GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects.

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

Zoniporide (CP-597396) hydrochloride hydrate is a potent and selective inhibitor of sodium-hydrogen exchanger type 1 (NHE-1). Zoniporide hydrochloride hydrate inhibits human NHE-1 (IC50=14 nM), and has >150-fold selectivity versus other NHE isoforms. Zoniporide hydrochloride hydrate potently inhibits ex vivo NHE-1-dependent swelling of human platelets (IC50=59 nM).

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

A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.

Sodium Channel inhibitor1, one of 3-Oxoisoindoline-1-carboxamides, is a novel and selective voltage-gated sodium channel for pain treatment.

Procaine is a benzoic acid derivative with local anesthetic and antiarrhythmic properties. Procaine binds to and inhibits voltage-gated sodium channels, thereby inhibiting the ionic flux required for the initiation and conduction of impulses.

Pilsicainide hydrochloride is a selective Na+ channel blocker (IC30 values are 9 and 60 μM for inward Na+ and Ca2+ currents respectively). Shows antiarrhythmic effects in vivo. Orally active.

Phenytoin sodium is an inactive voltage-gated sodium channel stabilizer.

PF-05241328 is a potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7), with an IC50 of 31 nM.

Oxcarbazepine inhibits the binding of [3H]BTX to sodium channels with IC50 of 160 μM and also inhibits the influx of 22Na+ into rat brain synaptosomes with IC50 about 100 μM.

Cariporide is a selective Na+/H+ exchanger isoform 1 (NHE1) inhibitor (IC50 values are 0.05, 3 and 1000 μM for NHE1, NHE3 and NHE2 respectively).

AM-2099 is a potent and selective NaV1.7 Inhibitor.

A-317567 (A317567) is a novel potent acid sensing ion channel (ASIC) blocker with IC50 of 2-30 uM.

A potent and selective voltage-gated sodium channel Nav1.7 antaognist with IC50 of 8.5 nM.