Sodium Channel Modulator

ATX-II TFA is a selective sodium channel modulator toxin. ATX-II TFA enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II TFA has pro-arrhythmic effect. ATX-II TFA slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II TFA can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.

KB130015 (KB015) is an orally active and potent ThRα and ThRβ (thyroid hormone receptor) inhibitor, with IC₅₀ values of 4.5 and 5.1 μM, respectively. KB130015 markedly slows the kinetics of inactivation of Na⁺ channels. KB130015 activates hERG1 channels (EC₅₀ = 12.2 μM) and large-conductance Ca²⁺-activated K⁺ (BKCa) channels formed by hSlo1 (α) subunits in HEK 293 cells. KB130015 has antiarrhythmic properties. KB130015 can be used for the study of cardiovascular disease.

ATX-II is a selective sodium channel modulator toxin. ATX-II enhances late sodium current, prevents full sodium channel inactivation, and generates persistent current fractions. ATX-II has pro-arrhythmic effect. ATX-II slows intrinsic heart rate, prolongs QT interval and sinus node recovery time, and causes sinus pauses and arrests. ATX-II can be used for the research of atrial fibrillation, long QT syndrome, and long QT3 syndrome.

Poneratoxin acetate is the acetate salt form of Poneratoxin (HY-P10234). Poneratoxin acetate is the modulator for voltage-gated sodium channel (NaV, EC₅₀ for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals.

Benzocaine hydrochloride is an orally active local anesthetic. Benzocaine hydrochloride non-competitively inhibits the binding of Ca-ATPase to Ca²⁺, with an IC₅₀ of 47.1 mM. Benzocaine hydrochloride exerts anesthetic effects by blocking voltage-gated sodium channels. Benzocaine hydrochloride induces methemoglobinemia in various experimental animals.

S-Bioallethrin (D-Trans-Allethrin) 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. S-Bioallethrin also causes inhibition of lymphocyte proliferation and induces histamine release from human basophils.

Brevetoxin B (Brevetoxin-2) is a red tide toxin. Brevetoxin B affects sodium, potassium and calcium currents in nerve terminals. Brevetoxin B also modulates the metabolic activity of Jurkat cells, reduces cell viability and induces apoptosis. Brevetoxin B can be used in research on synaptic transmission and tumors.

Crotamine TFA is a Na⁺ channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom.

OD1 is a scorpion α-toxin that can be isolated from the venom of the Iranian yellow scorpion (Odonthobuthus doriae. OD1 is a modulator of mammalian Nav1.7 (EC₅₀: 4.5 nM).

Anthopleurin-A TFA is a soidum channel toxin. Anthopleurin-A TFA is selective for cardiac channels and has cardiotonic effect. Anthopleurin-A TFA can be isolated from the sea anemone.

Heteropodatoxin-1 (HpTx1), a spider peptide toxin, is a Kv4.2 current inhibitor. Heteropodatoxin-1 also inhibits Nav1.7 and activates Nav1.9 but does not affect Nav1.8.

DPI 201-106 (SDZ 201106) is a cardiotonic agent with a synergistic sarcolemmal and intracellular mechanism of action. DPI 201-106 shows cardioselective modulation of voltage-gated sodium channels (VGSCs) resulting in a positive inotropic effect.

PF-05661014, a desmethyl analogue of PF-06526290, selectively inhibits Nav1.3 and Nav1.7 currents by stabilizing inactivated channels via interaction with D4 VSD. PF-05661014 can be used for research of sodium channel modulation.

Cariporide is a Na+/H+ Exchanger 1 (NHE-1) inhibitor. Cariporide inhibits the expression of monocyte endothelial cell adhesion and intercellular adhesion molecule-1 (ICAM-1) mediated by high glucose (HG) by inhibiting the activation of NHE-1.

Crotamine is a Na⁺ channel modulator. Crotamine is a 42 amino acid toxin cross-linked by three disulfide bridges. Crotamine has analgesic activity. Crotamine also interacts with lipid membranes and shows myonecrotic activity. Crotamine can be isolated from Crotalus durissus terrificus venom.

Poneratoxin is the modulator for voltage-gated sodium channel (NaV, EC₅₀ for NaV1.6 and NaV1.7 is 97 nM and 2.3 µM), that lowers the voltage threshold for activation and inhibits the inactivation of channels, enhances the excitability of neurons, and leads to the transmission of pain signals.

Clathrodin is a marine alkaloid that can be isolated from sponges of the genus, Agelas. Clathrodin is a modulator of voltage-gated sodium (NaV) channels. Clathrodin is a sodium channel neurotoxin influencing sodium channel ionic conductance.

Anthopleurin-A is a soidum channel toxin. Anthopleurin-A is selective for cardiac channels and has cardiotonic effect. Anthopleurin-A can be isolated from the sea anemone.

Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABA_A receptors and NaV_1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED₅₀ of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC₅₀ of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable.

Kurtoxin is a selective Cav3 (T-type) voltage-gated Ca²⁺ channel gating inhibitor with a K_d of 15 nM for Cav3.1 (α1G T-type) Ca²⁺ channel. Kurtoxin can interact with high affinity with native neuronal high-threshold L-type, N-type, and P-type Ca²⁺ channels in central and peripheral neurons. Kurtoxin also shows cross-reactivity with voltage-gated Na⁺ channel.