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HTS034M ChemiSCREEN™ NTR1 Membrane Preparation

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

ChemiSCREEN™ NTR1 Membrane Preparation MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-2 Uni Prot Number: P30989 Entrez Gene Number: NM_002531.2
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HTS034M
200 assays  
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Overview

Replacement Information

Key Spec Table

SpeciesHost CellsProtein Target
Human Chem-2NTR1 / NTS1
Description
Catalogue NumberHTS034M
Brand Family Chemicon®
Trade Name
  • ChemiScreen
  • Chemicon
DescriptionChemiSCREEN™ NTR1 Membrane Preparation
OverviewHuman NTR1
Background InformationNeurotensin 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.
References
Product Information
FormatMembranes
PresentationPACKAGING: 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.
Quality LevelMQ100
Applications
ApplicationHuman NTR1 / NTS1 GPCR membrane preparation for Radioligand binding Assays & GTPgammaS binding.
Key Applications
  • Radioligand binding assay
  • GTPγS binding
Application NotesRadioligand binding assay, and GTPgammaS binding.
Biological Information
Concentration0.5 mg/mL
Entrez Gene Number
Entrez Gene SummaryNeurotensin receptor 1 belongs to the large superfamily of G-protein coupled receptors. NTSR1 mediates the multiple functions of neurotensin, such as hypotension, hyperglycemia, hypothermia, antinociception, and regulation of intestinal motility and secretion.
Gene Symbol
  • NTSR1
  • NTRR
  • NT-R-1
  • NTRH
  • NTR
GPCR ClassA
Host CellsChem-2
Protein TargetNTR1 / NTS1
Target Sub-FamilyNeurotensin
UniProt Number
UniProt SummaryFUNCTION: SwissProt: P30989 # Receptor for the tridecapeptide neurotensin. It is associated with G proteins that activate a phosphatidylinositol- calcium second messenger system.
SIZE: 418 amino acids; 46259 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
SIMILARITY: SwissProt: P30989 ## Belongs to the G-protein coupled receptor 1 family.
Incubation ConditionsBinding 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.
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Signal:background and specific binding values obtained in a competition binding assay with NTR1 membrane prep:
Product Usage Statements
5 µg/well
Signal:Background 47
Specific Binding (cpm) 17556


SPECIFICATIONS: 1 unit = 5 µg
Bmax: 12.9 pmol/mg
Kd: 1.5 nM Usage Statement
  • 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.
Storage and Shipping Information
Storage ConditionsMaintain frozen at -70°C for up to 2 years. Do not freeze and thaw.
Packaging Information
Material Size200 assays
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
HTS034M 04053252287916

Documentation

Protocols

Title
Assembly of a Competition Binding Curve

ChemiSCREEN™ NTR1 Membrane Preparation MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overviewPub Med ID
Neurotensin, schizophrenia, and antipsychotic drug action
Kinkead, Becky and Nemeroff, Charles B
Int Rev Neurobiol, 59:327-49 (2004)  2004

15006494 15006494
The effects of deleting the mouse neurotensin receptor NTR1 on central and peripheral responses to neurotensin
Pettibone, Douglas J, et al
J Pharmacol Exp Ther, 300:305-13 (2002)  2002

11752130 11752130
Neurotensin is a proinflammatory neuropeptide in colonic inflammation
Castagliuolo, I, et al
J Clin Invest, 103:843-9 (1999)  1999

10079105 10079105
Mutagenesis and modeling of the neurotensin receptor NTR1. Identification of residues that are critical for binding SR 48692, a nonpeptide neurotensin antagonist
Labbé-Jullié, C, et al
J Biol Chem, 273:16351-7 (1998)  1998

9632698 9632698

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