HEK293 Mouse A2AR Stable Cell
Item | Cat# | Price |
Stable Cell Line | SNB-G-0019B | $19,800 |
Compound Testing Services | CT-001 | $1,850 per 384w plate (Up To 16 cpds Dose) |
Product Description
Adenosine receptors are a family of G-protein-coupled receptors (GPCRs) that mediate the physiological effects of the endogenous nucleoside adenosine. Four subtypes have been identified: A1, A2A, A2B, and A3, each with distinct tissue distribution and signaling profiles. A1 and A3 receptors primarily couple to Gi proteins, inhibiting adenylate cyclase and reducing intracellular cAMP, whereas A2A and A2B receptors couple to Gs proteins, stimulating adenylate cyclase and elevating cAMP levels. Through these pathways, adenosine receptors regulate diverse biological processes including cardiovascular function, neuronal activity, immune response, and inflammation. For example, A1 receptor activation promotes cardioprotection and neuromodulation, while A2A receptors play a critical role in vasodilation and immune suppression. Dysregulation of adenosine receptor signaling has been implicated in conditions such as ischemia, neurodegenerative disorders, asthma, and cancer, making them attractive targets for therapeutic intervention across multiple disease areas.
Screeningbio‘s mouse A2AR cell line stable express non-tag full length mouse A2A receptor in HEK293 cell. When activated, mouse A2AR cell response to extracellular stimuli and result in activation of Gs protein, increasing of intracellular cAMP level.
Product Specifications
Target Type | GPCR |
Species | Mouse |
HGNC Symbol | A2AR |
Accession Number | NM_009630 |
Parental Line | HEK293 |
Lot# | See Vial |
Storage | Liquid Nitrogen |
Data
![A2AR Antagonist Assay. HEK293/Mouse A1R cells were treated with the reference antagonist DPCPX, Rolofylline and FK-453. The assay was run based on Revvity cAMP HTRF protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.](https://static.wixstatic.com/media/56275b_7a28766419274a5bb76acfd4bcc5d1ab~mv2.png/v1/fill/w_75,h_75,al_c,q_85,usm_0.66_1.00_0.01,blur_2,enc_auto/56275b_7a28766419274a5bb76acfd4bcc5d1ab~mv2.png)
Target Background
The adenosine receptors (ARs) are a family of class A G-protein-coupled receptors (GPCRs) that mediate the physiological and pharmacological actions of the endogenous nucleoside adenosine. Four subtypes have been identified: A₁, A₂A, A₂B, and A₃. These receptors are widely distributed throughout the body, with subtype-specific patterns in the central nervous system, cardiovascular system, lungs, kidneys, and immune cells. Their broad distribution underlies diverse roles in neuromodulation, cardiac rhythm regulation, vasodilation, inflammation, and immune responses.
Adenosine receptors couple to different G-proteins depending on subtype. A₁ and A₃ receptors predominantly couple to Gi/o proteins, leading to inhibition of adenylate cyclase and reduced intracellular cAMP, whereas A₂A and A₂B receptors couple to Gs proteins, stimulating adenylate cyclase and elevating cAMP. Additional pathways involve modulation of ion channels, MAPK signaling, and phospholipase C, contributing to tissue- and context-dependent effects. For example, A₁ receptor activation in the CNS suppresses excitatory neurotransmission, while A₂A receptor activity in the striatum modulates dopaminergic signaling and motor control.
Pharmacologically, adenosine receptors are important therapeutic targets across multiple disease areas. A₂A receptor antagonists have been approved for Parkinson’s disease (e.g., istradefylline), while A₁ receptor agonists and antagonists are under exploration for cardiac arrhythmias and chronic kidney disease. A₂B and A₃ receptors have been implicated in asthma, pulmonary fibrosis, cancer, and inflammatory disorders, with selective ligands progressing in clinical development. With their central role in regulating neurotransmission, cardiovascular function, and immune homeostasis, adenosine receptors represent a versatile and expanding area of drug discovery.