top of page

HEK293 Human P2X7 Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-I-0037A

$19,800

Compound Test Services

CT-001

$1,850 per 384w plate

(Up To 16 cpds Dose)


Product Description


P2X receptors are a family of ligand-gated ion channels activated by extracellular adenosine triphosphate (ATP). Seven subtypes have been identified in mammals (P2X1–P2X7), each encoded by distinct genes and displaying unique tissue distributions, kinetics, and pharmacological properties. Structurally, each P2X subunit contains two transmembrane domains, a large extracellular loop with the ATP-binding site, and intracellular N- and C-termini. Three subunits assemble to form a functional trimeric channel. Upon ATP binding, P2X receptors undergo conformational changes that open a cation-permeable pore, allowing Na⁺ and Ca²⁺ influx and K⁺ efflux, thereby triggering diverse downstream signaling pathways. P2X receptors play critical roles in neurotransmission, pain sensation, inflammation, smooth muscle contraction, and immune regulation. Certain subtypes have specific physiological and pathological relevance: P2X3 is implicated in chronic pain and refractory cough; P2X4 contributes to neuropathic pain and central nervous system disorders; P2X7 is involved in inflammatory cytokine release and cell death. Due to their widespread expression and disease associations, P2X receptors have emerged as attractive therapeutic targets. Selective agonists and antagonists are being investigated for the treatment of pain, inflammatory diseases, neurodegenerative disorders, and cancer.

 

Screeningbio’s P2X7 cell line stable express non-tag full length human P2X7 receptor in HEK293 cell. When activated, P2X7 cell line response to extracellular stimuli (e.g. ATP) and result in channel opening and calcium influx. Increase of intercellular calcium was detected by calcium sensitive dye.


Product Specifications

Target Type

Ion Channel

Species

Human

HGNC Symbol

P2X7

Accession Number

NM_002562

Parental Line

HEK293

Lot#

See Vial

Storage

Liquid Nitrogen


Data

Human P2X7 Activator Assay. HEK293 Human P2X7 cells were seeded in 384-well plate and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference activator. The assay was run based on FLIPR Calcium assay protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.
Human P2X7 Activator Assay. HEK293 Human P2X7 cells were seeded in 384-well plate and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference activator. The assay was run based on FLIPR Calcium assay protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.
Human P2X7 Blocker Assay. HEK293 Human P2X7 cells were seeded in 384-well plate and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference blockers, and stimulated by activator. The assay was run based on FLIPR Calcium assay protocol. Non-linear regression was used to plot activity changes vs. [Compound, M], and EC50 /IC50 values were determined, using GraphPad Prism software.
Human P2X7 Blocker Assay. HEK293 Human P2X7 cells were seeded in 384-well plate and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference blockers, and stimulated by activator. The assay was run based on FLIPR Calcium assay 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



The purinergic receptor P2X7 (P2X7R) is a unique member of the ATP-gated P2X receptor family, functioning as a non-selective cation channel and, under sustained activation, forming large pores that allow the passage of molecules up to 900 Da. P2X7 is widely expressed in immune cells—including macrophages, microglia, dendritic cells, and lymphocytes—as well as in epithelial and certain tumor cells. It is activated by high concentrations of extracellular ATP, typically released during tissue injury, inflammation, or cell stress, positioning P2X7 as a key sensor of cellular danger signals.


Upon activation, P2X7 mediates calcium and sodium influx and potassium efflux, leading to downstream activation of the NLRP3 inflammasome, caspase-1, and subsequent release of pro-inflammatory cytokines such as IL-1β and IL-18. This signaling cascade plays an essential role in inflammation, immunity, and programmed cell death (pyroptosis). In the nervous system, P2X7 contributes to microglial activation and neuroinflammatory processes associated with neuropathic pain and neurodegenerative diseases.


Dysregulation or overactivation of P2X7 has been implicated in a wide range of pathological conditions, including chronic inflammation, autoimmune disorders, neurodegeneration, and cancer. Because of its dual role in promoting inflammation and inducing cell death, P2X7 represents an attractive therapeutic target for diseases such as rheumatoid arthritis, multiple sclerosis, Alzheimer’s disease, and certain malignancies. Its unique ability to link extracellular ATP signaling to immune activation underscores its importance as a central regulator of inflammation and tissue homeostasis.


Product Documentation



bottom of page