Millipore Sigma Vibrant Logo
Attention: We have moved. Merck Millipore products are no longer available for purchase on MerckMillipore.com.Learn More

HTS060M ChemiScreen™ Human V2 Vasopressin Receptor Membrane Preparation

Human V2 GPCR membrane preparation for Radioligand binding Assays & GTPγS binding.

ChemiScreen™ Human V2 Vasopressin 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: P30518 Entrez Gene Number: NM_000054.2
HTS060M
200 units  
Purchase on Sigma-Aldrich

Áttekintés

Replacement Information

Kulcsspecifikációk táblázata

SpeciesHost CellsProtein Target
Human Chem-1V2
Description
Catalogue NumberHTS060M
Brand Family Chemicon®
Trade Name
  • ChemiScreen
  • Chemicon
DescriptionChemiScreen™ Human V2 Vasopressin Receptor Membrane Preparation
OverviewTRANSFECTION: Full-length human AVPR2 cDNA encoding V2
Background InformationArginine vasopressin (AVP) is a 9 amino acid peptide that functions as an antidiuretic, vasoconstrictor and neurotransmitter. The three vasopressin receptors, V1a, V1b and V2, are GPCRs; V1a and V1b couple to Gq and calcium release, whereas V2 couples to Gs. V2 expressed in renal collecting ducts plays an important role in regulating renal free water excretion (Birnbaumer, 2000). Mutations in V2 result in X-linked nephrogenic diabetes insipidus, a syndrome in which the kidney is unable to concentrate urine, leading to dehydration and hypernatremia (Birnbaumer, 2001). Conversely, elevated levels of AVP lead to hyponatremia in the syndrome of inappropriate antidiuretic hormone secretion (SIADH), congestive heart failure or cirrhosis, and V2 selective antagonists have been developed to treat these conditions (Verbalis, 2002). Chemicon's V2 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 V2 interactions and its ligands. The membrane preparations exhibit a Kd of 2.83 nM for [3H]-[Arg8] Vasopressin. With 3.5 nM [3H]-[Arg8] Vasopressin, 10 μg/well V2 Membrane Prep yields greater than 8-fold signal-to-background ratio.
References
Product Information
FormatMembranes
PresentationLiquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA no preservatives.
Packaging method: Membranes protein were adjusted to 0.5 mg/ml in 1 ml packaging buffer, rapidly frozen, and stored at -80°C.
Quality LevelMQ100
Applications
ApplicationHuman V2 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
Concentration4mL; 0.5 mg/mL
Entrez Gene Number
Entrez Gene SummaryThis gene encodes the vasopressin receptor, type 2, also known as the V2 receptor, which belongs to the seven-transmembrane-domain G protein-coupled receptor (GPCR) superfamily, and couples to Gs thus stimulating adenylate cyclase. The subfamily that includes the V2 receptor, the V1a and V1b vasopressin receptors, the oxytocin receptor, and isotocin and mesotocin receptors in non-mammals, is well conserved, though several members signal via other G proteins. All bind similar cyclic nonapeptide hormones. The V2 receptor is expressed in the kidney tubule, predominantly in the distal convoluted tubule and collecting ducts, where its primary property is to respond to the pituitary hormone arginine vasopressin (AVP) by stimulating mechanisms that concentrate the urine and maintain water homeostasis in the organism. When the function of this gene is lost, the disease Nephrogenic Diabetes Insipidus (NDI) results. The V2 receptor is also expressed outside the kidney although its tissue localization is uncertain. When these 'extrarenal receptors' are stimulated by infusion of a V2 selective agonist (dDAVP), a variety of clotting factors are released into the bloodstream. The physiologic importance of this property is not known - its absence does not appear to be detrimental in NDI patients. The gene expression has also been described in fetal lung tissue and lung cancer associated with alternative splicing.
Gene Symbol
  • AVPR2
  • DI1
  • V2R
  • MGC126533
  • DIR
  • DIR3
  • ADHR
  • NDI
  • MGC138386
GPCR ClassA
Host CellsChem-1
Protein TargetV2
Target Sub-FamilyVasopressin
UniProt Number
UniProt SummaryFUNCTION: SwissProt: P30518 # Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase.
SIZE: 371 amino acids; 40279 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
TISSUE SPECIFICITY: Kidney.
DISEASE: SwissProt: P30518 # Defects in AVPR2 are the cause of nephrogenic syndrome of inappropriate antidiuresis (NSIAD) [MIM:300539]. This disorder is characterized by an inability to excrete a free water load, with inappropriately concentrated urine and resultant hyponatremia, hypoosmolarity, and natriuresis. & Defects in AVPR2 are a cause of X-linked nephrogenic diabetes insipidus, type I (NDI) [MIM:304800]. It is characterized by excessive water drinking (polydypsia) and urine excretion (polyuria) and fail to concentrate urine in response to vasopressin. Most cases of NDI appear to have an X-linked recessive pattern of inheritance.
SIMILARITY: SwissProt: P30518 ## 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: [3H]-[Arg8] Vasopressin (Perkin Elmer#:NET-800 )

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 a unit is the amount of membrane that will yield greater than 8-fold signal:background with 3H labeled [Arg8] Vasopressin at 3.5 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 V2 membrane prep:
Product Usage Statements
10 µg/well
Signal:Background 10.5
Specific Binding (cpm) 1972


SPECIFICATIONS: 1 unit = 10 μg

Bmax for [3H]-[Arg8] Vasopressin binding: 18.3 pmol/mg protein;

Kd for [3H]-[Arg8] Vasopressin binding: ~ 2.83 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
Katalógusszám GTIN
HTS060M 04053252402319

Documentation

ChemiScreen™ Human V2 Vasopressin Receptor Membrane Preparation MSDS

Title

Safety Data Sheet (SDS) 

References

Reference overviewPub Med ID
Vasopressin V2 receptor antagonists.
Verbalis, J G
J. Mol. Endocrinol., 29: 1-9 (2002)  2002

Kivonat megmutatása 		12200224 12200224
The V2 vasopressin receptor mutations and fluid homeostasis.
Birnbaumer, M
Cardiovasc. Res., 51: 409-15 (2001)  2001

Kivonat megmutatása 		11476731 11476731
Vasopressin receptors.
Birnbaumer, M
Trends Endocrinol. Metab., 11: 406-10 (2000)  1999

Kivonat megmutatása 		11091117 11091117

Kapcsolódó termékek és alkalmazások

Product Families

ChemiSCREEN™ GPCR Stable Cell Lines, Membranes Preparation and Ready-to-Assay™ Frozen Cells

Millipore offers a large selection of robust and reliable G-protein coupled receptor products, including Stable Cell Lines, Membrane Preparations, and Frozen Cells. See below for GPCR research tools.
További információk >>

Kapcsolódó termékek gyártója: Brand Facete

ChemiScreen™

Kategóriák

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