Purified Membrane Proteins
CALIXAR’s A2A GPCR (Adenosine receptor A2A) aids in the discovery, development, and validation of new molecules as well as therapeutic antibodies. They are ideal for CNS neuroprotection in order to develop new treatments for insomnia, pain, depression, Alzheimer and Parkinson’s diseases.
A2A Adenosine receptors are powerful therapeutic targets especially found in the treatment of such conditions as insomnia, pain, depression, and Parkinson’s disease.
This class A GPCR is involved in the regulation of myocardial blood flow/hypertension. This protein has a N-terminal Step tag II and an 8X His tag followed by a TEV protease cleavage site.
Target name: Adenosine receptor (A2A receptor)
Catalogue number: PP1
Class: GPCR Class A
Sequence: Full-length, wildtype sequence, with a N-terminus Strep tag II, 8xHis-tag, and TEV
protease cleavage site.
Affinity Tag: His/Strep (both N-terminal)
Origin: Human (Homo sapiens)
Theor. MW: 47,7kDa
Accession #: P29274 (UniProt)
Shipment temperature: Dry Ice
Storage conditions: Store at -80°C
Expression system: Sf9 insect cells (baculovirus)
Purification: Immobilized Metal Affinity Chromatography
Activity: Confirmed by radiobinding assay
Concentration: Up to 5mg/ml
Sample buffer: 50mM Hepes pH 7.4, 200mM NaCl, 0.05%/0.006% DDM/CHS
Available quantity: From 10µg up to mg scale
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Why choose us?
CALIXAR’s A2A GPCR Adenosine receptors facilitate reliable fragment-based drug design (FBDD), structure-based drug discovery (SBDD) and antibody discovery corresponding to this specific target.
Unlike CALIXAR’s A2A Adenosine receptors, other alternative methods result in an adenosine receptor that becomes mutated and truncated (96 amino-acids truncation in the C-terminus). Additionally, this mutated version becomes locked within an antagonist conformation.
As with all GPCRs, the A2A Adenosine receptor is an unstable target and is difficult to produce natively with conventional approaches. Previously, A2A Adenosine receptors could only be locked in one specific conformation (e.g. antagonist) and were only ever prepared in a solution that inherently could not be pure, nor native (truncated, mutated) and without PTMs. A2A’s have only ever been inherently unstable, but not anymore.
Today, CALIXAR’s A2A receptors are able to bind to agonists, antagonists, as well as allosteric modulators (Igonet S. et al., 2018, Scientific Reports). Our A2A receptors also maintain their structural and functional integrity and are purified and stabilized to full length and wild-type (native) proteins.
CALIXAR’s A2A Adenosine receptor is the first native full-length and functional target on the market. Other existing A2A targets are either mutated or truncated. Our A2A protein is produced in a eukaryotic system with the proper post-translational modifications (glycosylation).
CALIXAR’s A2A Adenosine receptors are high-quality membrane proteins used for (bio)drug discovery and are adapted for use in pharmaceutical, biotechnology companies, and as well as for academic teams that are involved in the life science fields.
Igonet S et al. 2018
Discovery on Target
Jawhari A. Boston, 2015
Desuzinges Mandon E. et al. 2017