Sodium Channel Inhibitors

Cat.No.	Product Name	Information	Product Use Citations
S3751	Quinidine hemisulfate hydrate	Quinidine hemisulfate hydrate (Quinidine, Pitayine, β-quinine, (+)-quinidine) acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.	J Immunother Cancer, 2024, 12(11)e009805 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 Channel, which prolongs action potential and refractory period of myocardial cells.	J Immunother Cancer, 2024, 12(11)e009805 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 Cancers (Basel), 2021, 13(21)5437
S2785	A-803467	A-803467 is a selective Na_V1.8 channel blocker with an IC50 of 8 nM, blocks tetrodotoxin-resistant currents, exhibiting >100-fold selectivity against human Na_V1.2, Na_V1.3, Na_V1.5, and Na_V1.7.	Anesthesiology, 2023, 139(6):782-800. Redox Biol, 2022, 55:102427
S1965	Primidone	Primidone (NCI-C56360) is an anticonvulsant of the pyrimidinedione class.	Inflammation, 2024, Life Sci, 2021, 268:118967
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 an IC50 of 4.5 μM.	Nat Commun, 2021, 12(1):6479 Cell Chem Biol, 2020, 24 pii: S2451-9456(20)30080-5
S4225	Mexiletine HCl	Mexiletine HCl (KO1173, Mexitil) belongs to Class IB anti-arrhythmic group of medicines, inhibits Sodium Channel to reduce the inward sodium current.	J Immunother Cancer, 2024, 12(11)e009805 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.	J Immunother Cancer, 2024, 12(11)e009805 bioRxiv, 2020, 2020/9/20.4.7.30734
S1256	Rufinamide	Rufinamide (CGP 33101, E 2080, RUF 331, Banzel) is a voltage-gated sodium channel blocker, used as an anticonvulsant medication.	Cancers (Basel), 2021, 13(21)5437
S2524	Phenytoin Sodium	Phenytoin Sodium (Aleviatin, Diphenylhydantoin sodium, Eptoin, Phenytoin soluble, Prompt; Phenytek, Dilantin sodium, Diphantoine) is an inactive voltage-gated Sodium Channel stabiliser.	Proc Natl Acad Sci U S A, 2021, 118(11)e2100066118
S4229	Oxybuprocaine HCl	Oxybuprocaine HCl (oxybuprocaine hydrochloride) is a local anaesthetic, which is used especially in ophthalmology and otolaryngology. Oxybuprocaine binds to Sodium Channel and reversibly stabilises the neuronal membrane which decreases its permeability to sodium ions.	Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433
S2500	Propafenone HCl	Propafenone HCl is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias.Propafenone HCl can be used to induce animal models of Heart Failure.	J Immunother Cancer, 2024, 12(11)e009805
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
S1619	Prilocaine	Prilocaine (NSC 40027) is a local anaesthetic of the amino amide type. It acts on Sodium Channel on the neuronal cell membrane, limiting the spread of seizure activity and reducing seizure propagation.	Nat Prod Res, 2021, 1-7
S1391	Oxcarbazepine	Oxcarbazepine (GP47680) inhibits the binding of [3H]BTX to Sodium Channel with an IC50 of 160 μM and also inhibits the influx of ²²Na⁺ into rat brain synaptosomes with an IC50 of about 100 μM.	NAR Genom Bioinform, 2024, 6(1):lqae001
S3911	Veratramine	Veratramine (NSC 17821, NSC 23880), a major alkaloid from Veratrum nigrum L., has distinct anti-tumour and anti-hypertension effects. It is a good membrane permeant, undergoes rapid passive diffusion, and has good stability in the gastrointestinal tract during its absorption.	Virus Res, 2023, 10.1016/j.virusres.2023.199260
S4200	Tolperisone HCl	Tolperisone HCl is an ion channel blocker and centrally-acting muscle relaxant.	Nat Commun, 2025, 16(1):212
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
S4294	Procainamide HCl	Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.	J Immunother Cancer, 2024, 12(11)e009805
S3064	Ambroxol HCl	Ambroxol HCl 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.
S3155	Mepivacaine HCl	Mepivacaine is a tertiary amine used as a local anesthetic.
E1186	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. This compound 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.
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 sparteine, 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.
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.
E6460^New	Phenamil methanesulfonate	Phenamil methanesulfonate, is a potent and less reversible inhibitor of epithelial sodium channel (ENaC) with an IC50 of 400 nM. Phenamil methanesulfonate is also a competitive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca2+ transport with an IC50 of 140 nM in a Ca2+ uptake assay. Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease.
S4038	Dibucaine HCl	Dibucaine HCl (Cinchocaine) is a local anaesthetic.
E4836	Bupivacaine	Bupivacaine is a potent local anaesthetic and sodium channel blocker used for local infiltration, nerve block, epidural, and intrathecal anaesthesia. 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 Channel depressing phase 0 of the action potential. This compound 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. This compound exhibits effects on motor and sensory nerves by inhibiting the opening of voltage-gated Sodium Channel.
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	Chlorthalidone (Chlorthalidone) is a diuretic drug widely used in antihypertensive therapy.
S5789	Propafenone	Propafenone (SA-79) is an orally active sodium channel blocking agent and a beta-adrenoceptor (β-adrenergic receptor) antagonist. This compound offers a broad spectrum of activity in the treatment of cardiac arrhythmias.It can be used to induce animal models of Heart Failure.
E1612	Suzetrigine (VX-548)	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 anaesthetic effects on the respiratory stretch receptors due to a tetracaine-like metabolite.
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 anaesthetic.
E1929	LTGO-33	LTGO-33 is a potent and selective inhibitor of voltage-gated sodium channel NaV1.8. This compound, 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. This chemical 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.
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 anaesthetic 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 anaesthetic that acts by preventing transmission of impulses along nerve fibres and at nerve endings.
S4339	Meticrane	Meticrane is a diuretic that inhibits the reabsorption of sodium and chloride ions in the distal convoluted tubule. This compound is used to treat essential hypertension.
E4949	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.
E7765	5-(N,N-Hexamethylene)-amiloride	5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride; HMA) is a potent inhibitor of the Na⁺/H⁺ exchanger, lowering intracellular pH and inducing apoptosis. It also inhibits the HIV-1 Vpu virus ion channel and suppresses replication of mouse hepatitis virus (MHV) and human coronavirus 229E (HCoV-229E) in cultured L929 cells, with EC₅₀ values of 3.91 μM and 1.34 μM, respectively.
S9446	7,8-dihydrokawain	7,8-dihydrokawain (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.
S5534	Cinchocaine	Dibucaine (Cinchocaine) is a potent, long-lasting local anaesthetic (LA) and a Na+ channel blocker from the 'caine' family. It delays anoxic depolarisation (AD) in human cortical slices during simulated ischaemia and also inhibits serum cholinesterase (SChE). It induces apoptosis in SK-N-MC human neuroblastoma cells and inhibits the growth of HL-60 promyelocytic leukaemia cells.
E4893	Flecainide hydrochloride	Flecainide hydrochloride, an antiarrhythmic drug, is a blocker of hydrophilic Sodium Channel 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 anaesthetic during surgical procedures.
S5749	Chlorpromazine (CPZ)	Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. This compound inhibits 5-HT(2A) receptor and dopamine D2 in vitro. It also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.	EMBO J, 2025, 10.1038/s44318-025-00537-7 Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6 J Thromb Haemost, 2025, 23(9):2926-2943
S9849	EIPA (L593754)	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.	J Adv Res, 2025, S2090-1232(25)00267-X J Nanobiotechnology, 2025, 23(1):173 iScience, 2025, 28(2):111830
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
S7848	QX-314 chloride	QX-314 chloride directly activates and permeates the human isoforms of TRPV1 and TRPA1 to induce inhibition of sodium channels.
S4657	Eslicarbazepine Acetate	Eslicarbazepine Acetate (BIA 2093, Zebinix, Exalief, Stedesa, Aptiom), an antiepileptic drug, is a dual inhibitor of β-Secretase and voltage-gated Sodium Channel.
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. This compound 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.
S0016	SN-6	SN-6 is a selective Na+/Ca2+ exchanger (NCX) inhibitor. This compound inhibits NCX1, NCX2, and NCX3 with IC50 of 2.9 μM, 16 μM and 8.6 μM, respectively. It abolishes acetylcholine (ACh)-induced vasodilation.
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.