HEK293 TREX hCav1.2 Stable Cell

HEK293 TREX hCav1.2 Stable Cell

Item	Cat#	Price
Stable Cell Line	SNB-I-0014A	$19,800
Compound Test Services	CT-001	$1,850 per 384w plate *(Up To 16 cpds Dose)*

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Product Description

The Cav1.2 is the pore-forming α1C subunit of human L-type voltage-gated calcium channels, essential for excitation–contraction coupling, excitation–transcription coupling, and diverse signaling pathways. It is a high-voltage-activated, Ca²⁺-selective channel that also permits minor Na⁺ permeation. Its activation requires strong membrane depolarization and is modulated by calmodulin‑mediated calcium‑dependent inactivation and voltage‑dependent inactivation. Structurally, the α1C subunit associates with auxiliary β and α2δ subunits, and contains four homologous domains (I–IV), each with six transmembrane segments; S4 acts as the voltage sensor, while the S5–S6 loop forms the selectivity filter. hCav1.2‑mediated Ca²⁺ entry sustains the cardiac action potential plateau, triggers vascular smooth muscle contraction, regulates neuronal gene expression, and mediates hormone secretion. Channel dysfunction, whether from gain‑of‑function mutations or pathological dysregulation, underlies Timothy syndrome, hypertension, cardiac arrhythmias, heart failure, neuropathic pain, and epilepsy, making it a critical drug target.

Screeningbio’s Cav1.2 cell line expresses non-tag full length human voltage-gated calcium channel Cav1.2 subunit in HEK293 cell. When depolarized and activated, cell line responds to membrane potential changes (e.g. high KCl stimulation) and results in channel opening and calcium influx. Increase of intracellular calcium was detected by calcium sensitive dye.

Product Specifications

Target Type	Ion Channel
Species	Human
HGNC Symbol	CACNA1C
Accession Number	NM_001167625
Parental Line	HEK293
Lot#	See Vial
Storage	Liquid Nitrogen

Data

Human Cav1.2 Blocker Assay. HEK293/TREX Human Cav1.2 cells were seeded in 384-well plate and incubated at 37°C in 5% CO₂ incubator for 24 hours before running the assay. The cells were treated with the reference blockers and stimulated by EC80 concentration of depolarizing agent (e.g., KCl). 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 Cav1.2 Blocker Assay.** HEK293/TREX Human Cav1.2 cells were seeded in 384-well plate and incubated at 37°C in 5% CO₂ incubator for 24 hours before running the assay. The cells were treated with the reference blockers and stimulated by EC80 concentration of depolarizing agent (e.g., KCl). 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 Cav1.2 is the pore-forming α1C subunit of human L-type voltage-gated calcium channels, essential for excitation–contraction coupling, excitation–transcription coupling, and diverse signaling pathways. It is a high-voltage-activated, Ca²⁺-selective channel that also permits minor Na⁺ permeation. Its activation requires strong membrane depolarization and is modulated by calmodulin‑mediated calcium‑dependent inactivation and voltage‑dependent inactivation.

Structurally, the α1C subunit associates with auxiliary β and α2δ subunits, and contains four homologous domains (I–IV), each with six transmembrane segments; S4 acts as the voltage sensor, while the S5–S6 loop forms the selectivity filter. hCav1.2‑mediated Ca²⁺ entry sustains the cardiac action potential plateau, triggers vascular smooth muscle contraction, regulates neuronal gene expression, and mediates hormone secretion.

Channel dysfunction, whether from gain‑of‑function mutations or pathological dysregulation, underlies Timothy syndrome, hypertension, cardiac arrhythmias, heart failure, neuropathic pain, and epilepsy, making it a critical drug target.