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
(11)
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Nav1.2
(16)
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Nav1.3
(14)
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Nav1.4
(14)
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Nav1.5
(21)
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Nav1.6
(12)
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Nav1.7
(61)
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Nav1.8
(41)
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Nav1.9
(2)
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All Product Categories
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Sodium Channel Inhibitors
(619)
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Sodium Channel Agonists
(10)
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Sodium Channel Antagonists
(30)
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Sodium Channel Activators
(35)
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Sodium Channel Modulators
(30)
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Sodium Channel Controls
(5)
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Sodium Channel Ligands
(3)
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Sodium Channel Related Products (802)
Related Products (802)
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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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PF 05089771 tosylate
0 ImagesCat. No.: HY-12883BCAS No.: 1430806-04-4PF 05089771 tosylate is a potent, orally active and selective arylsulfonamide Nav1.7 inhibitor, with IC50 values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNav1.7, cynNav1.7, dogNav1.7, ratNav1.7, and musNav1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.
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Nav1.8-IN-18
0 ImagesCat. No.: HY-172998CAS No.: 3003828-55-2Nav1.8-IN-19 (Compound 70) is a Nav1.8 inhibitor.
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Hm1a
0 ImagesCat. No.: HY-P5183Hm1a is a venom peptide and a selective hNaV1.1 activator with an EC50 of 7.5 nM. Hm1a enhances hNaV1.1 and hNaV1.3 channel currents via delayed inactivation. Hm1a restores action potential firing in Dravet syndrome GABAergic inhibitory interneurons, reduces interictal epileptiform discharges and whole-brain hyperexcitability, lowers seizure frequency, and rescues premature death in Dravet syndrome mice. Hm1a can be used for the research of neurological disease, such as Dravet syndrome.
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Ralfinamide mesylate
0 ImagesSynonyms: FCE-26742A mesylateRalfinamide mesylate (FCE-26742A mesylate) is an orally available Na+ channel blocker derived from α-aminoamide, with function of suppressing pain.
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RS-87337
0 ImagesCat. No.: HY-113841CAS No.: 107707-38-0RS-87337 is an orally active piperazine-amidine hybrid class Ia (inhibiting Vmax, IC50 = 17 μM)/class III (prolonging ADP90, EC15 = 2 μM) antiarrhythmic agent with selectivity for ventricular conduction. RS-87337 inhibits cardiac sodium channel, thereby reducing the maximum depolarization rate of action potential, with moderate onset and recovery kinetics. RS-87337 reduces cardiac outward potassium conductance (I_K), thus prolonging action potential duration. RS-87337 is applicable to research related to arrhythmia, ventricular arrhythmia, ventricular fibrillation, and myocardial ischemia-reperfusion injury.
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Tocainide (Standard)
0 ImagesCat. No.: HY-B1798RCAS No.: 41708-72-9Tocainide (Standard) is the analytical standard of Tocainide. This product is intended for research and analytical applications. Tocainide hydrochloride is an orally activesodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.
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P552-02 mesylate
0 ImagesCat. No.: HY-123493CAS No.: 587879-54-7Synonyms: 552-02P552-02 (552-02) mesylate is a sodium channel blocker that is potentially used for the treatment of cystic fibrosis, exhibiting biological activity that enhances mucociliary clearance in the lungs while minimizing the risk of hyperkalaemia.
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QLS-81
0 ImagesCat. No.: HY-171778CAS No.: 2835455-57-5QLS-81 is a Nav1.7 channel inhibitor (IC50: 1.5 μM). QLS-81 has significant analgesic activity and can relieve neuropathic and inflammatory pain. QLS-81 exerts frequency-dependent inhibitory effects by inhibiting the inactivated state of Nav1.7 channels. QLS-81 can be used in the study of chronic pain.
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Nav1.8-IN-23
0 ImagesCat. No.: HY-183646Nav1.8-IN-23 is a Nav1.8 voltage-gated sodium channel inhibitor with a pIC50 of 6.1. Nav1.8-IN-23 can be used for the research of pain-related diseases.
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hERG-IN-3
0 ImagesCat. No.: HY-175289hERG-IN-3 is an orally active hERG blocker with an IC50 of 44.5 nM. hERG-IN-3 exhibits a Ki for β2-adrenergic receptor of 14 nM. hERG-IN-3 exhibits the skeletal muscle Nav1.4 and sodium channel-blocking activities (IC50 = 4.4 μM, 3-fold increasement than hNav1.5). hERG-IN-3 displays a potent antimyotonic activity in an animal model. hERG-IN-3 can be used for the study of Myotonia Congenita.
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AM-0466
0 ImagesCat. No.: HY-135495CAS No.: 1642113-59-4AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing.
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Propylparaben sodium (Standard)
0 ImagesCat. No.: HY-N2026ARCAS No.: 35285-69-9Synonyms: Propyl parahydroxybenzoate sodium (Standard); Propyl 4-hydroxybenzoate sodium (Standard)Propylparaben (Propyl parahydroxybenzoate) sodium (Standard) is the analytical standard of Propylparaben sodium (HY-N2026A). Propylparaben (Propyl parahydroxybenzoate) sodium is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben sodium is an orally active weak estrogen receptor agonist. Propylparaben sodium regulates the PI3K-AKT and JNK signaling pathways, and induces oxidative stress. Propylparaben sodium is commonly used in cosmetics, pharmaceuticals and foods, and can be used in studies related to ovarian aging and myocardial ischemia-reperfusion injury.
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Bupivacaine hydrochloride monohydrate (Standard)
0 ImagesCat. No.: HY-W415121RCAS No.: 73360-54-0Bupivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Bupivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC50 of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.
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(R)-Duloxetine (Standard)
0 ImagesCat. No.: HY-B0161CRCAS No.: 116539-60-7Synonyms: (R)-LY248686 (Standard)(R)-Duloxetine (Standard) is the analytical standard of (R)-Duloxetine. This product is intended for research and analytical applications. (R)-Duloxetine is a form of Duloxetine (HY-B0161) that causes tonic and usage-dependent impairment of neuronal Na+ channels. (R)-Duloxetine can be used in pain research.
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Levosemotiadil
0 ImagesCat. No.: HY-121535CAS No.: 116476-16-5Levosemotiadil, an S-isomer of semotiadil, exhibits stronger binding affinity to human serum albumin (HSA) compared to its R-isomer counterpart. This study utilized high-performance frontal analysis (HPFA) to demonstrate that levosemotiadil binds approximately three times more strongly to HSA than semotiadil. The binding parameters were evaluated using Scatchard analysis, revealing specific interactions with the diazepam binding site on HSA. The presence of diazepam decreased the binding affinity of both enantiomers, while warfarin did not alter their binding characteristics. These findings highlight levosemotiadil's potential as a Ca- and Na-channel blocker with significant binding preferences for HSA, crucial for understanding its pharmacokinetics and therapeutic effects.
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MRS2768
0 ImagesCat. No.: HY-108649CAS No.: 1047980-83-5MRS2768 is a potent, selective, and metabolically stable P2Y2 receptor agonist with an EC50 of 1.89 μM for the human P2Y2 receptor. MRS2768 activates Gq/PLC/PKC signaling, leading to downstream phosphorylation of Akt, eNOS, and ERK, with effects varying by cell type. MRS2768 inhibits ENaC via Gq/PKC/Src/Akt to promote natriuresis and lower blood pressure in the kidney. MRS2768 activates eNOS to increase NO secretion in endothelial cells. MRS2768 drives proliferation via PI3K/Akt in fibroblasts and cancer cells. MRS2768 exerts anti-apoptotic effects through PKC/Src/Akt in cardiomyocytes. MRS2768 can be applied to investigate P2Y2-dependent pathological processes, including acute kidney injury, chronic kidney disease and renal fibrosis, DOCA-salt induced hypertension, myocardial infarction, pulmonary arterial hypertension, pancreatic cancer, cardiac fibrosis, dry eye disease, as well as shear stress-mediated vascular remodeling and atherosclerosis.
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(Z)-Flunarizine
0 ImagesCat. No.: HY-Z8176CAS No.: 693765-11-6(Z)-Flunarizine is the (Z)-isomer of Flunarizine (HY-B0358). Flunarizine is a potent dual Na+/Ca2+ channel (T-type) blocker. Flunarizine is a D2 dopamine receptor antagonist. Flunarizine shows anticonvulsive and antimigraine activity, and peripheral vasodilator effects.
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Anticonvulsant agent 5
0 ImagesCat. No.: HY-162757Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable.
