Sodium Channels

Cat. No.

A13937

CAS No.

85079-48-7

Brevetoxin-3

Synonyms: PbTx-3

Brevetoxin-3 (PbTx-3) is a potent allosteric activator of voltage-gated Na+ channels. It demonstrates high affinity for site 5 on these channels, effectively inhibiting their inactivation and prolonging the mean open time. This compound is valuable for research into airway hyperresponsiveness and lung inflammation, as repeated exposure has been shown to induce these conditions. Brevetoxin-3 serves as a critical tool for studying sodium channel modulation and its implications in respiratory pathophysiology.

Cat. No.

A15646

CAS No.

3175-95-9

3-Deoxyaconitine

3-Deoxyaconitine is a diterpenoid alkaloid identified as a sodium channel activator. It exhibits significant biological activity by modulating ion channel dynamics, making it a valuable tool for research into neuronal signaling and pain pathways. This compound can be utilized in studies focusing on the physiological and pharmacological roles of sodium channels.

Cat. No.

A68054

CAS No.

931928-13-1

E0199

E0199 is a potent dual-target KV7 activator and NaV inhibitor, specifically enhancing KV7.2/7.3 (EC50 = 12.78 nM), KV7.2 (EC50 = 0.50 μM), and KV7.5 (EC50 = 27.14 nM) channels while inhibiting NaV1.7 (IC50 = 0.52 μM), NaV1.8 (IC50 = 0.24 μM), and NaV1.9 (IC50 = 0.16 μM) channels. This compound demonstrates significant analgesic properties in a chronic constriction injury mouse model, effectively managing neuropathic pain without adversely impacting cardiac and skeletal muscle ion channels. E0199 serves as a valuable tool for research in neuropathic pain mechanisms and therapeutic strategies.

Cat. No.

A68432

CAS No.

1027997-01-8

S3969

S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). With an apparent EC50 of 1.2 μM, S3969 enhances sodium transport across epithelial tissues. This compound serves as a valuable tool for investigating cellular mechanisms related to sodium homeostasis and may be applied in studies of conditions such as hypertension and edema.

Cat. No.

A68434

CAS No.

2332897-85-3

Nav1.1 activator 1

Nav1.1 activator 1 is a potent activator of the Nav1.1 sodium channel, effectively enhancing the decay time constant (tau) of Nav1.1 currents at a concentration of 0.03 μM. This compound demonstrates significant selectivity for Nav1.1 over other sodium channels, including Nav1.2, Nav1.5, and Nav1.6, facilitating targeted research. Its ability to penetrate the blood-brain barrier makes it a valuable tool for studying neurological function and related therapeutic applications.

Cat. No.

A68439

CAS No.

82657-04-3

Bifenthrin

Bifenthrin is a synthetic pyrethroid insecticide that acts as a sodium channel activator, specifically targeting Nav1.8 sodium channels. By prolonging the opening time of these channels, Bifenthrin induces membrane depolarization and disrupts neural function in insects. It exhibits potent insecticidal activity with reported lethal doses (LD50) of 0.15 ng/mg against Aedes gambiae and 0.16 ng/mg against Culex quinquefasciatus, making it an effective agent for control of both susceptible and resistant mosquito populations. Its efficacy in inhibiting blood-sucking behavior presents potential applications in developing mosquito-repellent materials.

Cat. No.

A68446

CAS No.

849000-18-6

Lu AE98134

Lu AE98134 is a selective activator of voltage-gated sodium channel Nav1.1, functioning as a positive modulator. It also enhances the activity of Nav1.2 and Nav1.5 channels, while exhibiting no effect on Nav1.4, Nav1.6, or Nav1.7 channels. This compound serves as a valuable tool for investigating the pathophysiological roles of Nav1.1 in various central nervous system disorders, including potential applications in cognitive improvement in schizophrenia.

Cat. No.

A68509

CAS No.

1001417-92-0

Glucokinase activator 3

Glucokinase activator 3 is a potent activator of glucokinase (GK) with an AC50 of 38 nM. This compound has demonstrated significant efficacy in reducing blood glucose levels in diet-induced obese (DIO) mice, highlighting its potential in type 2 diabetes research. Additionally, glucokinase activator 3 has been shown to inhibit the hERG channel and sodium channels in patch clamp assays, providing insight into its pharmacological profile.

Cat. No.

A68598

CAS No.

120838-62-2

BDF 9148

BDF 9148 is a sodium-channel activator that exhibits antiarrhythmic properties and induces a notable cAMP-independent positive inotropic effect in the left ventricular myocardium of failing hearts. This compound is valuable for research into myocardial failure and its underlying mechanisms, providing insights into potential therapeutic strategies for cardiac dysfunction.