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HEK293/Human ETA Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-G-0087A

$19,800

Compound Testing Services

CT-001

$1,850 per 384w plate

(Up To 16 cpds Dose)


Product Description


ETA (EDNRA), the endothelin type-A receptor, is a G protein-coupled receptor crucial for vasoconstriction and cellular growth. Primarily located in vascular smooth muscle, heart, lungs, and kidneys, it exerts its core physiological functions by specifically binding endothelin-1 (ET-1): mediating potent and sustained vasoconstriction to regulate blood pressure and local blood flow, while also promoting cell proliferation and tissue remodeling. While these functions maintain circulatory homeostasis under normal conditions, its overactivation drives the development of various diseases such as hypertension, pulmonary arterial hypertension, heart failure, and organ fibrosis. Consequently, it has become a key therapeutic target for drugs like bosentan.

 

Screeningbio’s HEK293/Human ETA cell line overexpress EDNRA and is designed to detect increases in intracellular IP-1 levels in response to agonist stimulation of the receptor. Cisbio HTRF IP-1 kit can be used to detect the signal.

Product Specifications

Target Type

GPCR

Species

Human

HGNC Symbol

EDNRA

Accession Number

NM_001957

Parental Line

HEK293

Lot#

See Vial

Storage

Liquid Nitrogen


Data


HEK293/Human ETA Agonist Assay. HEK293/Human ETA cells were treated with the reference agonist. The assay was run based on Revvity IP-one HTRF protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.
HEK293/Human ETA Agonist Assay. HEK293/Human ETA cells were treated with the reference agonist. The assay was run based on Revvity IP-one HTRF protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.


Target Background


ETA (EDNRA), the endothelin type-A receptor, is a G protein-coupled receptor crucial for vasoconstriction and cellular growth. Primarily located in vascular smooth muscle, heart, lungs, and kidneys, it exerts its core physiological functions by specifically binding endothelin-1 (ET-1): mediating potent and sustained vasoconstriction to regulate blood pressure and local blood flow, while also promoting cell proliferation and tissue remodeling.


While these functions maintain circulatory homeostasis under normal conditions, its overactivation drives the development of various diseases such as hypertension, pulmonary arterial hypertension, heart failure, and organ fibrosis. Consequently, it has become a key therapeutic target for drugs like bosentan.



Product Documentation



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