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HEK293 Human TRPM8 Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-I-0004A

$19,800

Compound Test Services

CT-001

$1,850 per 384w plate

(Up To 16 cpds Dose)


Product Description


Transient Receptor Potential Melastatin subtype 8 (TRPM8) is a cold-sensitive, non-selective cation channel that serves as the primary molecular sensor for cool temperatures and menthol. It is predominantly expressed in peripheral sensory neurons, particularly in trigeminal and dorsal root ganglia, where it mediates sensations of coolness and cold-induced pain. TRPM8 can be activated by moderate cooling (below ~28°C), menthol, icilin, and other cooling agents, leading to calcium influx and neuronal depolarization. Beyond thermosensation, TRPM8 is also expressed in tissues such as the prostate, bladder, and cornea, where it contributes to physiological processes including smooth muscle regulation and epithelial homeostasis. Dysregulation of TRPM8 has been implicated in cold allodynia, neuropathic pain, and certain cancers, making it an attractive target for therapeutic interventions aimed at modulating pain and temperature sensitivity.

 

Screeningbio’s TRPM8 cell line stable express non-tag full length human TRPM8 receptor in HEK293 cell. When activated, TRPM8 cell line response to extracellular stimuli 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

TRPM8

Accession Number

NM_024080

Parental Line

HEK293

Lot#

See Vial

Storage

Liquid Nitrogen


Data

Human TRPM8 Activator Assay. HEK293 Human TRPM8 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 TRPM8 Activator Assay. HEK293 Human TRPM8 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 TRPM8 Blocker Assay. HEK293 Human TRPM8 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 TRPM8 Blocker Assay. HEK293 Human TRPM8 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 transient receptor potential melastatin 8 (TRPM8) is a non-selective cation channel belonging to the TRP superfamily and serves as the primary molecular sensor for environmental cold and cooling agents. TRPM8 is predominantly expressed in a subset of sensory neurons within the dorsal root and trigeminal ganglia, as well as in non-neuronal tissues such as the prostate, bladder, and vascular endothelium. It is activated by mild cool temperatures (below ~26 °C) and by cooling compounds like menthol, icilin, and eucalyptol, which induce characteristic cooling sensations.


Upon activation, TRPM8 mediates calcium and sodium influx, leading to depolarization of sensory neurons and initiation of cold-sensing and analgesic pathways. In addition to its role in thermosensation, TRPM8 is modulated by intracellular signaling pathways, phosphatidylinositol 4,5-bisphosphate (PIP₂), and hormonal factors such as testosterone and androgens, reflecting its broader physiological relevance.


Functionally, TRPM8 contributes to the perception of cold, thermoregulation, and modulation of pain, particularly in cold allodynia and neuropathic conditions. Beyond sensory neurons, aberrant TRPM8 expression has been linked to prostate, breast, and pancreatic cancers, suggesting a role in tumor proliferation and migration. Pharmacological modulation of TRPM8 offers therapeutic potential for neuropathic pain, migraine, and urinary disorders. As both a thermosensor and a therapeutic target, TRPM8 represents a crucial link between sensory physiology and clinical intervention.


Product Documentation



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