HEK293 TREX Human GluN1a/GluN2C Stable Cell

HEK293 TREX Human GluN1a/GluN2C Stable Cell

Item	Cat#	Price
Stable Cell Line	SNB-I-0040A	$19,800
Compound Test Services	CT-001	$1,850 per 384w plate *(Up To 16 cpds Dose)*

Ask For A Custom Quote

Product Description

The N-methyl-D-aspartate receptor (NMDA receptor or NMDAR) is a subtype of ionotropic glutamate receptor that plays a critical role in synaptic transmission, plasticity, and excitatory signaling in the central nervous system. It functions as a ligand-gated and voltage-dependent cation channel permeable to calcium, sodium, and potassium ions. Activation of NMDARs requires both glutamate binding and co-agonist glycine (or D-serine), as well as relief from magnesium ion block through membrane depolarization. Structurally, NMDA receptors are heterotetramers typically composed of GluN1 and GluN2 (A–D) subunits, which determine their functional and pharmacological properties. NMDAR-mediated calcium influx is essential for learning, memory, and long-term potentiation (LTP), but excessive activation can lead to excitotoxicity and neuronal injury, contributing to neurological disorders such as stroke, Alzheimer’s disease, and epilepsy.

Screeningbio’s GluN1a/GluN2C cell line express non-tag full length human NMDA receptor GluN1a and GluN2C subunit in HEK293 cell. When induced and activated, cell line response to extracellular stimuli (e.g. Glutamate) 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	NMDA
Accession Number	NM_007327 (GluN1a), NM_000826 (GluN2C)
Parental Line	HEK293
Lot#	See Vial
Storage	Liquid Nitrogen

Data

Human GluN1a/GluN2C Activator Assay. HEK293 TREX Human GluN1a/GluN2C 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 GluN1a/GluN2C Activator Assay.** HEK293 TREX Human GluN1a/GluN2C cells were seeded in 384-well plate and incubated at 37^oC 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 GluN1a/GluN2C Blocker Assay. HEK293 TREX Human GluN1a/GluN2C cells were seeded in 384-well plate and incubated at 30oC in 5% CO2 incubator for 24 hours before running the assay. The cells were treated with the reference blockers 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** **GluN1a/GluN2C** **Blocker Assay.** HEK293 TREX Human GluN1a/GluN2C cells were seeded in 384-well plate and incubated at 30^oC in 5% CO₂ incubator for 24 hours before running the assay. The cells were treated with the reference blockers 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 N-methyl-D-aspartate receptor (NMDAR) subunit GluN2C, encoded by the GRIN2C gene, is a member of the ionotropic glutamate receptor family that plays a key role in excitatory neurotransmission and synaptic plasticity. Like other NMDARs, GluN2C forms a heterotetrameric complex typically composed of two GluN1 and two GluN2 subunits, with GluN2C conferring unique pharmacological and biophysical properties to the receptor.

Receptors containing GluN2C subunits are characterized by reduced single-channel conductance, lower calcium permeability, and weaker voltage-dependent Mg²⁺ block compared to GluN2A- or GluN2B-containing receptors. These properties allow GluN2C-containing NMDARs to remain active at relatively hyperpolarized potentials and to contribute to sustained, low-level calcium signaling. GluN2C exhibits high affinity for glutamate and glycine, slower deactivation kinetics, and reduced desensitization, supporting its role in modulating tonic excitatory transmission.

GluN2C expression is enriched in the cerebellum, thalamus, and olfactory bulb, where it contributes to fine-tuning neuronal excitability and information processing. In the cerebellum, it is highly expressed in granule cells, influencing motor coordination and learning. In the thalamus, GluN2C participates in regulating relay neuron activity and sensory signal gating. Dysregulation of GluN2C function or expression has been implicated in various neurological and psychiatric disorders, including schizophrenia, ataxia, and cognitive dysfunction.

Pharmacologically, GluN2C-selective modulators are of increasing interest as therapeutic tools for targeting specific NMDAR subpopulations without broad excitotoxicity associated with pan-NMDAR blockade.