vgsc

VGSC blocker-1 is a powerful small molecule that serves as a blocker for the neonatal isoform of the VGSC subtype known as Nav1.5 (nNav1.5). It effectively blocks INa peak currents by 34.9% at a concentration of 1 μM, and demonstrates a 0.3% inhibition of cell invasion at the same concentration in the MDA-MB-231 human breast cancer cell line, without compromising cell viability.

Evenamide (NW-3509) is a sodium channel blocker. Which shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.

VGSCs-IN-1 is a potent VGSC inhibitor, a 2-piperazine analog of Riluzole that exhibits good blocking activity on Nav1.4.VGSCs-IN-1 can be used to study cellular excitability disorders.

Phenytoin sodium (Diphantoine) is an inactive stabilizer for voltage-gated sodium channel .

Phenytoin (5,5-Diphenylhydantoin) is a hydantoin derivative and a non-sedative antiepileptic agent with anticonvulsant activity. It potentially acts by promoting sodium efflux from neurons in the motor cortex, reducing post-tetanic potentiation at synapses. This prevents cortical seizure foci from spreading to adjacent areas and stabilizes the threshold against hyperexcitability. Additionally, it appears to reduce muscle spindle sensitivity to stretch, causing muscle relaxation.

Insecticidal agent 21 (Compound 6) is an insecticide targeting Culex pipiens larvae with an LC50 of 0.4 μg/mL. It achieves multi-target neurotoxicity by inhibiting acetylcholinesterase (AChE) and simultaneously targeting other neural receptors, including nicotinic acetylcholine receptors (nAChR), voltage-gated sodium channels (VGSC), and γ-aminobutyric acid receptors (GABAAR). Insecticidal agent 21 shows potent insecticidal activity and can be utilized in the development of new insecticides to combat mosquito resistance to conventional agents.

Neoline is an active ingredient of A. venetum root (PA) that ameliorates oxaliplatin-induced peripheral neuropathy in mice.Neoline inhibits Nav1.7 voltage-gated sodium channel currents (VGSC). It can be used as a labeling compound to determine the quality of PA products used in the study of neuropathic pain.

μ-Conotoxin KIIIA, an analgesic compound derived from Conus kinoshitai, selectively inhibits mammalian neuronal voltage-gated sodium channels (VGSCs) (Nav1.2), offering potential utility in pain research [1] [2].

Jingzhaotoxin-II, a neurotoxin composed of 32 amino acid residues featuring two acidic and two basic residues, selectively inhibits voltage-gated sodium channels (VGSC), notably slowing the rapid inactivation of TTX-resistant (TTX-R) VGSC in cardiac myocytes, with an IC50 of 0.26 μM [1].

μ-Conotoxin BuIIIB (Mu-Conotoxin BuIIIB), derived from cone snail venom, is a selective blocker of mammalian neuronal voltage-gated sodium channels (VGSC) and is used as a research probe for ion channel function and the investigation of neurological disorders like pain [1].

μ-Conotoxin BuIIIA (Mu-Conotoxin BuIIIA), derived from cone snail venom, functions as a voltage-gated sodium channel (VGSC) blocker and is utilized in researching neurological diseases [1].

Transfluthrin is a volatile pyrethroid insecticide that targets insect voltage-gated sodium channels (VGSC).

(-)-Sparteine ((-)-Lupinidine) is a quinolizidine alkaloid extracted from lupine, which is a voltage-gated sodium channel (VGSC) blocker with anticonvulsant activity.