Cav1.2 (L-type) Human Calcium Ion Channel Binding (Dihydropyridine Site) LeadHunter Assay - TW

Background Information:

Cav1.2 is an L-type voltage-gated calcium channel consisting of a pore-forming α1C subunit with four homologous domains (I-IV) and auxiliary β and α2δ subunits that mediate depolarization-induced calcium influx, regulating contraction, secretion, neurotransmission, and gene expression. As the predominant L-type calcium channel in cardiac myocytes and vascular smooth muscle, Cav1.2 generates the L-type calcium current (ICa,L) essential for excitation-contraction coupling and action potential duration. Mutations in Cav1.2 cause life-threatening cardiac arrhythmias, developmental abnormalities, and sudden death. L-type calcium channel blockers are widely used cardiovascular therapeutics acting via distinct mechanisms: phenylalkylamines (e.g., verapamil) block the intracellular pore, dihydropyridines (e.g., nifedipine) allosterically modulate channel gating, and benzothiazepines (e.g., diltiazem) bind overlapping phenylalkylamine receptor sites. Excessive Cav1.2 blockade causes bradycardia, heart block, and hypotension, making Cav1.2 essential for functional assays in cardiac safety liability assessment and therapeutic development.

Family:

Ion Channel

Sub Family:

Calcium

Class:

Voltage-Gated

Protein Name:

Cav1.2 (L-type)

Uniprot Number:

Q13936

Gene Name:

CACNA1C

Gene ID:

775

Gene Aliases:

CACH2, CACN2-IT2, CACNL1A1, CCHL1A1, CaV1.2, LQT8

Organism:

Human