Home Transmembrane Transporters Sodium Channel

Sodium Channel

Choose Selective Sodium Channel Inhibitors

Sodium Channel Signaling Pathway Map

Sodium Channel Signaling Pathways

Sodium Channel Products

  • All (65)
  • Sodium Channel Inhibitors (60)
  • Sodium Channel Activator (1)
  • Sodium Channel Antagonists (2)
  • New Sodium Channel Products
Catalog No. Product Name Information Product Use Citations Product Validations
E0144New Vernakalant (RSD1235) Hydrochloride

Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
S0016 SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S0036 PF-06869206 PF-06869206 is a selective inhibitor of NPT2a (also referred to as NaPi2a or SLC34A1) with an IC50 of 380 nM.
S0312 Rimeporide Rimeporide(EMD-87580) is a sodium hydrogen exchanger (NHE-1) inhibitor indicated for patients with Duchenne muscular dystrophy.
S1256 Rufinamide Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
S1335 VX-150 VX-150 (EOS-62073) is an orally bioavailable pro-drug that rapidly converts into its active moiety, which is a highly selective inhibitor of NaV1.8 relative to the other sodium channel subtypes (>400-fold).
S1391 Oxcarbazepine Oxcarbazepine (GP47680) inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.
S1445 Zonisamide Zonisamide (CI-912) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
Exp Neurol, 2021, S0014-4886(21)00182-5
S1614 Riluzole (PK 26124) Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Front Bioeng Biotechnol, 2022, 10:855755
Adv Biol (Weinh), 2022, e2101184
Mol Genet Metab, 2021, S1096-7192(21)00826-X
S1619 Prilocaine Prilocaine (NSC 40027) is a local anesthetic of the amino amide type. It acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation.
Nat Prod Res, 2021, 1-7
S1693 Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
mBio, 2022, e0217721
Front Pharmacol, 2021, 12:749930
Anticancer Res, 2021, 41(2):687-697
S1811 Amiloride (MK-870) HCl Amiloride (MK-870) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
PLoS Pathog, 2022, 18(6):e1010620
Mol Ther Methods Clin Dev, 2022, 24:11-19
Adv Sci (Weinh), 2021, 8(13):2100962
S1965 Primidone Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.
Life Sci, 2021, 268:118967
S2041 Dyclonine HCl Dyclonine HCl(Dyclocaine HCl) is a hydrochloride salt form of dyclonine which is an oral anaesthetic, reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation.
S2110 Vinpocetine Vinpocetine (RGH-4405) is a selective inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.
An Acad Bras Cienc, 2020, 92(4):e20200241
S2114 Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
Nat Commun, 2016, 7:13023
S2118 Ibutilide Fumarate Ibutilide Fumarate (U-70226E) is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current, which prolongs action potential and refractory period of myocardial cells.
Mol Pharmacol, 2022, 101(4):236-245
Gynecol Oncol, 2018, 151(3):525-532
S2318 Lappaconitine Lappaconitine (LC) is a natural diterpenoid alkaloid (DTA), acting as a human heart sodium channel blocker and possessing a wide range of biological activities, including anti-arrhythmic, anti-inflammatory, antioxidative, anticancer, epileptiform etc.
S2454 Bupivacaine HCl Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias.
Int J Mol Sci, 2019, 20(17)
J Steroid Biochem Mol Biol, 2017, 172:89-97
Sci Rep, 2015, 5:17772
S2500 Propafenone HCl Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.
S2524 Phenytoin Sodium Phenytoin Sodium (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
Proc Natl Acad Sci U S A, 2021, 118(11)e2100066118
S2525 Phenytoin Phenytoin (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
S2560 Amiloride HCl dihydrate Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
Mol Ther Methods Clin Dev, 2022, 24:11-19
Theranostics, 2021, 11(5):2364-2380
J Colloid Interface Sci, 2021, 601:650-660
S2785 A-803467 A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.
S2874 Camostat Mesilate Camostat (FOY-305, FOY-S980) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.
Front Microbiol, 2022, 13:884034
Antiviral Res, 2022, 202:105325
J Cell Biochem, 2022, 10.1002/jcb.30213
S3024 Lamotrigine Lamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
Nat Commun, 2022, 13(1):2785
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S3064 Ambroxol HCl AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
S3074 Chlorthalidone Chlortalidone (Chlortalidone) is a diuretic drug widely used in antihypertensive therapy.
S3155 Mepivacaine HCl Mepivacaine is a tertiary amine used as a local anesthetic.
S3751 Quinidine sulfate Quinidine (Chinidin, Pitayine, β-quinine, (+)-quinidine) acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.
J Biomed Res, 2021, 35(5):395-407
J Pharmacol Toxicol Methods, 2020, 106895
S3907 Bulleyaconi cine A Bulleyaconi cine A (Bulleyaconitine A, BLA) is an active ingredient of Aconitum bulleyanum plants and classified as an "aconitine-like" alkaloid. It is a potent use-dependent blocker for both Nav1.7 and Nav1.8 Na+ currents.
S4023 Procaine HCl Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.
Biomol Ther (Seoul), 2016, 24(5):489-94
Biomol Ther (Seoul), 2016, 24(5):489-94
S4038 Dibucaine HCl Dibucaine HCl (Cinchocaine) is a local anesthetics.
S4058 Ropivacaine HCl Ropivacaine HCl (LEA-103) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.
Elife, 2021, 10e65962
Oncol Rep, 2020, 43(5):1659-1668
Cancer Discov, 2020, CD-20-0160
S4061 Levobupivacaine HCl Levobupivacaine HCl ((S)-(-)-Bupivacaine), the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.
S4080 Triamterene Triamterene (SKF8542) blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
Nat Commun, 2021, 12(1):6479
Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
S4180 Nefopam HCl Nefopam HCl(Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.
S4200 Tolperisone HCl Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.
S4210 Benzocaine Benzocaine(ethyl 4-aminobenzoate) is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.
S4225 Mexiletine HCl Mexiletine HCl (KO1173,Mexitil) belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.
Biogerontology, 2016, 17(5-6):907-920
S4229 Oxybuprocaine HCl Oxybuprocaine HCl(oxybuprocaine hydrochloride) is a local anesthetic, which is used especially in ophthalmology and otolaryngology. Oxybuprocaine binds to sodium channel and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions
S4235 Phenazopyridine HCl Phenazopyridine HCl is a local analgesic that has been used in urinary tract disorders. It is an inhibitor of sodium channel protein type 1 subunit alpha.
bioRxiv, 2020, 2020/9/20.4.7.30734
S4284 Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
S4294 Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
S4339 Meticrane Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension.
S4657 Eslicarbazepine Acetate Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom), an antiepileptic drug, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
S4668 Procaine Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses.
S4669 Benzocaine hydrochloride Benzocaine hydrochloride (Ethyl 4-aminobenzoate, Ethyl p-aminobenzoate) is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.
S5181 Levobupivacaine Levobupivacaine (Chirocaine, (S)-(-)-Bupivacaine, L-(-)-Bupivacaine), the S (-)-enantiomer of bupivacaine, is a long-acting amide local anaesthetic used in analgesia and anaesthesia. Levobupivacaine exhibits effects on motor and sensory nerves by inhibiting the opening of voltage-gated sodium channels.
S5274 GS967 GS967 (GS458967) is a potent and selective inhibitor of late INa with anti-arrhythmic actions.
S5490 Disopyramide Disopyramide is a class IA antiarrhythmic drug which acts via blockade of sodium channels depressing phase 0 of the action potential. Disopyramide possesses significant negative inotropic, anticholinergic effects and enhances AV nodal conduction.
S5556 (-)-Sparteine Sulfate Sparteine Sulfate, a quinolizidine alkaloid, is the sulfate form of sparteini, which is a sodium channel blocker used as an oxytocic and an anti-arrhythmia agent.
S5710 Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
S5749 Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Pharmaceuticals (Basel), 2022, 15(2)241
Bioorg Chem, 2022, 127:106008
S5789 Propafenone Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias.
S5814 cariporide Cariporide is a selective and potent inhibitor of NHE1 with an IC50 of 30 nM for hNHE1 in CHO-K1 cells.
J Int Med Res, 2022, 50(5):3000605221097490
Int J Med Sci, 2020, 17(11):1652-1664
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
S9142 Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
S9849New 5-(N-Ethyl-N-isopropyl)-Amiloride (EIPA) 5-(N-Ethyl-N-isopropyl)-Amiloride (EIPA) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis.
Int J Mol Sci, 2022, 23(8)4419
Viruses, 2022, 14(3)496
S3250 Veratrine Veratridine (Cevadine, Cevadin, Cevadene), a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.
S1828 Proparacaine HCl Proparacaine HCl(Proxymetacaine Hydrochloride) is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
S3911 Veratramine Veratramine (NSC 17821, NSC 23880), a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.
S5534 Cinchocaine Cinchocaine (Dibucaine) is a potent and long-acting local anesthetics used for surface anesthesia.
S9446 Dihydrokavain Dihydrokavain (Marindinin) is a kavalactone source from kava beverages used in herbal medicine to treat sleep disturbances, as well as stress and anxiety.
E0144New Vernakalant (RSD1235) Hydrochloride

Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
S0016 SN-6 SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. SN-6 inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. SN-6 abolishes acetylcholine (ACh)-induced vasodilation.
S0036 PF-06869206 PF-06869206 is a selective inhibitor of NPT2a (also referred to as NaPi2a or SLC34A1) with an IC50 of 380 nM.
S0312 Rimeporide Rimeporide(EMD-87580) is a sodium hydrogen exchanger (NHE-1) inhibitor indicated for patients with Duchenne muscular dystrophy.
S1256 Rufinamide Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
S1335 VX-150 VX-150 (EOS-62073) is an orally bioavailable pro-drug that rapidly converts into its active moiety, which is a highly selective inhibitor of NaV1.8 relative to the other sodium channel subtypes (>400-fold).
S1391 Oxcarbazepine Oxcarbazepine (GP47680) inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.
S1445 Zonisamide Zonisamide (CI-912) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
Exp Neurol, 2021, S0014-4886(21)00182-5
S1614 Riluzole (PK 26124) Riluzole (PK 26124, RP-54274) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Front Bioeng Biotechnol, 2022, 10:855755
Adv Biol (Weinh), 2022, e2101184
Mol Genet Metab, 2021, S1096-7192(21)00826-X
S1619 Prilocaine Prilocaine (NSC 40027) is a local anesthetic of the amino amide type. It acts on sodium channels on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation.
Nat Prod Res, 2021, 1-7
S1693 Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
mBio, 2022, e0217721
Front Pharmacol, 2021, 12:749930
Anticancer Res, 2021, 41(2):687-697
S1811 Amiloride (MK-870) HCl Amiloride (MK-870) is a selective T-type calcium channel blocker, an epithelial sodium channel blocker and a selective inhibitor of urokinase plasminogen activator (uPA)(Ki=7 μM).
PLoS Pathog, 2022, 18(6):e1010620
Mol Ther Methods Clin Dev, 2022, 24:11-19
Adv Sci (Weinh), 2021, 8(13):2100962
S1965 Primidone Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.
Life Sci, 2021, 268:118967
S2041 Dyclonine HCl Dyclonine HCl(Dyclocaine HCl) is a hydrochloride salt form of dyclonine which is an oral anaesthetic, reversibly binds to activated sodium channels on the neuronal membrane, thereby decreasing the neuronal membrane's permeability to sodium ions, leading to an increased threshold for excitation.
S2110 Vinpocetine Vinpocetine (RGH-4405) is a selective inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.
An Acad Bras Cienc, 2020, 92(4):e20200241
S2114 Dronedarone HCl Dronedarone HCl (SR33589) is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
Nat Commun, 2016, 7:13023
S2118 Ibutilide Fumarate Ibutilide Fumarate (U-70226E) is a Class III antiarrhythmic agent that is indicated for acute cardioconversion of atrial fibrillation and atrial flutter of a recent onset to sinus rhythm by induction of slow inward sodium current, which prolongs action potential and refractory period of myocardial cells.
Mol Pharmacol, 2022, 101(4):236-245
Gynecol Oncol, 2018, 151(3):525-532
S2318 Lappaconitine Lappaconitine (LC) is a natural diterpenoid alkaloid (DTA), acting as a human heart sodium channel blocker and possessing a wide range of biological activities, including anti-arrhythmic, anti-inflammatory, antioxidative, anticancer, epileptiform etc.
S2454 Bupivacaine HCl Bupivacaine HCl binds to the intracellular portion of voltage-gated sodium channels and blocks sodium influx into nerve cells, used for treating cardiac arrhythmias.
Int J Mol Sci, 2019, 20(17)
J Steroid Biochem Mol Biol, 2017, 172:89-97
Sci Rep, 2015, 5:17772
S2500 Propafenone HCl Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.
S2524 Phenytoin Sodium Phenytoin Sodium (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
Proc Natl Acad Sci U S A, 2021, 118(11)e2100066118
S2525 Phenytoin Phenytoin (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
S2560 Amiloride HCl dihydrate Amiloride HCl dihydrate is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
Mol Ther Methods Clin Dev, 2022, 24:11-19
Theranostics, 2021, 11(5):2364-2380
J Colloid Interface Sci, 2021, 601:650-660
S2785 A-803467 A-803467 is a selective NaV1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human NaV1.2, NaV1.3, NaV1.5, and NaV1.7.
S2874 Camostat Mesilate Camostat (FOY-305, FOY-S980) is a trypsin-like protease inhibitor, inhibits airway epithelial sodium channel (ENaC) function with IC50 of 50 nM, less potent to trpsin, prostasin and matriptase.
Front Microbiol, 2022, 13:884034
Antiviral Res, 2022, 202:105325
J Cell Biochem, 2022, 10.1002/jcb.30213
S3024 Lamotrigine Lamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
Nat Commun, 2022, 13(1):2785
Hum Cell, 2022, 10.1007/s13577-022-00671-y
Hum Cell, 2021, 10.1007/s13577-021-00639-4
S3064 Ambroxol HCl AmbroxolHCl is a potent inhibitor of the neuronal Na+ channels, inhibits TTX-resistant Na+ currents with IC50 of 35.2 μM and 22.5 μM for tonic and phasic block, inhibits TTX-sensitive Na+ currents with IC50 of 100 μM. Phase 3.
S3074 Chlorthalidone Chlortalidone (Chlortalidone) is a diuretic drug widely used in antihypertensive therapy.
S3155 Mepivacaine HCl Mepivacaine is a tertiary amine used as a local anesthetic.
S3751 Quinidine sulfate Quinidine (Chinidin, Pitayine, β-quinine, (+)-quinidine) acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.
J Biomed Res, 2021, 35(5):395-407
J Pharmacol Toxicol Methods, 2020, 106895
S3907 Bulleyaconi cine A Bulleyaconi cine A (Bulleyaconitine A, BLA) is an active ingredient of Aconitum bulleyanum plants and classified as an "aconitine-like" alkaloid. It is a potent use-dependent blocker for both Nav1.7 and Nav1.8 Na+ currents.
S4023 Procaine HCl Procaine (Novocaine) is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.
Biomol Ther (Seoul), 2016, 24(5):489-94
Biomol Ther (Seoul), 2016, 24(5):489-94
S4038 Dibucaine HCl Dibucaine HCl (Cinchocaine) is a local anesthetics.
S4058 Ropivacaine HCl Ropivacaine HCl (LEA-103) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.
Elife, 2021, 10e65962
Oncol Rep, 2020, 43(5):1659-1668
Cancer Discov, 2020, CD-20-0160
S4061 Levobupivacaine HCl Levobupivacaine HCl ((S)-(-)-Bupivacaine), the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.
S4080 Triamterene Triamterene (SKF8542) blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
Nat Commun, 2021, 12(1):6479
Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
S4180 Nefopam HCl Nefopam HCl(Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.
S4200 Tolperisone HCl Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.
S4210 Benzocaine Benzocaine(ethyl 4-aminobenzoate) is the ethyl ester of p-aminobenzoic acid (PABA), it is a local anesthetic commonly used as a topical pain reliever or in cough drops.
S4225 Mexiletine HCl Mexiletine HCl (KO1173,Mexitil) belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.
Biogerontology, 2016, 17(5-6):907-920
S4229 Oxybuprocaine HCl Oxybuprocaine HCl(oxybuprocaine hydrochloride) is a local anesthetic, which is used especially in ophthalmology and otolaryngology. Oxybuprocaine binds to sodium channel and reversibly stabilizes the neuronal membrane which decreases its permeability to sodium ions
S4235 Phenazopyridine HCl Phenazopyridine HCl is a local analgesic that has been used in urinary tract disorders. It is an inhibitor of sodium channel protein type 1 subunit alpha.
bioRxiv, 2020, 2020/9/20.4.7.30734
S4284 Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
S4294 Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
S4339 Meticrane Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. Meticrane is used to treat essential hypertension.
S4657 Eslicarbazepine Acetate Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom), an antiepileptic drug, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
S4668 Procaine Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses.
S4669 Benzocaine hydrochloride Benzocaine hydrochloride (Ethyl 4-aminobenzoate, Ethyl p-aminobenzoate) is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.
S5181 Levobupivacaine Levobupivacaine (Chirocaine, (S)-(-)-Bupivacaine, L-(-)-Bupivacaine), the S (-)-enantiomer of bupivacaine, is a long-acting amide local anaesthetic used in analgesia and anaesthesia. Levobupivacaine exhibits effects on motor and sensory nerves by inhibiting the opening of voltage-gated sodium channels.
S5274 GS967 GS967 (GS458967) is a potent and selective inhibitor of late INa with anti-arrhythmic actions.
S5490 Disopyramide Disopyramide is a class IA antiarrhythmic drug which acts via blockade of sodium channels depressing phase 0 of the action potential. Disopyramide possesses significant negative inotropic, anticholinergic effects and enhances AV nodal conduction.
S5556 (-)-Sparteine Sulfate Sparteine Sulfate, a quinolizidine alkaloid, is the sulfate form of sparteini, which is a sodium channel blocker used as an oxytocic and an anti-arrhythmia agent.
S5710 Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
S5749 Chlorpromazine Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Pharmaceuticals (Basel), 2022, 15(2)241
Bioorg Chem, 2022, 127:106008
S5789 Propafenone Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. Propafenone offers a broad spectrum of activity in the treatment of cardiac arrhythmias.
S5814 cariporide Cariporide is a selective and potent inhibitor of NHE1 with an IC50 of 30 nM for hNHE1 in CHO-K1 cells.
J Int Med Res, 2022, 50(5):3000605221097490
Int J Med Sci, 2020, 17(11):1652-1664
S6920 SEA0400 SEA0400 is a selective and potent inhibitor of the Na+-Ca2+ exchanger (NCX) that inhibits Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50 of 33 nM, 5.0 nM and 8.3 nM, respectively. SEA0400 prevents sodium nitroprusside (SNP) from increasing ERK and p38 MAPK phosphorylation and production of reactive oxygen species (ROS) in an extracellular Ca(2+)-dependent manner.
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
S9142 Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
S9849New 5-(N-Ethyl-N-isopropyl)-Amiloride (EIPA) 5-(N-Ethyl-N-isopropyl)-Amiloride (EIPA) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis.
Int J Mol Sci, 2022, 23(8)4419
Viruses, 2022, 14(3)496
S3250 Veratrine Veratridine (Cevadine, Cevadin, Cevadene), a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.
S1828 Proparacaine HCl Proparacaine HCl(Proxymetacaine Hydrochloride) is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
S3911 Veratramine Veratramine (NSC 17821, NSC 23880), a major alkaloid from Veratrum nigrum L., has distinct anti-tumor and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has a good stability in the gastrointestinal tract during its absorption.
E0144New Vernakalant (RSD1235) Hydrochloride

Vernakalant (RSD-1235, MK-6621) is a novel, frequency-dependent Na+ channel and early activating K+ channel blocker that selectively prolongs the atrial refractory period.
S9849New 5-(N-Ethyl-N-isopropyl)-Amiloride (EIPA) 5-(N-Ethyl-N-isopropyl)-Amiloride (EIPA) acts as an inhibitor of macropinocytosis and sodium-hydrogen exchangers(NHE) (IC50=0.033μg/mL). EIPA blocks the activity of Na(+)/H(+) exchanger, which are plasma membrane proteins implicated in all forms of macropinocytosis.
Int J Mol Sci, 2022, 23(8)4419
Viruses, 2022, 14(3)496
Tags: Sodium Channel inhibitor|Sodium Channel agonist|Sodium Channel activator|Sodium Channel inducer|Sodium Channel antagonist|Sodium Channel signaling pathway|Sodium Channel assay kit