Sodium Channel Activator

Permethrin (NRDC-143) is an insecticide, acaricide and a high selectively inhibitor of the Mitochondrial complex I, found in sediment and water samples. Permethrin shows estrogenic in vivo and anti-estrogenic activity in vitro. Permethrin also acts as a neurotoxin affecting neuron membranes by prolonging Sodium channel activation. Permethrin decreases resistance to bacterial infections in medaka (Oryzias latipes).

Zorevunersen sodium is an antisense oligonucleotide targeting the Scn1a gene based on TANGO technology. Zorevunersen sodium increases Scn1a mRNA transcripts and elevates the expression level of NaV1.1 protein. Zorevunersen sodium restores the excitability of PV interneurons, thereby reducing seizures and prolonging survival in mice. Zorevunersen sodium can be used for research on Dravet syndrome.

Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD₅₀=0.15 ng/mg) and C. quinquefasciatus (LD₅₀=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material.

S3969 is a potent and reversible activator of the human epithelial sodium channel (hENaC). The apparent EC₅₀ for S3969 activation of hENaC is 1.2 μm.

GMQ (hydrochloride) is a ASIC (acid-sensing ion) channel activator with an EC₅₀ value of 1.83 mM for ASIC3 at pH 7.4. GMQ (hydrochloride) opens only ASIC3 but no other ASICs at pH 7.4. GMQ (hydrochloride) can be used for neurological disease research.

Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na⁺ channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain). Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na⁺ channels, inhibits the inactivation of Na⁺ channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation.

Lu AE98134, an activator of voltage-gated sodium channels, acts as a partly selective Na_v1.1 channels positive modulator. Lu AE98134 also increases the activity of Na_v1.2 and Na_v1.5 channels but not of Na_v1.4, Na_v1.6 and Na_v1.7 channels. Lu AE98134 can be used to analyze pathophysiological functions of the Na_v1.1 channel in various central nervous system diseases, including cognitive restoring in schizophrenia, et al.

MitTx is a complex formed by MitTx-α and MitTx-β. MitTx is an ASIC1 channel activator with EC₅₀ values of 9.4 and 23 nM for ASIC1a and ASIC1b isoforms, respectively. MitTx is highly selective for ASIC1 isoforms at neutral pH. Under acidic conditions, MitTx greatly enhances proton-evoked ASIC2a channel activation.

3-Deoxyaconitine a diterpenoid alkaloid, is a sodium channel activator.

Zorevunensen (STK-001) negative control is the negative control form of Zorevunensen (HY-148410). Zorevunensen is an antisense oligonucleotide that is intended to increase the level of productive SCN1A mRNA and consequently increase the expression of the sodium channel Nav_1.1 protein. Zorevunersen is used for the study of Dravet syndrome.

β-Pompilidotoxin (β-PMTX), a wasp venom, can slow sodium channel inactivation and increases steady-state sodium current in cells.

Bifenthrin (Standard) is the analytical standard of Bifenthrin. This product is intended for research and analytical applications. Bifenthrin is a synthetic pyrethroid insecticide. Bifenthrin prolongs the opening time of Nav1.8 sodium channels, leading to membrane depolarization and conductance block in the insect nervous system, thereby disrupting neural function. Bifenthrin was effective in inhibiting A. gambiae (LD50=0.15 ng/mg) and C. quinquefasciatus (LD50=0.16 ng/mg). Bifenthrin has good lethality against susceptible and resistant mosquitoes and is very effective in inhibiting blood sucking and can be developed as a mosquito-removal netting material.

Halofuginone hydrobromide (Standard) (RU-19110 hydrobromide (Standard)) is the analytical standard of Halofuginone hydrobromide (HY-N1584A). This product is intended for research and analytical applications. Halofuginone hydrobromide (RU-19110 hydrobromide), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrobromide is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromide is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrobromide has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

Halofuginone (Standard) (RU-19110 (Standard)) is the analytical standard of Halofuginone (HY-N1584). This product is intended for research and analytical applications. Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

Halofuginone hydrochloride (RU-19110 hydrochloride), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrochloride is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrochloride is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrochloride has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.

δ-Theraphotoxin-Hm1a toxin is a selective Na_v1.1 activator. δ-Theraphotoxin-Hm1a toxin elicits pain and touch sensitivity. δ-Theraphotoxin-Hm1a toxin can be used for the research of irritable bowel syndrome.

Cn2 toxin is aβ- toxoins. Cn2 toxin can bind to the voltage sensing domain of voltage gated sodium channels (Na_v) .

Jasmolin II is an insecticide targeting voltage-gated sodium channels in insects. Jasmolin II leads to neuronal hyperexcitation and insect paralysis. Jasmolin II is promising for research of agricultural pests.

BDF 9148 is a sodium-channel activator with antiarrhythmic properties that produces a significant CAMP-independent positive inotropic effect in left ventricular myocardium from failing hearts. BDF 9148 is promising for research of myocardial failure.

Halofuginone hydrochloride (Standard) (RU-19110 hydrochloride (Standard)) is the analytical standard of Halofuginone hydrochloride (HY-N1584B). This product is intended for research and analytical applications. Halofuginone hydrochloride (RU-19110 hydrochloride), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a K_i of 18.3 nM. Halofuginone hydrochloride is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrochloride is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca²⁺ channels. Halofuginone hydrochloride has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects.