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HEK293T/Mouse CRF2 β-Arrestin Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-A-0081B

Inquiry

Compound Testing Services

CT-001

$1,850 per 384w plate

(Up To 16 cpds Dose)


Product Description


The CRF2 receptor (CRHR2), another subtype of the corticotropin-releasing hormone receptor, exhibits high affinity for the ligands urocortin 1, 2, and 3. Its distribution in the brain differs from CRF1, being concentrated in areas like the lateral septum, hypothalamus, and amygdala; peripherally, it is widely expressed in the heart, skeletal muscle, and gastrointestinal tract. Functionally, the CRF2 receptor is believed to buffer or counteract the excessive stress responses mediated by the CRF1 receptor, contributing to reduced anxiety, suppressed appetite, enhanced cardiac function, and regulated gastrointestinal motility. Consequently, CRF2 receptor agonists are under investigation for treating anxiety disorders and heart failure.

 

ScreeningBio’s HEK293T/Mouse CRF2 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

Mouse

HGNC Symbol

CRHR2

Accession Number

NM_009953 (Mm)

Parental Line

HEK293T

Lot#

See Vial

Storage

Liquid Nitrogen


Data

HEK293T/Mouse CRF2 β-Arrestin Agonist Assay. HEK293T/Mouse CRF2 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/Mouse CRF2 β-Arrestin Agonist Assay. HEK293T/Mouse CRF2 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 CRF2 receptor (CRHR2), another subtype of the corticotropin-releasing hormone receptor, exhibits high affinity for the ligands urocortin 1, 2, and 3. Its distribution in the brain differs from CRF1, being concentrated in areas like the lateral septum, hypothalamus, and amygdala; peripherally, it is widely expressed in the heart, skeletal muscle, and gastrointestinal tract.


Functionally, the CRF2 receptor is believed to buffer or counteract the excessive stress responses mediated by the CRF1 receptor, contributing to reduced anxiety, suppressed appetite, enhanced cardiac function, and regulated gastrointestinal motility. Consequently, CRF2 receptor agonists are under investigation for treating anxiety disorders and heart failure.

 



Product Documentation



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