Sodium Channel Inhibitor

DAPI (4',6-Diamidino-2-phenylindole) dihydrochloride is a DAPI dye. DAPI is a fluorescent dye that binds strongly to DNA. It binds to the AT base pair of the double-stranded DNA minor groove, and one DAPI molecule can occupy three base pair positions. The fluorescence intensity of DAPI molecules bound to double-stranded DNA is increased by about 20 times, and it is commonly observed with fluorescence microscopy, and the amount of DNA can be determined based on the intensity of fluorescence. In addition, because DAPI can pass through intact cell membranes, it can be used to stain both live and fixed cells. DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment (Ex/Em = 356/451 nm).

Amiloride (MK-870) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

Suzetrigine (VX-548) is an orally active and highly selective Na_V1.8 inhibitor that acts as an analgesic. Suzetrigine is also a blocker of sodium channel protein type 10 subunit alpha. Suzetrigine is promising for research of acute pain after abdominoplasty and bunionectomy.

Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker with an IC₅₀ of 131 μM. Carbamazepine blocks voltage gated Na⁺, Ca²⁺, and K⁺ channels, and is also a HDAC inhibitor (IC₅₀: 2 μM). Carbamazepine is an anticonvulsant and can be used for research of epilepsy and neuropathic pain.

DAPI (4',6-Diamidino-2-phenylindole) dihydrochloride (solution) is a DAPI dye. DAPI is a fluorescent dye that binds strongly to DNA. It binds to the AT base pair of the double-stranded DNA minor groove, and one DAPI molecule can occupy three base pair positions. The fluorescence intensity of DAPI molecules bound to double-stranded DNA is increased by about 20 times, and it is commonly observed with fluorescence microscopy, and the amount of DNA can be determined based on the intensity of fluorescence. In addition, because DAPI can pass through intact cell membranes, it can be used to stain both live and fixed cells. DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment (Ex/Em = 356/451 nm).
Solvent and concentration: ddH2O: 5 mg/mL

Bupivacaine liposome is a liposome-encapsulated form of Bupivacaine (HY-B0405). Bupivacaine is an NMDA receptor inhibitor. During the action potential, Bupivacaine blocks sodium channels, thereby inhibiting the generation and conduction of nerve impulses induced by painful stimuli. Bupivacaine liposome reduces the release rate of Bupivacaine, thus achieving a long-lasting pain relief effect.

MK-5661 is an orally potent Na_V1.8 voltage-gated sodium channel inhibitor with an EC₅₀ of 4.3 nM. MK-5661 selectively inhibits peripheral nociceptive signaling mediators. MK-5661 reduces capsaicin-induced spontaneous nociceptive behaviors in humanized rats and attenuates capsaicin-induced skin flushing responses in rhesus monkeys. MK-5661 is applicable for pain-related research.

Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC₅₀ of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow.

20(S)-Ginsenoside Rg3 is the main component of Panax ginseng C. A. Meyer. Ginsenoside Rg3 inhibits Na⁺ and hKv1.4 channel with IC₅₀s of 32.2±4.5 and 32.6±2.2 μM, respectively. 20(S)-Ginsenoside Rg3 also inhibits Aβ levels, NF-κB activity, and COX-2 expression.

Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence. Lidocaine 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 is an amide derivative and has potential for the research of ventricular arrhythmia.

Riluzole is an anticonvulsant agent and belongs to the family of use-dependent Na⁺ channel blocker which can also inhibit GABA uptake with an IC₅₀ of 43 μM.

Amiloride hydrochloride (MK-870 hydrochloride) is an inhibitor of both epithelial sodium channel (ENaC) and urokinase-type plasminogen activator receptor (uTPA). Amiloride hydrochloride is a blocker of polycystin-2 (PC2; TRPP2) channel.

QX-314 chloride is a membrane-impermeable permanently charged sodium channel blocker.

Lamotrigine (BW430C) is a potent and orally active anticonvulsant or antiepileptic agent. Lamotrigine selectively blocks voltage-gated Na⁺ channels, stabilizing presynaptic neuronal membranes and inhibiting glutamate release. Lamotrigine can be used for the research of epilepsy, focal seizure, et al.

Phenytoin (5,5-Diphenylhydantoin) is a potent Voltage-gated Na⁺ channels (VGSCs) blocker. Phenytoin has antiepileptic activity and reduces breast tumour growth and metastasis in mice.

A-803467 is a potent and selective tetrodotoxin-resistant Na_v1.8 sodium channel blocker (IC₅₀=8 nM). A-803467 has shown significant anti-nociception in neuropathic and inflammatory pain models. A-803467 enhances the chemosensitivity of conventional anticancer agents through interaction with the ATP-binding cassette subfamily G member 2 (ABCG2) transporter.

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.

PF 05089771 is a potent, orally active and selective arylsulfonamide Na_v1.7 inhibitor, with IC₅₀ values of 11 nM, 12 nM, 13 nM, 171 nM and 8 nM for hNa_v1.7, cynNa_v1.7, dogNa_v1.7, ratNa_v1.7, and musNa_v1.7, respectively. PF 05089771 is under the study for pain and diabetic neuropathy.

Bupivacaine is a NMDA receptor inhibitor. Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine can be used for the research of chronic pain.

Topiramate (McN 4853) is a broad-spectrum antiepileptic agent. Topiramate is a GluR5 receptor antagonist. Topiramate produces its antiepileptic effects through enhancement of GABAergic activity, inhibition of kainate/AMPA receptors, inhibition of voltage-sensitive sodium and calcium channels, increases in potassium conductance, and inhibition of carbonic anhydrase.