Sodium Channel

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Inhibitory Selectivity
Solubility

Catalog No.	Product Name	Solubility(25°C)
Catalog No.	Product Name	Water	DMSO	Alcohol
S1614	Riluzole	<1 mg/mL	46 mg/mL	46 mg/mL
S2454	Bupivacaine HCl	23 mg/mL	65 mg/mL	65 mg/mL
S1811	Amiloride HCl	6 mg/mL	53 mg/mL	5 mg/mL
S1256	Rufinamide	<1 mg/mL	18 mg/mL	<1 mg/mL
S1603	Furosemide	<1 mg/mL	66 mg/mL	<1 mg/mL
S5814	cariporide	<1 mg/mL	87 mg/mL	3 mg/mL
S5710	Ambroxol	-1 mg/mL	76 mg/mL	-1 mg/mL
S5490	Disopyramide	-1 mg/mL	67 mg/mL	-1 mg/mL
S5274	GS967	<1 mg/mL	45 mg/mL	46 mg/mL
S3907	Bulleyaconi cine A	-1 mg/mL	7 mg/mL	-1 mg/mL
S1445	Zonisamide	<1 mg/mL	42 mg/mL	5 mg/mL
S2524	Phenytoin Sodium	3 mg/mL	32 mg/mL	11 mg/mL
S1693	Carbamazepine	<1 mg/mL	47 mg/mL	18 mg/mL
S2785	A-803467	<1 mg/mL	72 mg/mL	11 mg/mL
S2560	Amiloride HCl dihydrate	17 mg/mL	0 mg/mL	0 mg/mL
S2525	Phenytoin	<1 mg/mL	50 mg/mL	13 mg/mL
S2874	Camostat Mesilate	10 mg/mL	99 mg/mL	<1 mg/mL
S2114	Dronedarone HCl	<1 mg/mL	80 mg/mL	40 mg/mL
S3024	Lamotrigine	<1 mg/mL	10 mg/mL	3 mg/mL
S4016	Ouabain	<1 mg/mL	100 mg/mL	100 mg/mL
S1965	Primidone	<1 mg/mL	44 mg/mL	3 mg/mL
S3064	Ambroxol HCl	<1 mg/mL	4 mg/mL	<1 mg/mL
S2041	Dyclonine HCl	6 mg/mL	15 mg/mL	36 mg/mL
S4229	Oxybuprocaine HCl	69 mg/mL	69 mg/mL	69 mg/mL
S3155	Mepivacaine HCl	57 mg/mL	3 mg/mL	8 mg/mL
S2500	Propafenone HCl	<1 mg/mL	69 mg/mL	<1 mg/mL
S4023	Procaine HCl	55 mg/mL	55 mg/mL	<1 mg/mL
S1619	Prilocaine	<1 mg/mL	44 mg/mL	44 mg/mL
S4038	Dibucaine HCl	76 mg/mL	76 mg/mL	76 mg/mL
S1391	Oxcarbazepine	<1 mg/mL	7 mg/mL	<1 mg/mL
S4058	Ropivacaine HCl	46 mg/mL	62 mg/mL	<1 mg/mL
S4180	Nefopam HCl	21 mg/mL	1 mg/mL	<1 mg/mL
S4061	Levobupivacaine HCl	64 mg/mL	64 mg/mL	57 mg/mL
S4080	Triamterene	<1 mg/mL	20 mg/mL	<1 mg/mL
S4200	Tolperisone HCl	56 mg/mL	56 mg/mL	56 mg/mL
S4210	Benzocaine	<1 mg/mL	33 mg/mL	33 mg/mL
S4669	Benzocaine hydrochloride	<1 mg/mL	40 mg/mL	40 mg/mL
S4668	Procaine	<1 mg/mL	47 mg/mL	47 mg/mL
S4225	Mexiletine HCl	43 mg/mL	43 mg/mL	43 mg/mL
S4235	Phenazopyridine HCl	<1 mg/mL	50 mg/mL	<1 mg/mL
S3751	Quinidine sulfate	9 mg/mL	100 mg/mL	100 mg/mL
S4284	Chloroprocaine HCl	61 mg/mL	61 mg/mL	<1 mg/mL
S2110	Vinpocetine	<1 mg/mL	3 mg/mL
S4290	Digoxin	<1 mg/mL	100 mg/mL	<1 mg/mL
S2118	Ibutilide Fumarate	89 mg/mL	89 mg/mL	89 mg/mL
S4294	Procainamide HCl	54 mg/mL	54 mg/mL	54 mg/mL
S3911	Veratramine	-1 mg/mL	63 mg/mL	-1 mg/mL
S1828	Proparacaine HCl	66 mg/mL	12 mg/mL	<1 mg/mL

Sodium Channel Inhibitors (51)
New Sodium Channel Products

Catalog No.	Information	Product Use Citations	Product Validations
S1614	Riluzole Riluzole is a glutamate release inhibitor with neuroprotective, anticonvulsant, anxiolytic and anesthetic qualities.	Int J Mol Sci, 2016, 17(3):357 J Neuroimmune Pharmacol, 2013, 8(5):1098-105	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.
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).	Environ Sci Technol, 2013, 47(18):10601-10 Atherosclerosis, 2015, 239(1):252-9
S1256	Rufinamide Rufinamide 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.
S5814^New	cariporide Cariporide is a selective and potent inhibitor of NHE1 with an IC50 of 30 nM for hNHE1 in CHO-K1 cells.
S5710^New	Ambroxol Ambroxol, a substituted benzylamine, is an active metabolite of bromhexine. It is a potent inhibitor of the neuronal Na+ channels.
S9142^New	Sparteine Sparteine, which could be extracted from scotch broom, is a sodium channel blocker and a class 1a antiarrhythmic agent.
S5556^New	(-)-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.
S5490^New	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.
S5274^New	GS967 GS967 is a potent and selective inhibitor of late I_Na with anti-arrhythmic actions.
S3907^New	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.
S1445	Zonisamide Zonisamide is a voltage-dependent sodium channel and T-type calcium channel blocker, used as an antiepileptic drug.
S2524	Phenytoin Sodium Phenytoin Sodium is an inactive voltage-gated sodium channel stabilizer.
S1693	Carbamazepine Carbamazepine (Carbatrol) is a sodium channel blocker with IC50 of 131 μM in rat brain synaptosomes.
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.	Environ Sci Technol, 2013, 47(18):10601-10 Sci Rep, 2017, 7(1):5586
S2525	Phenytoin Phenytoin is an inactive voltage-gated sodium channel stabilizer.
S2874	Camostat Mesilate Camostat 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.
S2114	Dronedarone HCl Dronedarone HCl is a multichannel blocker targeting potassium channel, sodium channel and calcium channel, used as an antiarrhythmic drug for treatment of atrial fibrillation (AF).	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 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.
S4016	Ouabain Ouabain is a selective Na+/K+, -ATPase inhibitor, binds to α2 /α3 subunit with K_i of 41 nM/15 nM.	Antiviral Res, 2016, 132:38-45 Nat Methods, 2015, 12(12):1129-31	Effect of pharmacological agents capable of increasing intracellular calcium concentration on RSV. HEp-2 cells were infected with RSV strain long at an MOI of 0.1, and treated with a specific Na+/K+-ATPase inhibitor ouabain at indicated concentrations. Supernatants were collected at 48 h postinfection and viral titers were determined by immunoplaque assay. Grey bars represent cytotoxicity of the compounds. The data presented were obtained from two independent experiments. Error bars represent the standard deviations from two independent experiments. Statistical significance between treated and control group were analyzed by t-test (, p < 0.05, *, p < 0.01).
S1965	Primidone Primidone 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.
S4023	Procaine HCl Procaine 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 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.
S4038	Dibucaine HCl Dibucaine HCl is a local anesthetics.
S1391	Oxcarbazepine Oxcarbazepine 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.
S4058	Ropivacaine HCl Ropivacaine HCl is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.
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, the pure S(-)-enantiomer of bupivacaine, is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.
S4080	Triamterene Triamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner with IC50 of 4.5 μM.
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 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 belongs to Class IB anti-arrhythmic group of medicines, inhibits sodium channels to reduce the inward sodium current.
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.
S3751	Quinidine sulfate Quinidine acts as a blocker of voltage-gated sodium channels, also an antimuscarinic and antimalarial.
S4284	Chloroprocaine HCl Chloroprocaine HCl is a local anesthetic during surgical procedures.
S2110	Vinpocetine Vinpocetine is a selective inhibitor of voltage-sensitive sodium channel for the treatment of stroke, vascular dementia and Alzheimer's disease.
S4290	Digoxin Digoxin is a classical Na,K-ATPase inhibitor, with selectivity for the α2β3 isoform over the common α1β1 isoform, used in the treatment of atrial fibrillation and heart failure.
S2118	Ibutilide Fumarate Ibutilide 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.
S4294	Procainamide HCl Procainamide HCl is a sodium channel blocker, and also a DNA methyltransferase inhibitor, used in the treatment of cardiac arrhythmias.
S3911	Veratramine Veratramine, 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.

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