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HEK293 Human P2X2 Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-I-0034A

$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 P2X2 cell line stable express non-tag full length human P2X2 receptor in HEK293 cell. When activated, P2X2 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

P2X2

Accession Number

NM_170682

Parental Line

HEK293

Lot#

See Vial

Storage

Liquid Nitrogen


Data

Human P2X2 Activator Assay. HEK293 Human P2X2 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 P2X2 Activator Assay. HEK293 Human P2X2 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 P2X2 Blocker Assay. HEK293 Human P2X2 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 P2X2 Blocker Assay. HEK293 Human P2X2 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 P2X2 (P2X2R) is a member of the ATP-gated P2X receptor family, functioning as a trimeric, non-selective cation channel permeable to sodium, potassium, and calcium ions. Activated by extracellular ATP, P2X2 is widely expressed in the nervous system—particularly in sensory and autonomic ganglia, the brainstem, and cochlear hair cells—as well as in smooth muscle and endocrine tissues. This broad distribution enables P2X2 to mediate diverse physiological processes including neurotransmission, hearing, autonomic control, and hormone secretion.

Distinct from rapidly desensitizing receptors such as P2X1, P2X2 exhibits slower activation and desensitization kinetics, allowing it to sustain depolarizing currents in response to prolonged ATP exposure. In sensory neurons, P2X2 forms functional heteromers with P2X3, generating receptors that play key roles in nociception, chemosensation, and reflex control of respiration and cardiovascular function. In the auditory system, P2X2-mediated purinergic signaling contributes to sound transduction and adaptation to noise-induced stress within the cochlea.

Alterations in P2X2 function have been linked to hereditary hearing loss, autonomic dysfunction, and inflammatory pain. Because of its involvement in both neural and sensory signaling, P2X2 represents a vital component of ATP-mediated intercellular communication and a promising target for therapeutic intervention in auditory, pain, and autonomic disorders.


Product Documentation



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