ChemiScreen™ Membrane Preparation Human Recombinant d (delta)

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ChemiScreen™ Membrane Preparation Human Recombinant d (delta)

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货号：HTS100M

品牌：Millipore 密理博

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北京朝阳

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EA (预计3-5工作日到货)

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Replacement Information

重要规格表

Species	Host Cells	Protein Target
Human	Chem-1	Delta / OP1 / DOP / DOR

Description
Catalogue Number	HTS100M
Brand Family	Chemicon®
Trade Name	ChemiScreen Chemicon
Description	ChemiSCREEN™ Human δ Opioid Receptor Membrane Preparation
Overview	Full-length human OPRD1 cDNA encoding δ opioid receptor
Background Information	Opiates 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, δ, κ, and μ (also known as OP1, OP2 and OP3, resepctively), that activate Gi/o to reduce intracellular cAMP levels. Although most clinically used opioids function by activation of the µ opioid receptor, agonits of spinal δ opioid receptors have antinociceptive activity that is independent of µ. In addition, activation of δ increases locomotor activity, inhibits gastrointestinal motility, and decreases respiratory frequency (Dhawan et al., 1996). Agonists for δ opioid receptors also exhibit antidepressant-like activity in animal models (Broom et al., 2002). Chemicon's δ 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 agonists and antagonists at δ. The membrane preparations exhibit a Kd of 1.12 nM for [3H]-DADLE. With 0.9 nM [3H]-DADLE, 10 µg/well δ Membrane Prep typically yields greater than 4-fold signal-to-background ratio.

References

Product Information
Format	Membranes
Presentation	One package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 4-fold signal:background with 3H-labeled DADLE at 0.9 nM Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives. Packaging method: Membranes protein were adjusted to 1 mg/mL in packaging buffer, and dispensed at 1 mL/vial. Vials were rapidly frozen, and stored at -80°C.

Product Information

Format

Membranes

Presentation

One package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 4-fold signal:background with 3H-labeled DADLE at 0.9 nM

Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
Packaging method: Membranes protein were adjusted to 1 mg/mL in packaging buffer, and dispensed at 1 mL/vial. Vials were rapidly frozen, and stored at -80°C.

Applications
Application	Human Delta / OP1 / DOP / DOR GPCR membrane preparation for Radioligand binding Assays & GTPγS.
Key Applications	Radioligand binding assay GTPγS binding
Application Notes	Radioligand binding assay and GTPγS

Biological Information
Entrez Gene Number	NM_000911.3
Gene Symbol	OPRD1 OPRD DOR-1
GPCR Class	A
Host Cells	Chem-1
Protein Target	Delta / OP1 / DOP / DOR
Target Sub-Family	Opioid
UniProt Number	P41143
UniProt Summary	FUNCTION: SwissProt: P41143 # Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective. receptor for enkephalins. SIZE: 372 amino acids; 40413 Da SUBUNIT: Interacts with GPRASP1. SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein. SIMILARITY: SwissProt: P41143 ## Belongs to the G-protein coupled receptor 1 family.
Incubation Conditions	Membranes 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, an FC 96-well harvest plate (Millipore cat. # MAHF C1H) is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM Tris-HCl. 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 Tris-HCl, filtered and stored at 4°C Radioligand: [3H] DADLE (Perkin Elmer#: NET-648) Wash Buffer: 50 mM Tris-HCl, filtered and stored at 4°C.

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Table 1. Signal:background and specific binding values obtained in a competition binding assay with δ membrane prep and unlabeled DPDPE.

Product Usage Statements

	10 µg/well
Signal:Background	7.32
Specific Binding (cpm)	955

SPECIFICATIONS: 1 unit = 10 µg
Bmax for [3H] DADLE binding: 11.6 pmol/mg protein
Kd for [3H] DADLE binding: ~1.12 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 Conditions	Store at –70°C. Product is stable for at least 6 months from the date of receipt when stored as directed. Do not freeze and thaw.