推荐产品
生物源
human
品質等級
重組細胞
expressed in Chem-2 cells
製造商／商標名
ChemiScreen
Chemicon®
濃度
0.5 mg/mL
技術
ligand binding assay: suitable (GTPγS)
radioligand binding assay (RLBA): suitable
NCBI登錄號
UniProt登錄號
運輸包裝
dry ice
一般說明
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.
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.
應用
Radioligand binding assay, and GTPgammaS binding.
生化／生理作用
GPCR Class: A
Protein Target: NTR1 / NTS1
Target Sub-Family: Neurotensin
品質
Signal:background and specific binding values obtained in a competition binding assay with NTR1 membrane prep:
SPECIFICATIONS: 1 unit = 5 µg
Bmax: 12.9 pmol/mg
Kd: 1.5 nM
| 5 µg/well | |
|---|---|
| Signal:Background | 47 |
| Specific Binding (cpm) | 17556 |
SPECIFICATIONS: 1 unit = 5 µg
Bmax: 12.9 pmol/mg
Kd: 1.5 nM
規格
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.
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.
外觀
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.
儲存和穩定性
Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw.
法律資訊
CHEMICON is a registered trademark of Merck KGaA, Darmstadt, Germany
免責聲明
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.
儲存類別代碼
12 - Non Combustible Liquids
水污染物質分類（WGK）
WGK 2
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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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