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Figure 1. Saturation binding for A1. 5 µg/well A1 Membrane Preparation was incubated with increasing amount of 3H-l ...

Figure 2. Competition binding for A1. 10 µg/well A1 Membrane Preparation (A1; HTS047M) and wild type Chem-3 Membra ...

ChemiScreen™ A1 Membrane Preparation


Description:
ChemiScreen™ A1 Membrane Preparation
Trade Name:
ChemiScreen
Background Information:
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.
Application Notes:
Radioligand binding assay and GTPγS binding.
Species Reactivity:
Human
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.
Concentration:
1 mL, 0.5 mg/mL
Cell Type:
Chem-3
Gene Symbol:
  • ADORA1
  • RDC7
Presentation:
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.
Protein or Enzyme Type:
Membrane Preparations
Storage Conditions:
Maintain frozen at -70°C for up to 2 years. Do not freeze and thaw
Species:
Human