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Sodium Channel

Sodium Channel Products

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Catalog No. Product Name Information Product Use Citations Product Validations
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.
Nat Commun, 2024, 15(1):1669
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
S1811 Amiloride HCl Amiloride HCl 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).
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
Virus Res, 2024, 339:199258
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.
CNS Neurosci Ther, 2024, 30(6):e14822
Elife, 2022, 11e77444
Antiviral Res, 2022, 202:105325
S1614 Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Neurotherapeutics, 2023, none
J Endocr Soc, 2023, 7(10):bvad117
Front Bioeng Biotechnol, 2022, 10:855755
S3024 Lamotrigine Lamotrigine (BW-430C,LTG) 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
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2560 Amiloride HCl dihydrate Amiloride HCl dihydrate(MK-870 hydrochloride dihydrate) is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
Adv Sci (Weinh), 2022, 9(29):e2202039
Mol Ther Methods Clin Dev, 2022, 24:11-19
Theranostics, 2021, 11(5):2364-2380
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
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
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).
Cancers (Basel), 2022, 14(19)4883
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
S9849 EIPA EIPA (L593754; MH 12-43) 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.
Gastroenterology, 2024, S0016-5085(24)05182-5
Microbiol Spectr, 2023, 10.1128/spectrum.02553-23
Int J Mol Sci, 2022, 23(8)4419
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
Cancer Discov, 2020, CD-20-0160
Oncol Rep, 2020, 43(5):1659-1668
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.
Anesthesiology, 2023, 139(6):782-800.
Redox Biol, 2022, 55:102427
S2525 Phenytoin Phenytoin (Di-Hydan, Dihycon, Dilabid, Diphedan, Diphenat, Diphenylan, Diphenylhydantoin, Hydantol, Lehydan, NSC 8722) is an inactive voltage-gated sodium channel stabilizer.
Front Cell Neurosci, 2023, 17:1175895
World J Gastroenterol, 2023, 29(20):3103-3118
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
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
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
S3751 Quinidine hemisulfate hydrate Quinidine hemisulfate hydrate(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
S2118 Ibutilide Fumarate Ibutilide Fumarate (U-70226E,Corvert Fumarate) 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
S1445 Zonisamide Zonisamide (Zonegran,CI-912,AD 810) 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
S2524 Phenytoin Sodium Phenytoin Sodium (Aleviatin, Diphenylhydantoin sodium, Eptoin, Phenytoin soluble, Prompt; Phenytek,Dilantin sodium, Diphantoine) is an inactive voltage-gated sodium channel stabilizer.
Proc Natl Acad Sci U S A, 2021, 118(11)e2100066118
S1965 Primidone Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.
Life Sci, 2021, 268:118967
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
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.
Virus Res, 2023, 10.1016/j.virusres.2023.199260
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
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
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.
Phytochem Anal, 2022, 33(7):1121-1134
S2110 Vinpocetine Vinpocetine (RGH-4405,Ethyl apovincaminate,AY 27255) 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
S1256 Rufinamide Rufinamide (CGP 33101,E 2080,RUF 331,Banzel) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
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(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.
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
S3155 Mepivacaine HCl Mepivacaine is a tertiary amine used as a local anesthetic.
E1186New Tenapanor Tenapanor (AZD1722, RDX5791) is a potent and orally active inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3). It exhibits an IC50 of 2 and 6 nM in human and mouse ileum monolayers, respectively. Tenapanor reduces intestinal phosphate absorption predominantly by reducing passive paracellular phosphate flux.
S0036 PF-06869206 PF-06869206 is a selective inhibitor of NPT2a (also referred to as NaPi2a or SLC34A1) with an IC50 of 380 nM.
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.
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 INa with anti-arrhythmic actions.
S0755 SLC13A5-IN-1 SLC13A5-IN-1 is a selective inhibitor of sodium-citrate co-transporter (SLC13A5/NaCT). It completely blocks the uptake of 14 C-citrate and has the potential for the treatment of metabolic and/or cardiovascular diseases.
S4038 Dibucaine HCl Dibucaine HCl (Cinchocaine) is a local anesthetics.
E4836New Bupivacaine Bupivacaine is a potent local anesthetic and sodium channel blocker used for local infiltration, nerve block, epidural, and intrathecal anesthesia. It significantly reduces cell viability and induces apoptosis. It also stimulates the production of ROS and activates MAPK pathways, which increases the expression of WDR35 in mouse neuroblastoma Neuro2a cells. It also activates NF-κB and c-Jun/AP-1 signalling pathways in Neuro2a cells.
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.
S0312 Rimeporide Rimeporide(EMD-87580) is a sodium hydrogen exchanger (NHE-1) inhibitor indicated for patients with Duchenne muscular dystrophy.
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.
S0073 BI 01383298 BI 01383298 is an irreversible and non-competitive inhibitor of human sodium-coupled citrate transporter (hNaCT), in which the inhibition is evident for the constitutively expressed transporter in HepG2 cells and for the ectopically expressed human NaCT in HEK293 cells, with IC50 of ~100 nM.
S3074 Chlorthalidone Chlortalidone (Chlortalidone) is a diuretic drug widely used in antihypertensive therapy.
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
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.
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.
NAR Genom Bioinform, 2024, 6(1):lqae001
E1612New Suzetrigine VX-548 (Suzetrigine), is an oral, highly selective inhibitor of voltage-gated sodium channel 1.8 (NaV1.8) with an IC50 of 0.7 nM. It can be used in research of transmitting nociceptive signals and treatment of acute pain after abdominoplasty or bunionectomy.
S9461 Benzonatate Benzonatate(Benzononatine) has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite.
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.
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.
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.
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.
E1929New LTGO-33 LTGO-33 is a potent and selective inhibitor of voltage-gated sodium channel NaV1.8. LTGO-33, with its potency in the nanomolar range, selectively inhibits NaV1.8 over 600 times more than human NaV1.1-NaV1.7 and NaV1.9. Its inhibition is not dependent on the state of the channels and displays consistent potency against both closed and inactivated conformations. LTGO-33 holds promise for research in pain disorders.
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).
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.
E0100 Sodium ionophore III Sodium ionophore III (ETH2120) is a Na+ ionophore suitable for the assay of sodium activity in blood, plasma, serum. etc.
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.
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.
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.
E4949New Eslicarbazepine Eslicarbazepine (BIA 2-194), an active metabolite of the prodrug eslicarbazepine acetate is an inhibitor of voltage-gated sodium channel (Nav). It acts by enhancing the slow activation of voltage-gated sodium channels, reducing their availability.
D4010 Lifastuzumab vedotin Lifastuzumab vedotin (LIFA, DNIB0600A, RG-7599) is an antibody-drug conjugate (ADC) composed of a humanized anti-NaPi2b monoclonal antibody and an anti-mitotic cytotoxic agent, monomethyl auristatin E (MMAE) . Lifastuzumab vedotin is used in the treatment of platinum-resistant ovarian cancer.
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.
S1828 Proparacaine HCl Proparacaine HCl(Proxymetacaine Hydrochloride) is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
S5534New Cinchocaine Dibucaine (Cinchocaine) is a potent, long-lasting local anesthetic (LA) and a Na+ channel blocker from the caine family. It delays anoxic depolarization (AD) in human cortical slices during simulated ischemia and also inhibits serum cholinesterase (SChE). It induces apoptosis in SK-N-MC human neuroblastoma cells and inhibits the growth of HL-60 promyelocytic leukemia cells.
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.
E4893New Flecainide hydrochloride Flecainide hydrochloride, an antiarrhythmic drug, is a blocker of hydrophilic sodium channels with a pKa of 9.3. At pH 7.4. It also inhibits the ryanodine receptor (RyR2), reducing spontaneous calcium release from the sarcoplasmic reticulum.
A2348 Anti-SLC44A4  Anti-SLC44A4 is a fully human IgG2k monoclonal antibody targeting SLC44A4 (AGS-5) with potential antineoplastic activity. MW : 145.5 KD.
S4284 Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
A2349 Anti-SLC40A1 Anti-SLC40A1 is a monoclonal antibody targeting SLC40A1. It has the potential to do research on mineral absorption, insulin receptor recycling, and transmembrane transporter activity. MW : 145.5 KD.
A2350 Lifastuzumab (Anti-SLC34A2) Lifastuzumab (Anti-SLC34A2) is a humanized monoclonal antibody targeting NaPi2b. MW : 145.5 KD.
A2351 Upifitamab (Anti-SLC34A2) Upifitamab (Anti-SLC34A2) is a humanized monoclonal antibody targeting NaPi2b. Upifitamab can be used to synthesize an ADC compound, Upifitamab rilsodotin, used in ovarian cancer research, particularly in platinum-resistant recurrent ovarian cancer. MW : 145.5 KD.
E0144 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.
S4294 Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
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.
Nat Commun, 2024, 15(1):1669
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
S1811 Amiloride HCl Amiloride HCl 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).
J Extracell Vesicles, 2024, 13(4):e12426
J Extracell Vesicles, 2024, 13(4):e12426
Virus Res, 2024, 339:199258
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.
CNS Neurosci Ther, 2024, 30(6):e14822
Elife, 2022, 11e77444
Antiviral Res, 2022, 202:105325
S1614 Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.
Neurotherapeutics, 2023, none
J Endocr Soc, 2023, 7(10):bvad117
Front Bioeng Biotechnol, 2022, 10:855755
S3024 Lamotrigine Lamotrigine (BW-430C,LTG) 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
J Pers Med, 2022, 12(2)258
Hum Cell, 2022, 10.1007/s13577-022-00671-y
S2560 Amiloride HCl dihydrate Amiloride HCl dihydrate(MK-870 hydrochloride dihydrate) is a potent epithelial sodium channel (ENaC) blocker, used in the management of hypertension and congestive heart failure.
Adv Sci (Weinh), 2022, 9(29):e2202039
Mol Ther Methods Clin Dev, 2022, 24:11-19
Theranostics, 2021, 11(5):2364-2380
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
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
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).
Cancers (Basel), 2022, 14(19)4883
Chem Res Toxicol, 2021, 10.1021/acs.chemrestox.1c00127
Cell Syst, 2019, 8(2):97-108
S9849 EIPA EIPA (L593754; MH 12-43) 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.
Gastroenterology, 2024, S0016-5085(24)05182-5
Microbiol Spectr, 2023, 10.1128/spectrum.02553-23
Int J Mol Sci, 2022, 23(8)4419
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
Cancer Discov, 2020, CD-20-0160
Oncol Rep, 2020, 43(5):1659-1668
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.
Anesthesiology, 2023, 139(6):782-800.
Redox Biol, 2022, 55:102427
S2525 Phenytoin Phenytoin (Di-Hydan, Dihycon, Dilabid, Diphedan, Diphenat, Diphenylan, Diphenylhydantoin, Hydantol, Lehydan, NSC 8722) is an inactive voltage-gated sodium channel stabilizer.
Front Cell Neurosci, 2023, 17:1175895
World J Gastroenterol, 2023, 29(20):3103-3118
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
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
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
S3751 Quinidine hemisulfate hydrate Quinidine hemisulfate hydrate(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
S2118 Ibutilide Fumarate Ibutilide Fumarate (U-70226E,Corvert Fumarate) 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
S1445 Zonisamide Zonisamide (Zonegran,CI-912,AD 810) 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
S2524 Phenytoin Sodium Phenytoin Sodium (Aleviatin, Diphenylhydantoin sodium, Eptoin, Phenytoin soluble, Prompt; Phenytek,Dilantin sodium, Diphantoine) is an inactive voltage-gated sodium channel stabilizer.
Proc Natl Acad Sci U S A, 2021, 118(11)e2100066118
S1965 Primidone Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.
Life Sci, 2021, 268:118967
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
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
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
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.
Phytochem Anal, 2022, 33(7):1121-1134
S2110 Vinpocetine Vinpocetine (RGH-4405,Ethyl apovincaminate,AY 27255) 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
S1256 Rufinamide Rufinamide (CGP 33101,E 2080,RUF 331,Banzel) is a voltage-gated sodium channel blocker, used an anticonvulsant medication.
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(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.
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
S3155 Mepivacaine HCl Mepivacaine is a tertiary amine used as a local anesthetic.
E1186New Tenapanor Tenapanor (AZD1722, RDX5791) is a potent and orally active inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3). It exhibits an IC50 of 2 and 6 nM in human and mouse ileum monolayers, respectively. Tenapanor reduces intestinal phosphate absorption predominantly by reducing passive paracellular phosphate flux.
S0036 PF-06869206 PF-06869206 is a selective inhibitor of NPT2a (also referred to as NaPi2a or SLC34A1) with an IC50 of 380 nM.
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.
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 INa with anti-arrhythmic actions.
S0755 SLC13A5-IN-1 SLC13A5-IN-1 is a selective inhibitor of sodium-citrate co-transporter (SLC13A5/NaCT). It completely blocks the uptake of 14 C-citrate and has the potential for the treatment of metabolic and/or cardiovascular diseases.
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.
S0312 Rimeporide Rimeporide(EMD-87580) is a sodium hydrogen exchanger (NHE-1) inhibitor indicated for patients with Duchenne muscular dystrophy.
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.
S0073 BI 01383298 BI 01383298 is an irreversible and non-competitive inhibitor of human sodium-coupled citrate transporter (hNaCT), in which the inhibition is evident for the constitutively expressed transporter in HepG2 cells and for the ectopically expressed human NaCT in HEK293 cells, with IC50 of ~100 nM.
S3074 Chlorthalidone Chlortalidone (Chlortalidone) is a diuretic drug widely used in antihypertensive therapy.
S7848 QX-314 chloride QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
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.
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.
NAR Genom Bioinform, 2024, 6(1):lqae001
E1612New Suzetrigine VX-548 (Suzetrigine), is an oral, highly selective inhibitor of voltage-gated sodium channel 1.8 (NaV1.8) with an IC50 of 0.7 nM. It can be used in research of transmitting nociceptive signals and treatment of acute pain after abdominoplasty or bunionectomy.
S9461 Benzonatate Benzonatate(Benzononatine) has sodium channel-blocking properties and local anesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite.
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.
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.
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.
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.
E1929New LTGO-33 LTGO-33 is a potent and selective inhibitor of voltage-gated sodium channel NaV1.8. LTGO-33, with its potency in the nanomolar range, selectively inhibits NaV1.8 over 600 times more than human NaV1.1-NaV1.7 and NaV1.9. Its inhibition is not dependent on the state of the channels and displays consistent potency against both closed and inactivated conformations. LTGO-33 holds promise for research in pain disorders.
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).
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(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.
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.
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.
E4949New Eslicarbazepine Eslicarbazepine (BIA 2-194), an active metabolite of the prodrug eslicarbazepine acetate is an inhibitor of voltage-gated sodium channel (Nav). It acts by enhancing the slow activation of voltage-gated sodium channels, reducing their availability.
D4010 Lifastuzumab vedotin Lifastuzumab vedotin (LIFA, DNIB0600A, RG-7599) is an antibody-drug conjugate (ADC) composed of a humanized anti-NaPi2b monoclonal antibody and an anti-mitotic cytotoxic agent, monomethyl auristatin E (MMAE) . Lifastuzumab vedotin is used in the treatment of platinum-resistant ovarian cancer.
S5534New Cinchocaine Dibucaine (Cinchocaine) is a potent, long-lasting local anesthetic (LA) and a Na+ channel blocker from the caine family. It delays anoxic depolarization (AD) in human cortical slices during simulated ischemia and also inhibits serum cholinesterase (SChE). It induces apoptosis in SK-N-MC human neuroblastoma cells and inhibits the growth of HL-60 promyelocytic leukemia cells.
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.
E4893New Flecainide hydrochloride Flecainide hydrochloride, an antiarrhythmic drug, is a blocker of hydrophilic sodium channels with a pKa of 9.3. At pH 7.4. It also inhibits the ryanodine receptor (RyR2), reducing spontaneous calcium release from the sarcoplasmic reticulum.
S4284 Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
E0144 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.
S4294 Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
A2348 Anti-SLC44A4  Anti-SLC44A4 is a fully human IgG2k monoclonal antibody targeting SLC44A4 (AGS-5) with potential antineoplastic activity. MW : 145.5 KD.
A2349 Anti-SLC40A1 Anti-SLC40A1 is a monoclonal antibody targeting SLC40A1. It has the potential to do research on mineral absorption, insulin receptor recycling, and transmembrane transporter activity. MW : 145.5 KD.
A2350 Lifastuzumab (Anti-SLC34A2) Lifastuzumab (Anti-SLC34A2) is a humanized monoclonal antibody targeting NaPi2b. MW : 145.5 KD.
A2351 Upifitamab (Anti-SLC34A2) Upifitamab (Anti-SLC34A2) is a humanized monoclonal antibody targeting NaPi2b. Upifitamab can be used to synthesize an ADC compound, Upifitamab rilsodotin, used in ovarian cancer research, particularly in platinum-resistant recurrent ovarian cancer. MW : 145.5 KD.
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.
Virus Res, 2023, 10.1016/j.virusres.2023.199260
S1828 Proparacaine HCl Proparacaine HCl(Proxymetacaine Hydrochloride) is a voltage-gated sodium channels antagonist with ED50 of 3.4 mM.
E1186New Tenapanor Tenapanor (AZD1722, RDX5791) is a potent and orally active inhibitor of sodium/hydrogen exchanger isoform 3 (NHE3). It exhibits an IC50 of 2 and 6 nM in human and mouse ileum monolayers, respectively. Tenapanor reduces intestinal phosphate absorption predominantly by reducing passive paracellular phosphate flux.
E4836New Bupivacaine Bupivacaine is a potent local anesthetic and sodium channel blocker used for local infiltration, nerve block, epidural, and intrathecal anesthesia. It significantly reduces cell viability and induces apoptosis. It also stimulates the production of ROS and activates MAPK pathways, which increases the expression of WDR35 in mouse neuroblastoma Neuro2a cells. It also activates NF-κB and c-Jun/AP-1 signalling pathways in Neuro2a cells.
E1612New Suzetrigine VX-548 (Suzetrigine), is an oral, highly selective inhibitor of voltage-gated sodium channel 1.8 (NaV1.8) with an IC50 of 0.7 nM. It can be used in research of transmitting nociceptive signals and treatment of acute pain after abdominoplasty or bunionectomy.
E1929New LTGO-33 LTGO-33 is a potent and selective inhibitor of voltage-gated sodium channel NaV1.8. LTGO-33, with its potency in the nanomolar range, selectively inhibits NaV1.8 over 600 times more than human NaV1.1-NaV1.7 and NaV1.9. Its inhibition is not dependent on the state of the channels and displays consistent potency against both closed and inactivated conformations. LTGO-33 holds promise for research in pain disorders.
E4949New Eslicarbazepine Eslicarbazepine (BIA 2-194), an active metabolite of the prodrug eslicarbazepine acetate is an inhibitor of voltage-gated sodium channel (Nav). It acts by enhancing the slow activation of voltage-gated sodium channels, reducing their availability.
S5534New Cinchocaine Dibucaine (Cinchocaine) is a potent, long-lasting local anesthetic (LA) and a Na+ channel blocker from the caine family. It delays anoxic depolarization (AD) in human cortical slices during simulated ischemia and also inhibits serum cholinesterase (SChE). It induces apoptosis in SK-N-MC human neuroblastoma cells and inhibits the growth of HL-60 promyelocytic leukemia cells.
E4893New Flecainide hydrochloride Flecainide hydrochloride, an antiarrhythmic drug, is a blocker of hydrophilic sodium channels with a pKa of 9.3. At pH 7.4. It also inhibits the ryanodine receptor (RyR2), reducing spontaneous calcium release from the sarcoplasmic reticulum.

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