Sodium Channel
Na channels; Na+ channels
Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na+) through a cell's plasma membrane. They are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials. Voltage-gated Na+ channels can exist in any of three distinct states: deactivated (closed), activated (open), or inactivated (closed). Ligand-gated sodium channels are activated by binding of a ligand instead of a change in membrane potential.
Sodium Channel Isoform Specific Products
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Sodium Channel
(629)
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Nav1.1
(12)
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Nav1.2
(17)
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Nav1.3
(15)
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Nav1.4
(15)
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Nav1.5
(27)
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Nav1.6
(13)
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Nav1.7
(63)
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Nav1.8
(42)
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Nav1.9
(3)
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All Product Categories
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Sodium Channel Inhibitors
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Sodium Channel Agonists
(10)
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Sodium Channel Antagonists
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Sodium Channel Activators
(35)
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Sodium Channel Modulators
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Sodium Channel Controls
(5)
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Sodium Channel Ligands
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Sodium Channel Related Products (810)
Related Products (810)
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Antibodies (9)
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Related Compound Screening Libraries (1)
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Sodium Channel Isoform Comparison
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Oxazosulfyl
0 ImagesOxazosulfyl is a sulfyl insecticide with potent and cross-spectrum insecticidal activity. Oxazosulfyl inhibits sodium currents by binding to and stabilizing the slow-inactivated state of voltage-gated sodium channels, leading to insect paralysis. Oxazosulfyl's ability to block sodium channels is correlated with its insecticidal activity.
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Taplucainium chloride
0 ImagesTaplucainium chloride is a sodium channel blocker. Taplucainium chloride selectively inhibits nociceptors in an activated or inflammatory state. Taplucainium chloride may be used in research on chronic cough.
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VU6032735
0 ImagesCat. No.: HY-175728Purity: 99.26%VU6032735 is a potent and subtype-selective sperm-specific potassium channel 3 (SLO3) inhibitor with IC50 values of 165 nM (hSLO3) and 730 nM (mSLO3). VU6032735 also inhibits sodium channel and L-type calcium channel VU6032735 can sustain high tissue exposure in the fertilized oviduct. VU6032735 can be used for the research of contraception.
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Nav1.8-IN-2
0 ImagesNav1.8-IN-2 (compound 35A) is a Nav1.8 voltage-gated sodium ion inhibitor with an IC50 of 0.4 nM (HEK 293 cells). Nav1.8-IN-2 inhibits the activity of Nav1.8 voltage-gated sodium ion channels, mediates sodium ion influx in excitable cells, and is associated with the initiation and conduction of action potentials. Nav1.8-IN-2 can be used for research related to pain, cough, itching, etc.
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Z-Gly-Gly-Phe-OH
0 ImagesZ-Gly-Gly-Phe-OH is a substrate for pepsin and thermolysin. Z-Gly-Gly-Phe-OH has an IC50 of 15.8 μM for open sodium channels under pepsin catalysis. Z-Gly-Gly-Phe-OH forms peptide bonds with amine components (such as H-Leu-NHPh) through enzyme-catalyzed condensation reactions, and is active as an intermediate in peptide synthesis.
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Piromelatine
0 ImagesSynonyms: Neu-P11Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
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Bepridil
0 ImagesSynonyms: CERM 1978 free base; Org 5730Bepridil (CERM 1978 (free base); Org 5730) is an orally active non-selective calcium channel antagonist with multi-ion channel blocking activity. Bepridil modulates Calmodulin, the 20S proteasome, T-type/L-type calcium channels, cardiac sodium channels, multiple potassium channels, γ-secretase, β-secretase, and mitoKATP/sarcKATP channels. Bepridil acts as a hydroxyl radical scavenger, regulates mitochondrial and intracellular calcium handling, and exerts antiarrhythmic, antianginal, and cardioprotective effects. Bepridil alters amyloid precursor protein processing, reduces β-amyloid and thalamic calcium levels, restores seladin-1/DHCR24 expression, and improves sensorimotor recovery after cerebral ischemia. Bepridil also exhibits potent inhibitory effects on SARS-CoV-2 replication. Bepridil is used in studies related to stable angina, arrhythmias, cerebral ischemia, Alzheimer's disease, and SARS-CoV-2 infection.
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Bupivacaine hydrochloride (Standard)
0 ImagesBupivacaine (hydrochloride) (Standard) is the analytical standard of Bupivacaine (hydrochloride). This product is intended for research and analytical applications. Bupivacaine hydrochloride is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride can be used for the research of chronic pain.
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Aprindine hydrochloride
0 ImagesAprindine hydrochloride is an Ib-class anti-arrhythmic agent. Aprindine hydrochloride mainly exerts its effect by blocking sodium channels (INa), thereby reducing the excitability and conduction velocity of cardiac muscle cells. Aprindine hydrochloride significantly inhibits delayed potassium currents, which helps to prolong the atrial effective refractory period (AERP) and inhibit the occurrence of atrial fibrillation. Aprindine hydrochloride can also regulate intracellular calcium ion concentration by inhibiting Na+/Ca2+ exchange current (INCX), thereby further stabilizing cardiac electrical activity. Aprindine hydrochloride can be used for the study of atrial fibrillation (AF) and ventricular arrhythmias.
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PF-05186462
0 ImagesPF-05186462 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channel, with an IC50 of 21 nM. PF-05186462 shows significant selectivity for Nav1.7 versus other sodium channels (Nav 1.1, 1.2, 1.3, 1.4, 1.5, 1.6, and 1.8). PF-05186462 can be used for the research of acute or chronic pain.
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Phrixotoxin 3-NH2 TFA
0 ImagesCat. No.: HY-P1218BPurity: 98.96%Phrixotoxin 3-NH2 TFA is a derivative of Phrixotoxin 3 TFA (HY-P1218A). Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.
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Glycinexylidide
0 ImagesCat. No.: HY-W357818CAS No.: 18865-38-8Synonyms: GXGlycinexylidide (GX) is the active metabolite of Lidocaine. Lidocaine is a local agent that can suppress or relieve pain, that inhibits sodium channels involving complex voltage and dependence. Lidocaine also reduces the growth, migration and invasion of gastric cancer cells. Glycinexylidide has research potential for use in anesthesia, cancer, and cardiovascular disease.
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Riluzole (Standard)
0 ImagesRiluzole (Standard) is the analytical standard of Riluzole. This product is intended for research and analytical applications. Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na+ channel blocker which can also inhibit GABA uptake with an IC50 of 43 μM.
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Pramocaine hydrochloride
0 ImagesPramocaine (Pramoxine) hydrochloride is a topical surface anesthetic and antipruritic agent. Pramocaine hydrochloride reversibly inhibits voltage-gated sodium channel, reduces transmembrane permeability of sodium ions, stabilizes cell membranes, prevents depolarization, blocks action potential conduction, and inhibits peripheral slow C-fiber pathways associated with pain, pruritus and thermoception. Pramocaine hydrochloride can be used in research related to chronic pruritus, renal pruritus, atopic dermatitis, xerotic pruritus, uremic pruritus, and cutaneous hyperalgesia/pain.
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Atomoxetine
0 ImagesSynonyms: Tomoxetine; (R)-TomoxetineAtomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research.
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PF-05198007
0 ImagesPF-05198007 is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor. PF-05198007 is a compound with a similar pharmacodynamic profile to PF-05089771.
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Ipidacrine
0 ImagesSynonyms: NIK-247 free base; Amiridine free baseIpidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K+ and Na+-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases.
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Amitriptyline-d6 hydrochloride
0 ImagesAmitriptyline-d6 hydrochloride is the deuterium labeled Amitriptyline hydrochloride (HY-B0527A). Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
