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
(18)
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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
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Sodium Channel Antagonists
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Sodium Channel Activators
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Sodium Channel Modulators
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Sodium Channel Controls
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Sodium Channel Ligands
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Sodium Channel Related Products (811)
Related Products (811)
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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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Phenytoin-d10
0 ImagesSynonyms: 5,5-Diphenylhydantoin-d10Phenytoin-d10 is the deuterium labeled Phenytoin. Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na+ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.
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Ropivacaine-d7
0 ImagesRopivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent?sodium channel?blocker. Ropivacain blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane. Ropivacaine is used for the research of neuropathic pain?management.
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NS383
0 ImagesNS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits.
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Phenamil methanesulfonate
0 ImagesPhenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM. Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay. Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
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Azimilide dihydrochloride
0 ImagesSynonyms: NE-10064 dihydrochlorideAzimilide (NE-10064) dihydrochloride is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide dihydrochloride is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide dihydrochloride blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide dihydrochloride also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide dihydrochloride can be used for the study of atrial fibrillation and ventricular fibrillation.
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Nav1.7 inhibitor
0 ImagesNav1.7 inhibitor (compound II), a sulfonamide, is a potent Nav1.7 inhibitor. Nav1.7 inhibitor has the potential for a wide range of disorders, particularly pain, including acute pain, inflammatory pain and/or neuropathic pain.
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Licarbazepine
0 ImagesSynonyms: BIA 2-005; GP 47779Licarbazepine (BIA 2-005; GP 47779) is a voltage-gated sodium channel blocker with anticonvulsant and mood-stabilizing effects.
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Azimilide
0 ImagesSynonyms: NE-10064Azimilide (NE-10064) is a class III antiarrhythmic agent, which works by blocking potassium channels in the heart. Azimilide is a dual blocker of IKs (IC50 = 2.6 μM (2mM [K⁺]ₑ)) and IKr (IC50 = 1 μM (4 mM [K⁺])). Azimilide blocked HERG channel at 0.1 and 1 Hz with IC50s of 1.4 μM and 5.2 μM respectively. Azimilide also inhibits L-type calcium current (ICa) (IC50 = 17.8 μM) and sodium current (INa) (IC50 = 19 μM). Azimilide can be used for the study of atrial fibrillation and ventricular fibrillation.
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DS-1971a
0 ImagesDS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.
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GNE-131
0 ImagesGNE-131 is a potent and selective inhibitor of human sodium channel NaV1.7, with an IC50 of 3 nM.
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PF-06649298
0 ImagesPF-06649298 is a sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor. PF-06649298 specifically interacts with NaCT with an IC50 value of 16.2 μM to inhibits the transport of citrate in human hepatocytes. PF-06649298 can be used for the research of regulating glucose metabolism and lipid metabolism.
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Nisoxetine
0 ImagesNisoxetine is a potent and selective inhibitor of noradrenaline transporter (NET), with a Kd of 0.76 nM. Nisoxetine is an antidepressant and local anesthetic, it can block voltage-gated sodium channels.
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DAPI dihydrochloride (solution)
0 ImagesCat. No.: HY-DY1081CAS No.: 28718-90-3Synonyms: 4',6-Diamidino-2-phenylindole dihydrochloride (solution)DAPI (4',6-Diamidino-2-phenylindole) dihydrochloride (solution) is a DAPI dye. DAPI is a fluorescent dye that binds strongly to DNA. It binds to the AT base pair of the double-stranded DNA minor groove, and one DAPI molecule can occupy three base pair positions. The fluorescence intensity of DAPI molecules bound to double-stranded DNA is increased by about 20 times, and it is commonly observed with fluorescence microscopy, and the amount of DNA can be determined based on the intensity of fluorescence. DAPI cannot penetrate intact cell membranes and is commonly used for staining damaged and fixed cells. DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment (Ex/Em = 356/451 nm).
Solvent and concentration: ddH2O: 5 mg/mL
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Amitriptyline hydrochloride (Standard)
0 ImagesAmitriptyline hydrochloride (Standard) is the analytical standard of Amitriptyline hydrochloride (HY-B0527A). This product is intended for research and analytical applications. 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.
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(±)-Indoxacarb
0 ImagesSynonyms: (RS)-Indoxacarb; DPX-JW062Indoxacarb ((±)-Indoxacarb; DPX-JW062) is a broad-spectrum oxadiazine insecticide with high insecticidal activity and low mammalian toxicity. Indoxacarb blocks insect sodium channels in nerve preparations and isolated neurons.
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(+)-Kavain
0 Images(+)-Kavain, a main kavalactone that can be extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels. (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy. (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied.
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ErSO-TFPy
0 ImagesSynonyms: TEQ103; Sera2ErSO-TFPy (TEQ103) is an ERα+ tumor cell inhibitor with low nanomolar cytotoxic activity against ERα+ breast cancer cells. ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy dysregulates calcium homeostasis in ERα+ tumor cells, triggers the anticipatory unfolded protein response, and induces rapid immune cell-independent necrotic cell death. ErSO-TFPy can be used for the research of estrogen receptor alpha positive breast cancer.
