HEK293 Human H2 Stable Cell

HEK293/Human H2 Stable Cell

Item	Cat#	Price
Stable Cell Line	SNB-G-0116A	$19,800
Compound Testing Services	CT-001	$1,850 per 384w plate *(Up To 16 cpds Dose)*

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Product Description

The histamine H2 receptor (HRH2) is a G protein-coupled receptor primarily mediating gastric acid secretion. It is predominantly located in gastric mucosal parietal cells, with additional expression in cardiomyocytes, vascular smooth muscle, immune cells, and the central nervous system. Its function is achieved by activating the Gs protein-adenylyl cyclase-cAMP signaling pathway upon histamine binding, potently stimulating gastric acid secretion from parietal cells and partially promoting pepsinogen release. Furthermore, it contributes to positive chronotropic effects in the heart and modulates cytokine secretion in immune cells. This receptor is a classic therapeutic target for peptic ulcers and gastroesophageal reflux disease, with H2 receptor antagonists (e.g., ranitidine, famotidine) effectively inhibiting excessive acid secretion by blocking this pathway.

Screeningbio’s HEK293/Human H2 cell line overexpress HRH2 and is designed to detect increases in intracellular cAMP levels in response to agonist stimulation of the receptor. Cisbio HTRF cAMP kit can be used to detect the signal.

Product Specifications

Target Type	GPCR
Species	Human
HGNC Symbol	HRH2
Accession Number	AY136744 (Hs)
Parental Line	HEK293
Lot#	See Vial
Storage	Liquid Nitrogen

Data

HEK293/Human H2 Agonist Assay. HEK293/Human H2 cells were treated with the reference agonist. The assay was run based on Revvity cAMP HTRF protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 values were determined, using GraphPad Prism software. — **HEK293/Human H2 Agonist Assay.** HEK293/Human H2 cells were treated with the reference agonist. The assay was run based on Revvity cAMP HTRF protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 values were determined, using GraphPad Prism software.

Target Background

The histamine H2 receptor (HRH2) is a G protein-coupled receptor primarily mediating gastric acid secretion. It is predominantly located in gastric mucosal parietal cells, with additional expression in cardiomyocytes, vascular smooth muscle, immune cells, and the central nervous system.

Its function is achieved by activating the Gs protein-adenylyl cyclase-cAMP signaling pathway upon histamine binding, potently stimulating gastric acid secretion from parietal cells and partially promoting pepsinogen release. Furthermore, it contributes to positive chronotropic effects in the heart and modulates cytokine secretion in immune cells.

This receptor is a classic therapeutic target for peptic ulcers and gastroesophageal reflux disease, with H2 receptor antagonists (e.g., ranitidine, famotidine) effectively inhibiting excessive acid secretion by blocking this pathway.