Sodium Channel

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Sodium Channel Products

All (57) Sodium Channel Inhibitors (54) Sodium Channel Activators (1) Sodium Channel Antagonists (2)

Catalog No.	Information	Product Use Citations	Product Validations
S1614	Riluzole Riluzole (RP-54274, PK 26124) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183 J Cell Biochem, 2019, 10.1002/jcb.29533	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
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 Breast Cancer Res Treat, 2015, 150(3):535-45
S1811	Amiloride HCl Amiloride 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).	Signal Transduct Target Ther, 2020, 5(1):214 PLoS Genet, 2020, 16(10):e1009100 Drug Discov Ther, 2020, 14(5):256-258
S1256	Rufinamide Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
S1603	Furosemide Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.	Sci Rep, 2018, 8(1):9302 Biomed Pharmacother, 2018, 101:145-154 Vascul Pharmacol, 2017, 99:74-82
S6920^New	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.
S4339^New	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.
S0016^New	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.
S1445	Zonisamide Zonisamide (CI-912) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
S2524	Phenytoin Sodium Phenytoin Sodium (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
S1693	Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.	PLoS One, 2019, 14(2):e0211644 DNA Cell Biol, 2019, 10.1089/dna.2018.4553
S2785	A-803467 A-803467 is a selective Na_V1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human Na_V1.2, Na_V1.3, Na_V1.5, and Na_V1.7.
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.	PLoS Genet, 2020, 16(10):e1009100 Sci Rep, 2017, 7(1):5586 Peptides, 2015, 73:67-76
S1287	Bumetanide Bumetanide (Bumex) is a loop diuretic of the sulfamyl category to treat heart failure. Bumetanide is a selective Na+-K+-Cl- cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.	Cell Mol Gastroenterol Hepatol, 2019, 10.1016/j
S2525	Phenytoin Phenytoin (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
S2874	Camostat Mesilate Camostat (FOY-305) 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.	EMBO J, 2020, e2020106057 Sci Immunol, 2020, 13;5(47):eabc3582 bioRxiv, 2020, 2020.11.04.364315
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).	Cell Syst, 2019, 8(2):97-108 Nat Commun, 2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
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.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1965	Primidone Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.
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.
S2041	Dyclonine HCl Dyclonine 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.
S4229	Oxybuprocaine HCl Oxybuprocaine HCl 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
S3155	Mepivacaine HCl Mepivacaine is a tertiary amine used as a local anesthetic.
S2500	Propafenone HCl Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.
S9142	Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
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 K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
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.
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.
S5274	GS967 GS967 (GS458967) is a potent and selective inhibitor of late I_Na with anti-arrhythmic actions.
S4038	Dibucaine HCl Dibucaine HCl (Cinchocaine) is a local anesthetics.
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.
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.
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.
S4058	Ropivacaine HCl Ropivacaine HCl (LEA-103) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.	Cancer Discov, 2020, CD-20-0160
S4180	Nefopam HCl Nefopam HCl is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.
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.
S5814	cariporide Cariporide is a selective and potent inhibitor of NHE1 with an IC50 of 30 nM for hNHE1 in CHO-K1 cells.	Int J Med Sci, 2020, 17(11):1652-1664
S4080	Triamterene Triamterene (SKF8542) blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.	Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
S8615	Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na⁺-K⁺-2Cl^- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.	Cell Death Dis, 2020, 11(11):991
S5710	Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
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.
S4200	Tolperisone HCl Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.
S4210	Benzocaine Benzocaine 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.
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.
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.
S4225	Mexiletine HCl Mexiletine HCl (KO1173) 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
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
S3751	Quinidine sulfate Quinidine (Chinidin, Pitayine, β-quinine, (+)-quinidine) acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.	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.
S4284	Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
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.	Biomaterials, 2020, 232:119701 Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734
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
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.	Gynecol Oncol, 2018, 151(3):525-532
S4294	Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
S3250^New	Veratrine Veratridine, a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.
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.
S1828	Proparacaine HCl Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.

Catalog No.	Information	Product Use Citations	Product Validations
S1614	Riluzole Riluzole (RP-54274, PK 26124) is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Cancer Res, 2019, 79(8):1799-1809 Neuropharmacology, 2019, 150:175-183 J Cell Biochem, 2019, 10.1002/jcb.29533	Spatial memory performance. a Latency to find the hidden platform. LPS-infused controls and Aged controls were impaired (p<0.001) compared to young aCSF-infused rats. The performance of Aged rats improved across days only when treated with Ril (†t=0.035). b Distance. LPS controls swam a greater distance than aCSF controls and Aged controls (p≤0.036). c Swim Speed. Aged rats swam the most slowly (p≤0.001). d Thigmotaxis. Aged controls spent the greatest percentage of time within the pool perimeter (p<0.001).
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 Breast Cancer Res Treat, 2015, 150(3):535-45
S1811	Amiloride HCl Amiloride 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).	Signal Transduct Target Ther, 2020, 5(1):214 PLoS Genet, 2020, 16(10):e1009100 Drug Discov Ther, 2020, 14(5):256-258
S1256	Rufinamide Rufinamide (CGP 33101) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
S1603	Furosemide Furosemide is a potent NKCC2 (Na-K-2Cl symporter) inhibitor, used in the treatment of congestive heart failure and edema.	Sci Rep, 2018, 8(1):9302 Biomed Pharmacother, 2018, 101:145-154 Vascul Pharmacol, 2017, 99:74-82
S6920^New	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.
S4339^New	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.
S0016^New	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.
S1445	Zonisamide Zonisamide (CI-912) is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
S2524	Phenytoin Sodium Phenytoin Sodium (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
S1693	Carbamazepine Carbamazepine (Carbatrol, NSC 169864) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.	PLoS One, 2019, 14(2):e0211644 DNA Cell Biol, 2019, 10.1089/dna.2018.4553
S2785	A-803467 A-803467 is a selective Na_V1.8 channel blocker with IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibits >100-fold selectivity against human Na_V1.2, Na_V1.3, Na_V1.5, and Na_V1.7.
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.	PLoS Genet, 2020, 16(10):e1009100 Sci Rep, 2017, 7(1):5586 Peptides, 2015, 73:67-76
S1287	Bumetanide Bumetanide (Bumex) is a loop diuretic of the sulfamyl category to treat heart failure. Bumetanide is a selective Na+-K+-Cl- cotransporter 1 (NKCC1) inhibitor, weakly inhibits NKCC2, with IC50s of 0.68 and 4.0 μM for hNKCC1A and hNKCC2A, respectively.	Cell Mol Gastroenterol Hepatol, 2019, 10.1016/j
S2525	Phenytoin Phenytoin (Diphenylhydantoin) is an inactive voltage-gated sodium channel stabilizer.
S2874	Camostat Mesilate Camostat (FOY-305) 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.	EMBO J, 2020, e2020106057 Sci Immunol, 2020, 13;5(47):eabc3582 bioRxiv, 2020, 2020.11.04.364315
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).	Cell Syst, 2019, 8(2):97-108 Nat Commun, 2016, 7:13023	Results of hit validation experiments for these four compounds for animals treated at L1 stage at four different concentrations (0.5, 5, 25, and 50 μM). The blue bars represent the values obtained from the original screen as reference points. Error bars are standard error of the mean. Statistical significance for all different doses for individual compounds was calculated with respect to the lowest concentration using two-tailed, t-test (nZ70 animals except n = 37 for Geld 25 μM). The statistical significance values are represented as P<0.05 () and P<0.005 (*).
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.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S1965	Primidone Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.
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.
S2041	Dyclonine HCl Dyclonine 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.
S4229	Oxybuprocaine HCl Oxybuprocaine HCl 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
S3155	Mepivacaine HCl Mepivacaine is a tertiary amine used as a local anesthetic.
S2500	Propafenone HCl Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.
S9142	Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
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 K_D of 1.7 μM.	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. p<0.05, *p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
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.
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.
S5274	GS967 GS967 (GS458967) is a potent and selective inhibitor of late I_Na with anti-arrhythmic actions.
S4038	Dibucaine HCl Dibucaine HCl (Cinchocaine) is a local anesthetics.
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.
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.
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.
S4058	Ropivacaine HCl Ropivacaine HCl (LEA-103) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.	Cancer Discov, 2020, CD-20-0160
S4180	Nefopam HCl Nefopam HCl is a centrally-acting but non-opioid analgesic drug by blocking voltage-gated sodium channel and inhibition of serotonin, dopamine and noradrenaline reuptake.
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.
S5814	cariporide Cariporide is a selective and potent inhibitor of NHE1 with an IC50 of 30 nM for hNHE1 in CHO-K1 cells.	Int J Med Sci, 2020, 17(11):1652-1664
S4080	Triamterene Triamterene (SKF8542) blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.	Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
S8615	Sodium dichloroacetate (DCA) Sodium dichloroacetate (DCA, Dichloroacetic acid, bichloroacetic acid, BCA), a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress Na⁺-K⁺-2Cl^- cotransporter and a mitochondrial potassium-ion channel axis. Sodium dichloroacetate increases reactive oxygen species (ROS) generation, triggers apoptosis in cancer cells, and inhibits tumor growth.	Cell Death Dis, 2020, 11(11):991
S5710	Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
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.
S4200	Tolperisone HCl Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.
S4210	Benzocaine Benzocaine 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.
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.
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.
S4225	Mexiletine HCl Mexiletine HCl (KO1173) 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
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
S3751	Quinidine sulfate Quinidine (Chinidin, Pitayine, β-quinine, (+)-quinidine) acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.	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.
S4284	Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
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.	Biomaterials, 2020, 232:119701 Drug Metab Dispos, 2020, 48(8):613-621 bioRxiv, 2020, 2020/9/20.4.7.30734
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
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.	Gynecol Oncol, 2018, 151(3):525-532
S4294	Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.

Catalog No.	Information	Product Use Citations	Product Validations
S3250^New	Veratrine Veratridine, a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.

Catalog No.

Information

Product Use Citations

Product Validations

S3250^New

Veratrine

Veratridine, a steroidal alkaloid found in plants of the lily family, is a voltage-gated sodium channel activator. Veratridine induces anxiogenic-like behaviors in rats.

Catalog No.	Information	Product Use Citations	Product Validations
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.
S1828	Proparacaine HCl Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.

Catalog No.

Information

Product Use Citations

Product Validations

S3911

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.

S1828

Proparacaine HCl

Proparacaine HCl is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.

Choose Your Country or Region

By Signaling Pathways

By product type

Sodium Channel

Signaling Pathway Map

Research Area

Inhibitory Selectivity

Sodium Channel Products