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HEK293T/Human A3 β-Arrestin Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-A-0021A

Inquiry

Compound Testing Services

CT-001

$1,850 per 384w plate

(Up To 16 cpds Dose)


Product Description


The A3 adenosine receptor (ADORA3) is a Gi-coupled receptor primarily expressed on immune cells (e.g., mast cells), in the CNS (glia), and the eye. It has context-dependent roles, offering anti-inflammatory, cardioprotective, and neuroprotective benefits, but can promote inflammation and apoptosis if overactivated. This makes it a promising yet complex target for treating inflammatory/autoimmune diseases, ischemic injury, and certain cancers.

 

ScreeningBio’s HEK293T/Human A3 β-Arrestin cell line is an ideal tool for studying GPCR/β-arrestin interactions. In this system, the GPCR C-terminus is fused to a smallBiT tag, and the β2-arrestin N-terminus is fused to a largeBiT tag. Upon receptor activation, GPCR/β-arrestin interaction brings the two fragments together to reconstitute an active NanoLuc enzyme, which can be quantified using the NanoBiT substrate. This cell line is designed to evaluate a compound’s ability to activate the β-arrestin signaling pathway. 

Product Specifications

Target Type

GPCR

Species

Human

HGNC Symbol

ADORA3

Accession Number

NM_000677 (Hs)

Parental Line

HEK293T

Lot#

See Vial

Storage

Liquid Nitrogen


Data

HEK293T/Human A3 β-Arrestin Agonist Assay. HEK293T/Human A3 β-Arrestin cells were treated with the reference agonist. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.
HEK293T/Human A3 β-Arrestin Agonist Assay. HEK293T/Human A3 β-Arrestin cells were treated with the reference agonist. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.


Target Background


The adenosine A3 receptor (ADORA3) is a subtype of the adenosine receptor family, belonging to the Gi protein-coupled receptor class. Its expression in the body is relatively restricted, primarily found on peripheral immune cells, within the central nervous system, and in the eye.


Its function is bidirectional: short-term or low-intensity activation mediates anti-inflammatory effects, cardioprotective ischemic preconditioning, and neuroprotection; whereas high-intensity or sustained activation may lead to pro-inflammatory responses and apoptosis.


Consequently, ADORA3 is a complex regulatory target. Selective agonists hold potential for treating inflammatory and autoimmune diseases and ischemia/reperfusion injury, while its antagonists may be explored for certain cancer therapies.

 



Product Documentation



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