A2AR, active

Background Information:

The adenosine A2A receptor (A2AR) is a class A GPCR central to purinergic signaling, activated by extracellular adenosine to regulate diverse physiological processes. Upon ligand binding, A2AR couples to Gαs, stimulating adenylyl cyclase and increasing intracellular cAMP, which activates downstream effectors such as PKA. Through this pathway, A2AR modulates neurotransmission, motor control, and cardiovascular vasodilation.
Because of its broad regulatory roles, A2AR is a major target in therapeutic development, particularly for small molecule agonists and antagonists. Extensive structural and pharmacological characterization has made A2AR one of the best studied GPCRs, enhancing its value in drug discovery. In the CNS, A2AR is implicated in neurodegenerative diseases, with antagonists already used clinically for Parkinson’s disease and growing interest in its involvement in Alzheimer’s disease and related disorders. A2AR also contributes to vascular tone and vasodilation, reinforcing its importance in cardiovascular physiology.
Our recombinant full length A2AR is produced in a eukaryotic expression system to preserve native folding and physiologically relevant post translational modifications, including glycosylation. The purified receptor maintains structural and functional integrity and is stabilized in its full-length, wild-type configuration. For efficient purification and versatility in downstream applications, the construct includes an N terminal Strep tag II and an 8×His tag followed by a TEV protease cleavage site, enabling optional tag removal. This high quality A2AR preparation is an excellent reagent for biochemical, structural, and pharmacological studies, supporting ligand screening, antibody discovery, and mechanistic research.

Target Class:

GPCR

Sub Family:

Class A

Protein Name:

A2AR

Protein Aliases:

ADORA2A

Accession Number:

P29274

UniProt Number:

P29274

Gene Name:

ADORA2A

Gene ID:

135

Gene Aliases:

A2aR; RDC8; ADORA2

Target Species:

Human