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Calcium Channels

    Calcium Channels

    Voltage-gated calcium channels hetero-multimeric protein complexes.Calcium channel is an important target for drug action, and is of key importance in the cardiovascular diseases, pain, Alzheimer's disease, etc.

    1. Detailed information

    Voltage-gated calcium channels hetero-multimeric protein complexes consisting of an alpha1 sub- unit, as well as ancillary beta, alpha2-delta, and possibly gamma subunits are a primary route through which calcium can enter cells.

    Calcium channels are encoded by 10 genes, among those 4 encode the L-type calcium channel family.

    The calcium channel is highly sensitive to calcium ions and allow Ca2+ to enter the cells, resulting in definite physiological functions.



    Calcium channel is an important target for drug action, and is of key importance in the cardiovascular diseases, pain, Alzheimer's disease, etc.



    ICE has established the stable cell line of the following calcium channels. Cav 1.2, Cav 2.1, Cav 2.2, Cav 3.2. 

     

    Cav

    subtypes

    Antagonist IC50 (nM)

    Distribution

    Related diseases

    CaV1.2

    (L-type)

    Nifedipine

    10.5±1.8

    Heart

    Skeletal muscle, smooth muscle,

    bone dendrites and dendritic spines of cortical neurones

    Timothy syndrome, long QT syndrome, 

    Pain, epilepsy, hypertension, stroke, arrhythmia, Autism

    Cav2.1

    (P/Q-type)

    Cadmium

    2900 ± 658.2

    Purkinje neurons in the cerebellum / Cerebellar granule cells

    migraine, seizure and ataxia syndromes

    Cav2.2

    (N-type)

    Cadmium

    7000±714.1

    CNS, PNS

    Pain, Spinal cord injury, Kleefstra syndrome

    Cav3.2

    (T-type)

    NiCl

    1200

    neurons, cells that have pacemaker activity, bone

    Convulsion

     

     

    1.     L-type calcium channel (CaV1.2)

     

    Channel

    Cav1.2/β2/α2/δ1, L-type

    Catalog Ref.

    ICE-CHO-Cav1.2

    Gene

    CACNA1C

    Sources

    human

    Expression system

    CHO

    Method

    whole cell patch clamp

    Reference Inhibitor

    Nifedipine(31.3nM±6.8nM), verapamil

    Target

    Timothy syndrome, long QT syndrome,  Pain, epilepsy, hypertension, stroke, arrhythmia, Autism

     

    image.pngimage.pngimage.png

    2.     N-type calcium channel (CaV2.2)

    Channel

    Cav2.2/β3/α2δ1 , N-type

    Catalog Ref.

    ICE-CHO-Cav2.2

    Gene

    CACNA1B

    Sources

    human

    Expression system

    CHO

    Method

    whole cell patch clamp

    Reference compound

    Nifedipine, verapamil, Cadmium (IC50=7.0µm±704nM)

    Target

    Pain, Spinal cord injury, Kleefstra syndrome

     image.pngimage.pngimage.png

    3.     T-type calcium channel (CaV3.2)

    Channel

    CaV3.2, T-type

    Catalog Ref.

    ICE-CHO-Cav3.2

    Gene

    CACNA1H

    Sources

    human

    Expression system

    HEK293

    Method

    whole cell patch clamp

    Reference compound

    Nifedipine, verapamil, NiCl

    Target

    Convulsion

     

     image.png image.pngimage.png


     

    4.       P/Q-type calcium channel (CaV2.1)

     

    Channel

    Cav2.1

    Catalog Ref.

    ICE-CHO-Cav2.1

    Gene

    CACNA1A

    Sources

    human

    Expression system

    CHO

    Method

    whole cell patch clamp

    Reference inhibitor

    Cadmium (2.9 ± 0.658µM)

    Target

    migraine, seizure and ataxia syndromes

     image.png image.png image.png

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