du produit après les mots "Lot" ou "Batch".

Déjà en possession de ce produit ?

Retrouvez la documentation relative aux produits que vous avez récemment achetés dans la Bibliothèque de documents.

Consulter la Bibliothèque de documents

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)
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.
Neurotensin, schizophrenia, and antipsychotic drug action
Kinkead, Becky and Nemeroff, Charles B
International Review of Neurobiology, 59, 327-349 (2004)
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

Notre équipe de scientifiques dispose d'une expérience dans tous les secteurs de la recherche, notamment en sciences de la vie, science des matériaux, synthèse chimique, chromatographie, analyse et dans de nombreux autres domaines..

Contacter notre Service technique