Sodium Channel Inhibitor

Jingzhaotoxin-V, a 29-residue polypeptide, is derived from the venom of the spider Chilobrachys jingzhao. Jingzhaotoxin-V inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC₅₀ values of 27.6 nM and 30.2 nM, respectively. Jingzhaotoxin-V also inhibits Kv4.2 potassium currents expressed in Xenpus Laevis oocytes (IC₅₀ of 604.2 nM).

BW-4030W92 is a sodium channel blocker. BW-4030W92 induces ataxia.

NaPi2b-IN-3 (compound 5) is a potent sodium-dependent transport protein 2b (SLC34A2, NaPi2b) inhibitor with IC₅₀s of 71 nM and 28 nM for human NaPi2b and rat NaPi2b, respectively. NaPi2b-IN-3 can be used for researching hyperphosphatemia.

DL-017 is a Quinazoline derivative. DL-017 shows inhibitory constants of approximately 0.90 nM for α1-adrenergic receptors and 404 nM for Na⁺ channels. DL-017 exerts antihypertensive effect.

Cyfluthrin-d₆ (β-Cyfluthi-d₆) is deuterium labeled Cyfluthrin. Cyfluthrin is a type II pyrethroid and has effects on various insects. Cyfluthrin is a modulator of Nav_1.8 sodium channels by repetitive stimulation. Cyfluthrin can be applied in agriculture,veterinary, insecticide,pyrethroid and stored product.

Pterinotoxin-1 is a sodium channel inhibitor peptide toxin.

Lidocaine-d₆ (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor.

BmK-M1 is a scorpion toxin, and is composed of 64 amino acids cross-linked by four disulfide bridges. BmK-M1 inhibits Na⁺ channel and can be considered both as a cardiotoxin and a neurotoxin.

Mepivacaine (hydrochloride) (Standard) is the analytical standard of Mepivacaine (hydrochloride). This product is intended for research and analytical applications. Mepivacaine hydrochloride binds to specific voltage-gated sodium ion channels in neuronal cell membranes, which inhibits both sodium influx and membrane depolarization.

Olisutrigine bromide is a sodium channel blocker, which can be used as analgesics.

BI-8668 (compound 40), a chemical probe, is an inhibitor of ENaC. BI-8668 can be used in the study of cystic fibrosis.

Zocainone is an antiarrhythmic agent. Zocainone blocks sodium channels in cardiac tissue, stabilizing the cardiac action potential and reducing abnormal electrical activity. Zocainone is promising for research of cardiac arrhythmias.

Fluphenazine hydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine hydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine hydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine hydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine hydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2.

Quinacainol (PK 10139) is an inhibitor for sodium current with an EC₅₀ of 95 µM. Quinacainol exhibits antiarrhythmic activity by affecting the electrophysiological properties of the heart.

Rufinamide-¹⁵N,d₂ (CGP 33101-¹⁵N,d₂) is the deuterium and ¹⁵N labeled Rufinamide (HY-A0042).Rufinamide (CGP 33101) is an orally active antiepileptic compound that inhibits Na⁺ current activation, inhibits neuronal hyperexcitability, and has anticonvulsant effects. Rufinamide is used in the study of Lennox-Gastaut syndrome.

Nav1.7-IN-22 (P58 13-2) is a selective inhibitor of voltage-gated sodium channel Nav1.7. Nav1.7-IN-22 inhibits abnormal electrical signal generation and conduction in sensory neurons by blocking Nav1.7 channel activity. Nav1.7-IN-22 can be used for the study of pain.

NVP-QBE170 is a selective Epithelial sodium channel (ENaC) inhibitor with an IC₅₀ of 57.5 nM. NVP-QBE170 potently inhibits ENaC function in HBECs and shows a longer duration of action. NVP-QBE170 significantly attenuates ENaC activity in the airways of guinea pig models. NVP-QBE170 can be used for hyperkalaemia research.

DS43260857 is a potentNaV1.7inhibitor, which has a high inhibitory effect on both human and mouse NaV1.7. The IC₅₀ values of DS43260857 for hNaV1.1, hNaV1.5, hNaV1.7, mNaV1.7 are 6.6, 14, 0.015 and 0.061 μM, respectively.

Irampanel hydrochloride (BIIR 561-CL) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel hydrochloride inhibits Kainic acid (HY-N2309)-induced currents in rat cortical neurons.

Denzimol is an orally active anticonvulsant agent. Denzimol inhibits cytochrome P450, and interacts with benzodiazepine receptors. Denzimol selectively antagonizes tonic components of Metrazol-induced seizures in rats and mice. Denzimol can be used for the research of epilepsy and convulsions.