Sodium Channel Antagonist

Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.

LK-2 is an antagonist for ASIC1a with a K_d of 1.9 μM. LK-2 reduces glutamate-induced ASIC1a current-enhancement with an IC₅₀ of 6.6 μM. LK-2 exhibits neuroprotective efficacy in mouse ischemic stroke model, with improved motor and coordination skills. LK-2 is blood-brain barrier (BBB) penetrable.

Hardwickiic acid ((-)-Hardwickiic acid) is a diterpenoid compound. Hardwickiic acid can block tetrodotoxin-sensitive voltage-dependent sodium channels and possesses multiple activities such as insecticidal, antinociceptive, and neurotransmitter release-regulating effects. Hardwickiic acid can be used in the study of neurological diseases.

ASIC1a antagonist-1 (Compound 5b) is an orthosteric noncompetitive Acid sensing ion channels 1a (ASIC1a) antagonist with an IC₅₀ of 27 nM (pH 6.7). ASIC1a antagonist-1 shifts pH dependence of ASIC1a activation and inhibits its maximal evoked response. ASIC1a antagonist-1 completely inhibits long-term potentiation (LTP) induction in CA3-CA1 pathway. ASIC1a antagonist-1 can be used for brain diseases and pathologies research.

Hainantoxin-IV is a specific antagonist of Sodium Channel, targeting to tetrodotoxin-sensitive (TTX-S) voltage-gated sodium channels. His28 and Lys32 are the key resiudes of Hainantoxin-IV for binding with target, while Hainantoxin-IV adopts an inhibitor cystine knot motif.

Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na⁺ channel, is a weak uncompetitive NMDA receptor antagonist with IC₅₀s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively. Remacemide hydrochloride is an anticonvulsant agent.

Irampanel (BIIR 561) is an AMPA receptor and voltage-dependent sodium channel blocker. Irampanel inhibits kainate-induced currents in rat cortical neurons.

Nav1.7-IN-15 (Compd 9) is a potent and state-dependent Nav1.7 antagonist, with an IC₅₀ of 0.42 μM for hNav1.7 PX.

AM-36 is a neuroprotective agent with combined antioxidant and sodium channel blocking actions. AM-36 can inhibit cell apoptosis and ROS prodiction. AM-36 can reduce neuronal damage and DA release after middle cerebral artery occlusion in rats. AM-36 can be used for the researches of inflammation and neurological disease, such as stroke.

Fosphenytoin (disodium) (Standard) is the analytical standard of Fosphenytoin (disodium). This product is intended for research and analytical applications. Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.

Fosphenytoin-d₁₀ (disodium) is deuterium labeled Fosphenytoin (disodium). Fosphenytoin sodium is a phenytoin proagent with similar anticonvulsant properties. Its main mechanism is to block frequency-dependent, use-dependent and voltage-dependent neuronal sodium channels, and therefore limit repetitive firing of action potentials.

Diphenidol (hydrochloride) (Standard) is the analytical standard of Diphenidol (hydrochloride). This product is intended for research and analytical applications. Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M1-M4 receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na+, K+, and Ca2+) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea[4].

Anti-SLC34A2 (Lifastuzumab)-McMMAF is an antibody-drug conjugate (ADC) consisting of the humanized anti-SLC34A2 (sodium-dependent phosphate transporter 2) antibody Lifastuzumab (HY-P99970) conjugated to the protective group maleimidocaproyl and the tubulin inhibitor MMAF (HY-15579). The ADC toxic molecule and linker part McMMAF (HY-15578). Anti-SLC34A2 (Lifastuzumab)-McMMAF induces apoptosis and can be used in cancer research.

Anti-SLC34A2 (Lifastuzumab)-SMCC-DM1 is an antibody-drug conjugate (ADC) consisting of the humanized anti-SLC34A2 (sodium-dependent phosphate transporter 2) antibody Lifastuzumab (HY-P99970) conjugated to the linker SMCC (HY-42360) and the the cytotoxic microtubule inhibitor DM1 (HY-19792). The ADC toxic molecule and linker part are SMCC-DM1 (HY-101070). Anti-SLC34A2 (Lifastuzumab)-SMCC-DM1 can be used in the research of cancer.

Nefopam (Fenazoxine) is an orally active, non-opioid and non-steroidal centrally acting analgesic agent. Nefopam blocks voltage-sensitive sodium channels (IC₅₀=27 μM) and modulates glutamatergic transmission in rodents. Nefopam can be used in studies of neuropathic pain, anticonvulsant, as well as the prevention of postoperative shivering and hiccups.

Anti-SLC34A2 (Lifastuzumab)-SPDB-DM4 is an antibody-drug conjugate (ADC) consisting of the humanized anti-SLC34A2 (sodium-dependent phosphate transporter 2) antibody Lifastuzumab (HY-P99970) conjugated with the linker SPDB (HY-12448) and the tubulin inhibitor DM4 (HY-12454). The ADC toxic molecule and linker part are sulfo-SPDB-DM4 (HY-101141). Anti-SLC34A2 (Lifastuzumab)-SPDB-DM4 can be used in cancer research.

N-Depropylpropafenone is an active metabolite of Propafenone (HY-B0432), generated through the CYP450 enzyme system (mainly CYP2D6). It functions by blocking sodium ion channels, slowing myocardial conduction and exhibiting certain antiarrhythmic effects.

EO-122 is a potent antagonist of calcium channel and sodium channel potentially for the research of arrhythmia.

Diphenidol-d₁₀ (hydrochloride) (Difenidol hydrochloride-d₁₀) is deuterium labeled Diphenidol (hydrochloride). Diphenidol hydrochloride (Difenidol hydrochloride) is a non-selective muscarinic M₁-M₄ receptor antagonist, has anti-arrhythmic activity. Diphenidol hydrochloride is also a potent non-specific blocker of voltage-gated ion channels (Na⁺, K⁺, and Ca²⁺) in neuronal cells. Diphenidol hydrochloride can be used in the study of antivertigo and antinausea.

PF 04531083 (Standard) is the analytical standard of PF 04531083 (HY-105283). This product is intended for research and analytical applications. PF 04531083 is an orally active and selective NaV1.8 blocker with an IC₅₀ of 0.7 μM. PF 04531083 is a blood-brain barrier (BBB) penetrant compound. PF 04531083 can be used for the research of respiratory system and neuropathic/inflammatory pain.