2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. Sodium Channel

Sodium Channel

Na channels; Na+ channels

Sodium Channel

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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:

Sodium Channel Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-139346
    VX-150
    		Inhibitor 98.36%
    VX-150 is an orally active, highly selective NaV1.8 inhibitor. VX-150 has the potential for various pain indications research.
    VX-150
  • HY-101383
    PF-01247324
    		Inhibitor 99.77%
    PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
    PF-01247324
  • HY-B1167
    Ajmaline
    		Inhibitor 99.73%
    Ajmaline (Cardiorythmine) is a sodium channel blocking, class 1A anti-arrhythmic agent. Ajmaline blocks HERG currents with an IC50 of 1 μM in HEK cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia.
    Ajmaline
  • HY-120669
    PF-06761281
    		Inhibitor 99.52%
    PF-06761281 (Compound 4a) is a potent, orally active, partial selective sodium-coupled citrate transporter (NaCT or SLC13A5) inhibitor with IC50 values of 0.51, 13.2 and 14.1 µM against HEKNaCT, HEKNaDC1 and HEKNaDC3, respectively.
    PF-06761281
  • HY-B0653A
    Levobupivacaine hydrochloride
    		Inhibitor 99.86%
    Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer.
    Levobupivacaine hydrochloride
  • HY-B0285AR
    Amiloride hydrochloride (Standard)
    		Inhibitor
    Amiloride (hydrochloride) (Standard) is the analytical standard of Amiloride (hydrochloride). This product is intended for research and analytical applications. Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.
    Amiloride hydrochloride (Standard)
  • HY-126429
    Nav1.1 activator 1
    		Activator 98.98%
    Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.
    Nav1.1 activator 1
  • HY-120026
    KB130015
    		Modulator 98.45%
    KB130015 (KB015) is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na+ channels. KB130015 activates hERG1 channels (EC50 = 12.2 μM) and large-conductance Ca2+-activated K+ (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease.
    KB130015
  • HY-145894
    NaPi2b-IN-2
    		Inhibitor 98.93%
    NaPi2b-IN-2 (compound 5) is a potent inhibitor of sodium-dependent transport protein 2b (SLC34A2, NaPi2b), with an IC50 of 38 nM for human NaPi2b. NaPi2b-IN-2 can be used for the research of hyperphosphatemia.
    NaPi2b-IN-2
  • HY-107757
    GMQ hydrochloride
    		Activator 99.86%
    GMQ (hydrochloride) is a ASIC (acid-sensing ion) channel activator with an EC50 value of 1.83 mM for ASIC3 at pH 7.4. GMQ (hydrochloride) opens only ASIC3 but no other ASICs at pH 7.4. GMQ (hydrochloride) can be used for neurological disease research.
    GMQ hydrochloride
  • HY-101109
    Sodium ionophore III
    		99.86%
    Sodium ionophore III (ETH2120) is a Na+ ionophore suitable for the assay of sodium activity in blood, plasma, serum. etc.
    Sodium ionophore III
  • HY-B0824
    Bifenthrin
    		Activator 99.76%
    Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material.
    Bifenthrin
  • HY-B0185B
    Lidocaine hydrochloride hydrate
    		Inhibitor 99.80%
    Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia.
    Lidocaine hydrochloride hydrate
  • HY-B0563A
    Ropivacaine hydrochloride monohydrate
    		Inhibitor 99.82%
    Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and 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 widely used for regional anesthesia and neuropathic pain management in vivo.
    Ropivacaine hydrochloride monohydrate
  • HY-125990
    SLC13A5-IN-1
    		Inhibitor 98.62%
    SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
    SLC13A5-IN-1
  • HY-112065
    PF-06869206
    		Inhibitor 99.88%
    PF-06869206 is an orally bioavailable selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1) with an IC50 of 380 nM.
    PF-06869206
  • HY-148792
    Relutrigine
    		Inhibitor 99.13%
    Relutrigine (PRAX-562) is an orally active inhibitor of persistent sodium channel. Relutrigine potently and preferentially inhibits persistent INa induced by ATX-II (Nav 1.5 activator) or the SCN8A mutation N1768D with IC50 values of 141 nM and 75 nM, respectively. Relutrigine exhibits potent use-dependent block and reduces neuronal intrinsic excitability. Relutrigine has effective anticonvulsant activity.
    Relutrigine
  • HY-12545
    Brevetoxin-3
    		Activator
    Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.
    Brevetoxin-3
  • HY-B1657A
    Fosphenytoin disodium
    		Antagonist 99.81%
    Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.
    Fosphenytoin disodium
  • HY-114301
    PF-06305591
    		Inhibitor 99.74%
    PF-06305591 is a potent and highly selective voltage gated sodium channel NaV1.8 blocker, with an IC50 of 15 nM. An excellent preclinical in vitro ADME and safety profile.
    PF-06305591
Cat. No. Product Name / Synonyms Application Reactivity
Sodium Channel Isoform Comparison

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