top of page

HEK293 TREX Human TRPV1 Stable Cell

Item
Cat#
Price

Stable Cell Line

SNB-I-0006A

$19,800

Compound Test Services

CT-001

$1,850 per 384w plate

(Up To 16 cpds Dose)


Product Description


Transient Receptor Potential Vanilloid subtype 1 (TRPV1) channels are a diverse family of non-selective cation channels involved in sensing a wide range of physical and chemical stimuli, including temperature, mechanical forces, pH, and ligands such as capsaicin and menthol. They are broadly expressed in sensory neurons and other tissues, playing essential roles in pain perception, thermoregulation, inflammation, and cellular homeostasis. The TRP channel family is divided into several subfamilies, including TRPC, TRPV, TRPM, TRPA, TRPP, and TRPML, each with distinct physiological functions and activation mechanisms. Due to their central role in sensory signaling and disease, TRP channels are emerging as promising therapeutic targets for pain, inflammation, and various neurological and cardiovascular disorders.

Screeningbio’s TRPV1 cell line express non-tag full length human TRPV1 receptor in HEK293 cell. When induced and activated, TRPV1 cell line response to extracellular stimuli (e.g. Capsaicin) 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

TRPV1

Accession Number

NM_018727

Parental Line

HEK293

Lot#

See Vial

Storage

Liquid Nitrogen


Data

Human TRPV1 Activator Assay. HEK293 TREX Human TRPV1 cells were seeded in 384-well plate with 1 μg/mL doxycycline and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference activator Capsaicin. 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 TRPV1 Activator Assay. HEK293 TREX Human TRPV1 cells were seeded in 384-well plate with 1 μg/mL doxycycline and incubated at 37oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference activator Capsaicin. 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 TRPV1 Blocker Assay. HEK293 TREX Human TRPV1 cells were seeded in 384-well plate with 1 μg/mL doxycycline and incubated at 30oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference blockers Ruthenium Red or Capsazepine, and stimulated by activator Capsaicin. 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 TRPV1 Blocker Assay. HEK293 TREX Human TRPV1 cells were seeded in 384-well plate with 1 μg/mL doxycycline and incubated at 30oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference blockers Ruthenium Red or Capsazepine, and stimulated by activator Capsaicin. 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 vanilloid 1 (TRPV1), also known as the capsaicin receptor, is a non-selective cation channel that belongs to the TRP channel superfamily. TRPV1 is predominantly expressed in sensory neurons of the dorsal root and trigeminal ganglia, but is also found in the brain, bladder, skin, and various epithelial tissues. It serves as a molecular integrator of noxious stimuli, responding to heat (>43 °C), acidic conditions, and vanilloid compounds such as capsaicin.


Upon activation, TRPV1 undergoes conformational changes that permit the influx of calcium and sodium ions, leading to depolarization and initiation of pain signaling pathways. This ionic flux not only drives acute nociception but also activates downstream signaling cascades, including MAPK and PKC pathways, which contribute to neurogenic inflammation, sensitization, and chronic pain states. TRPV1 activity is tightly regulated by phosphorylation, lipid interactions, and association with scaffolding proteins, allowing dynamic modulation in response to injury or inflammation.


TRPV1 is a validated therapeutic target for pain management, inflammation, and related disorders. Antagonists of TRPV1 have been explored for the treatment of neuropathic pain, osteoarthritis, and migraine, while topical agonists such as capsaicin are clinically used to desensitize sensory neurons and provide long-lasting analgesia. Beyond pain, TRPV1 modulation has implications in cough reflex, bladder overactivity, and metabolic regulation. Given its central role in nociception and inflammation, TRPV1 remains a high-value target for both pharmacological intervention and mechanistic studies in translational research.


Product Documentation



bottom of page