ChemiScreen™ A1 Membrane Preparation

ChemiScreen™ A1 Membrane Preparation

• ChemiScreen
• Chemicon (Millipore)

200 units

Extracellular adenosine mediates a multitude of biological effects, including wakefulness, antiarrythmia, bronchoconstriction and response to ischemia and oxidative stress. A family of four GPCR adenosine receptors, A1, A2A, A2B and A3, is responsible for these effects. The A1 receptor, which couples to Gi/o, is most highly expressed in brain, and mediates endogenous antinociception and neuronal response to hypoxia (Fredholm et al., 2001). A1 is also expressed in kidney, where it contributes to tubuloglomerular feedback. Chemicon's cloned human A1-expressing cell line is made in the Chem-3 host, which supports high levels of recombinant A1 expression on the cell surface and contains high levels of the 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 A1 and its ligands.

Chemicon's A1 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 A1 interactions with its ligands. The membrane preparations exhibit a Kd of 1.2 nM for [3H]-Cyclopentyl-1, 3-dipropylxanthine, 8-[dipropyl-2, 3-3H (N)]. With 5mg/well A1 Membrane Prep and 20nM [3H]-DPCPX, a greater than 6-fold signal-to-background ratio is obtained.

Radioligand binding assay and GTPγS binding.

Human

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.

The protein encoded by this gene is an adenosine receptor that belongs to the G-protein coupled receptor 1 family. There are 3 types of adenosine receptors, each with a specific pattern of ligand binding and tissue distribution, and together they regulate a diverse set of physiologic functions. The type A1 receptors inhibit adenylyl cyclase, and play a role in the fertilization process. Animal studies also suggest a role for A1 receptors in kidney function and ethanol intoxication. Transcript variants with alternative splicing in the 5' UTR have been found for this gene.

FUNCTION: SwissProt: P30542 # Receptor for adenosine. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase.
SIZE: 326 amino acids; 36512 Da
SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
SIMILARITY: SwissProt: P30542 ## Belongs to the G-protein coupled receptor 1 family.

Human

Chem-3

Chemicon

Chem-3

Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA no preservatives.Packaging method: Membranes protein were adjusted to the indicated concentration in packaging buffer, rapidly frozen, and stored at -80°C.

A1

P30542

non-peptide

Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw

Adenosine

For special offers Click here http://www.millipore.com/drugdiscovery/dd3/gpcrtargetsolutions

A

• ADORA1
• RDC7

GPCR Membrane Preparations

ChemiScreen™ A1 Membrane Preparation

• NM_000674.2
• NM_001048230.1

1 mL, 0.5 mg/mL

GPCR