Sodium Channel Antagonist

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.

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.

PF 04531083 is an orally active and selective Na_V1.8 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.

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.

GX-674 is a potent, state-dependent, isoform-selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC₅₀ of 0.1 nM at -40 mV.

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.

GpTx-1 TFA is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 TFA demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and Na_V1.5 (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively.

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379. AMG8379 is a potent, orally active and selective sulfonamide antagonist of NaV1.7, with IC₅₀s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively .

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.

AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC₅₀s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC₅₀ of 3.1 nM.

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.

GpTx-1 is a peptide-based Na_V1.7 sodium channel antagonist isolated from the venom of the Chilean spider Grammostola porter. GpTx-1 demonstrates potent inhibitory activity against the Na_V1.7 channel with an IC₅₀ value of 10 nM, while exhibiting excellent selectivity for Na_V1.4 (IC₅₀ = 0.301 μM) and Na_V1.5 (IC₅₀ = 4.20 μM), showing >20-fold and >950-fold selectivity respectively.

Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38 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 Mc-VC-PAB and the topoisomerase I inhibitor SN38 (HY-13704). The ADC toxic molecule and linker part are Mc-VC-PAB-SN38 (HY-131057). Anti-SLC34A2 (Lifastuzumab)-MC-Vc-PAB-SN38 can be used in cancer research.

Jingzhaotoxin-V is a peptide that inhibits potassium currents in Xenopus laevis oocytes with an IC₅₀ value of 604.2 nM. Jingzhaotoxin-V also inhibits tetrodotoxin-resistant and tetrodotoxin-sensitive sodium currents in rat dorsal root ganglion neurons with IC₅₀ values of 27.6 and 30.2 nM, respectively.