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HTS101M CHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN µ (Mu) OPIOID RECEPTOR

Human Mu / OP3 / MOP / MOR GPCR membrane preparation for GTPγS Binding & Radioligand Binding Assays.

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Host Cell: Chem-5 Uni Prot Number: P35372 Entrez Gene Number: NM_000914.2, NM_001008503.1, NM_001008504.1, NM_001008505.1
HTS101M
200 units  
Purchase on Sigma-Aldrich

Descripción

Tabla espec. clave

SpeciesHost CellsProtein Target
Human Chem-5Mu / OP3 / MOP / MOR
Description
Catalogue NumberHTS101M
Trade Name
  • ChemiScreen
  • Chemicon
DescriptionCHEMISCREEN™ MEMBRANE PREPARATION RECOMBINANT HUMAN µ (Mu) OPIOID RECEPTOR
OverviewFull-length human OPRM1 cDNA encoding Mu
Background InformationOpiates derived from the opium poppy, Papaver somniferum, have been used in for millenia for their anti-diarrheal, analgesic and euphoric properties. More recently, endogenous peptides, enkephalins, dynorphins, and endorphins, were found to bind to the same sites as opiate alkaloids. The receptors for the classical opioids are three related GPCRs, µ κ and δ that activate Gi/o to reduce intracellular cAMP levels. Most clinically used opioids function by activation of the µ opioid receptor (Dhawan et al., 1996). Chemicon's µ opioid receptor 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 µ opioid receptor interactions with its ligands. The membrane preparations exhibit an EC50 of 1.6nM for DAMGO in a GTPγS binding assay.
Product Information
FormatMembranes
PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
Packaging method: Membrane protein was adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C
Quality LevelMQ100
Applications
ApplicationHuman Mu / OP3 / MOP / MOR GPCR membrane preparation for GTPγS Binding & Radioligand Binding Assays.
Key Applications
  • GTPγS binding
  • Radioligand binding assay
Application NotesGTPγS Binding and Radioligand Binding Assay.
Biological Information
Entrez Gene Number
Gene Symbol
  • OPRM1
  • MOR-1
  • MOR1
  • KIAA0403
  • OPRM
GPCR ClassA
Host CellsChem-5
Protein TargetMu / OP3 / MOP / MOR
Target Sub-FamilyOpioid
UniProt Number
UniProt SummaryFUNCTION: SwissProt: P35372 # Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for beta-endorphin.
SIZE: 400 amino acids; 44779 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
SIMILARITY: SwissProt: P35372 ## Belongs to the G-protein coupled receptor 1 family.
Incubation ConditionsASSAY CONDITIONS: Membranes are permeabilized by addition of saponin to an equal concentration by mass, then mixed with [35S]-GTPγS (final concentration of 0.3 nM) in 20 mM HEPES, pH 7.4/100 mM NaCl/10 mM MgCl2/0.5 μM GDP in a nonbinding 96-well plate. Unlabeled DAMGO added to the final concentration indicated in Figure 1 (final volume 100 μL), and incubated for 30 min at 30°C. The binding reaction is transferred to an FB filter plate (Millipore MAHF B1H) previously prewetted with water, and washed 3 times (1 mL per well per wash) with cold 10 mM sodium phosphate, pH 7.4. The plate is dried and counted.

One vial contains enough membranes for at least 200 assays (units), where one unit is the amount of membrane that will yield greater than 1000 cpm specific DAMGO-stimulated [35S]-GTPγS binding.
The μ opioid receptor membrane preparation is expected to be functional in a radioligand binding assay; however, the end user will need to determine the optimal radiolabeled ligand for use with this product.
Product Usage Statements
Quality AssuranceEC50 in GTPγS binding assay by DAMGO: ~ 1.6 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
Global Trade Item Number
Número de referencia GTIN
HTS101M 04053252323010