Bifenthrin is a synthetic pyrethroid insecticide that prolongs opening of sodium channels resulting in membrane depolarization and conductance block in the insect nervous system. Bifenthrin is effective against A. gambiae and C. quinquefasciatus mosquitos (LD50s = 0.15 and 0.16 ng/mg, respectively) and increases O. insidiosus mortality in treated corn and sorghum plants.
Eleclazine hydrochloride is a novel late Na+ current inhibitor with IC50 value of 0.7 uM. target: Na+ current.IC50: 0.7 uM.In vitro: Eleclazine hydrochloride inhibits ATX-II enhanced late INa in ventricular myocytes, shorten the ATX-II induced prolongation of APD, MAPD, QT interval, and decreased spatiotemporal dispersion of repolarization and ventricular arrhythmias. Inhibition by GS-6615 of ATX-II enhanced late INa is strongly correlated with shortening of myocyte APD and isolated heart MAPD[1]. Selective inhibition of cardiac late INa with eleclazine hydrochloride confers dual protection against vulnerability to ischemia-induced AF and reduces atrial and ventricular repolarization abnormalities before and during adrenergic stimulation without negative inotropic effects. [2]
KC 12291 hydrochloride is an orally active blocker of voltage-gated sodium channel (VGSC). KC 12291 hydrochloride reduces the amplitude of sustained Na+ current to exert antiischemic activity. KC 12291 hydrochloride has significant cardioprotective effect in vitro and in vivo[1].
BI-9627 is a sodium−hydrogen exchanger isoform 1 (NHE1) inhibitor with an EC50 of 31 nM[1].
Atomoxetine (Tomoxetine) is a selective noradrenaline reuptake inhibitor with Ki values of 5, 77 and 1451 nM for norepinephrine (NE), serotonin (5-HT) and dopamine (DA) transporters, respectively. Atomoxetine (Tomoxetine) increases of DAEX and NEEX in the PFC and enhances catecholaminergic neurotransmission. Atomoxetine (Tomoxetine) is a potent Na+ channels (VGSCs) blocker. Atomoxetine (Tomoxetine) can be used for attention-deficit hyperactivity disorder (ADHD) research[1][2][3].
Eslicarbazepine acetate, an antiepileptic drug, is a dual a dual Inhibitor of β-Secretase and voltage-gated sodium channel.
μ-Conotoxin-CnIIIC is a 22-residue conopeptide that can be isolated from Conus consors. μ-Conotoxin-CnIIIC is a potent and persistent blocker of NaV1.4 channel. μ-Conotoxin-CnIIIC has analgesic, anaesthetic and myorelaxant properties[1][2].
Ranolazine-d8 (CVT 303-d8) is the deuterium labeled Ranolazine. Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (INa and IKr with IC50 values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)[1][2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor[3]. Antianginal agent.
S-Bioallethrin is a pyrethroid insecticide. S-Bioallethrin disrupts nerve function by modifying the gating kinetics of transitions between the conducting and nonconducting states of voltage-gated sodium channels[1].
EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel inhibitor with an IC50 of 10.5 μM[1]. EIPA also inhibits Na+/H+-exchanger (NHE)[2] and macropinocytosis[3].
Taplucainium chloride is a Sodium Channel blocker. Taplucainium chloride exhibits 70-95% inhibition at 10μM. Taplucainium chloride can be used as an analgesic agent[1][2].
(-)-Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker. It is an alkaloid, can chelate the bivalents calcium and magnesium.
μ-Conotoxin BuIIIC (Mu-Conotoxin BuIIIC) is a potent Nav1.4 inhibitor[1].
Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2[1][2][3][4][5][6].
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na+ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain)[1]. Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na+ channels, inhibits the inactivation of Na+ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation[2].
Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Na+/H+ exchange inhibitor.
ω-Conotoxin CVIB is a non-selective N- and P/Q-type voltage-gated calcium channels (VGCCs) antagonist. ω-Conotoxin CVIB inhibits depolarization-activated whole-cell VGCC currents in dorsal root ganglion (DRG) neurons with a pIC50 of 7.64[1].
PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker with an IC50 of 196 nM for recombinant human Nav1.8 channel.
Carbamazepine-D10 (CBZ-D10) is the deuterium labeled Carbamazepine. Carbamazepine (CBZ), a sodium channel blocker, is an anticonvulsant agent[1][2].
Propafenone Hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.Target: Sodium ChannelPropafenone Hydrochloride is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial and ventricular arrhythmias. According to the Allergic Rhinitis and its Impact on Asthma (ARIA) treatment guidelines, intranasal anti-histamines are recommended for the first line therapy of mild intermittent, moderate/severe intermittent and mild persistent rhinitis (new classification system for rhinitis). Propafenone works by slowing the influx of sodium ions into the cardiac muscle cells, causing a decrease in excitability of the cells. Propafenone is more selective for cells with a high rate, but also blocks normal cells more than class Ia or Ib. Propafenone differs from the prototypical class Ic antiarrhythmic in that it has additional activity as a beta-adrenergic blocker which can cause bradycardia and bronchospasm .
PF 04531083 is a selective NaV1.8 blocker, and used for the research of neuropathic/inflammatory pain.
Funapide (TV 45070; XEN402) is a potent Sodium Channel Nav1.7 inhibitor.
VX-150 is an orally active, highly selective NaV1.8 inhibitor. VX-150 has the potential for various pain indications research[1].
μ-Conotoxin BuIIIB (Mu-Conotoxin BuIIIB) is a mammalian neuronal voltage-gated sodium channel (VGSC) blocker. μ-Conotoxin BuIIIB can be obtained from the venom of Cone snails and is a probe for ion channel function research. μ-Conotoxin BuIIIB can be used in the study of neurological diseases such as pain[1].