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HTS121M ChemiSCREEN™ Human Motilin Receptor Membrane Preparation

Human motilin receptor / MTLR / GPR38 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

ChemiSCREEN™ Human Motilin Receptor Membrane Preparation MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-1 Uni Prot Number: O43193 Entrez Gene Number: NM_001507.1
HTS121M
200 units  
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Replacement Information

Tabulka spec. kláve

SpeciesHost CellsProtein Target
Human Chem-1motilin receptor / MTLR / GPR38
Description
Catalogue NumberHTS121M
Brand Family Chemicon®
Trade Name
  • ChemiScreen
  • Chemicon
DescriptionChemiSCREEN™ Human Motilin Receptor Membrane Preparation
OverviewHuman Motilin Receptor
Background InformationMotilin is a 22 amino acid peptide that potently stimulates gastrointestinal contractility. The biological effects of motilin are mediated by a Gq-coupled seven transmembrane protein, currently termed motilin receptor (MR), that shares significant sequence similarity with the ghrelin receptor (Feighner et al., 1999). The motilin receptor is also activated by the antibiotic erythromycin; this interaction appears to mediate some of the gastrointestinal side effects of erythromycin. Although motilides (non-antibiotic derivatives of erythromycin) such as ABT-229 have been investigated for treatment of diabetic gastroporesis, the effectiveness has been limited by tachyphylaxis (decreased response to ligand) resulting from receptor downregulation (Thielemans et al., 2005). Agonists of the motilin receptor with reduced densensitization activity remain a potential treatment for disorders of gastric motility. Chemicon's cloned human Motilin Receptor-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant Motilin Receptor expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between the Motilin Recptor and its ligands. Chemicon's motilin 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 motilin receptor interactions with motilin. The membrane preparations exhibit a Kd of 0.43nM for [125I]-Motilin. With 5.0 µg/well Motilin Membrane Prep and 0.5 nM [125I]-Motilin, a greater than 30-fold signal-to-background ratio was obtained.
References
Product Information
FormatMembranes
PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.
Quality LevelMQ100
Applications
ApplicationHuman motilin receptor / MTLR / GPR38 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.
Key Applications
  • Radioligand binding assay
  • GTPγS binding
Application NotesRadioligand binding assay, and GTPγS binding.
Biological Information
Entrez Gene Number
Gene Symbol
  • MLNR
  • GPR38
  • MTLR
  • MTLR1
GPCR ClassA
Host CellsChem-1
Protein Targetmotilin receptor / MTLR / GPR38
Target Sub-FamilyMotilin
UniProt Number
UniProt SummaryFUNCTION: SwissProt: O43193 # Receptor for motilin.
SIZE: 412 amino acids; 45344 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Expressed only in thyroid, stomach, and bone marrow.
SIMILARITY: SwissProt: O43193 ## Belongs to the G-protein coupled receptor 1 family.
Incubation ConditionsMembranes 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, a GF/C 96-well filter plate is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM HEPES, pH 7.4, 0.5% BSA. 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 buffer: 50 mM Hepes, pH 7.4, 5 mM MgCl2, 1 mM CaCl2, 0.2% BSA, filtered and stored at 4°C
Radioligand: [125I] Motilin (Perkin Elmer # NEX378)
Wash Buffer: 50 mM Hepes, pH 7.4, 500mM NaCl , 0.1% BSA, filtered and stored at 4°C.
One package contains enough membranes for at least 200 assays (units), where an unit is the amount of membrane that will yield greater than 30-fold signal:background with 125I-labeled motilin 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 varying amounts of Motilin Receptor membrane prep:
Product Usage Statements
5 µg/well 10 µg/well
Signal:Background 75 65
Specific Binding (cpm) 46348 54457


SPECIFICATIONS: 1 unit = 5 µg membrane preparation
Bmax: 5.6 pmol/mg
Kd: 0.43 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 units
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Katalogové číslo GTIN
HTS121M 04053252584190

Documentation

ChemiSCREEN™ Human Motilin Receptor Membrane Preparation MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overviewPub Med ID
Desensitization of the human motilin receptor by motilides.
Thielemans, Leen, et al.
J. Pharmacol. Exp. Ther., 313: 1397-405 (2005)  2004

Zobrazit abstrakt 		15764739 15764739
Receptor for motilin identified in the human gastrointestinal system.
Feighner, S D, et al.
Science, 284: 2184-8 (1999)  1998

Zobrazit abstrakt 		10381885 10381885

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Life Science Research > Drug Discovery and Development > GPCR Cell Lines & Assays > GPCR Membrane Preparations
Life Science Research > Proteins and Enzymes > GPCR Membrane Preparations