PF-04885614 is a potent NaV1.8 inhibitor, extracted from patent US2018328915. PF-04885614 has potential for neurological and neurodevelopmental diseases treatment.

6-Benzoylheteratisine is a naturally occurring antagonist of the Na+ channel activator aconitine.

GDC-0310 is a selective acyl-sulfonamide Nav1.7 inhibitor, with an IC50 of 0.6 nM for hNav1.7.

Nav1.7-IN-8 is a potent blockage of NaV1.7 with high selectivity for the inhibition of NaV1.7 over the subtypes hNaV1.1 and hNaV1.5. Nav1.7-IN-8 inhibits CYP2C9 and CYP3A4 with an IC50 of 0.17 μM and 0.077 μM, respectively. Nav1.7-IN-8 displays significant analgesic effects in rodent models of acute and inflammatory pain.

GX-201 is a selective NaV1.7 inhibitor, with an IC50 of <3.2 nM for hNaV1.7.

Phrixotoxin 3 TFA is a potent blocker of voltage-gated sodium channels, with IC50s of 0.6, 42, 72, 288, 610 nM for NaV1.2, NaV1.3, NaV1.4, NaV1.1 and NaV1.5, respectively. Phrixotoxin 3 TFA modulates voltage-gated sodium channels with properties similar to those of typical gating-modifier toxins, both by causing a depolarizing shift in gating kinetics and by blocking the inward component of the sodium current.

Propafenone D5 (SA-79 D5) hydrochloride is the deuterium labeled Propafenone hydrochloride. Propafenone (SA-79) hydrochloride is a class of anti-arrhythmic medication, which treats illnesses associated with rapid heart beats such as atrial and ventricular arrhythmias.

Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.

NHE3-IN-2 is a Na+/H+ exchanger-3 (NHE3) inhibitor ( patent WO2001079186A1, example 6-Chlor-4-phenyl-2-chinazolinyl-guanidin).

Idrevloride, an epithelial sodium channel (ENaC) inhibitor (WO2016133967), can be used for the research of skin disorders.

TC-N 1752 is a potent and orally active inhibitor of Nav1.7, with IC50s of 0.17 μM, 0.3 μM, 0.4 μM, 1.1 μM and 2.2 μM at hNav1.7, hNav1.3, hNav1.4, hNaV1.5 and rNav1.8, respectively. TC-N 1752 also inhibits tetrodotoxin-sensitive sodium channels. TC-N 1752 shows analgesic efficacy in the Formalin model of pain.

NBI921352 is a Nav1.6 inhibitor with an IC50 value of 3.765 μM.

Bliretrigine is a sodium channel blocker. Bliretrigine has the effect of relieving pain.

S-Bioallethrin is a pyrethroid insecticide. S-Bioallethrin disrupts nerve function by modifying the gating kinetics of transitions between the conducting and nonconducting states of voltage-gated sodium channels.

QX-222 chloride, a trimethyl analogue of Lignocaine, is a potent Na+ channel blocker.

Tocainide hydrochloride is an orally activesodium channel blocker, it blocks the sodium channels in the pain-producing foci in the nerve membranes. Tocainide hydrochloride is a primary amine analog of lidocaine, can be used for the treatment of tinnitus.

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.

Nav1.8-IN-1 (Compound 31) is a potent inhibitor of Na(v)1.8 sodium channel. Nav1.8-IN-1 has the potential for the research of inflammatory and neuropathic pain.

NS383 is a potent and uniquely selective inhibitor of rat ASICs containing 1a and/or 3 subunits. NS383 inhibits H(+)-activated currents recorded from rat homomeric ASIC1a, ASIC3, and heteromeric ASIC1a+3 with IC50 values ranging from 0.61 to 2.2 μM. NS383 is well tolerated and capable of reversing pathological painlike behaviors, presumably via peripheral actions, but possibly also via actions within central pain circuits.

ASIC1a inhibitor 5b is a highly selective and potent ASIC1a inhibitor, inhibits proton-evoked ASIC1a currents with an apparent IC50 of 27 nM at pH 6.7.ASIC1a inhibitor 5b can potently and selectively inhibit acid-induced activation of ASIC1a-containing channels, including both ASIC1a homotrimers and ASIC1a-ASIC2 heterotrimers, in a pH-dependent manner.ASIC1a inhibitor 5b binds to the acidic pocket of ASIC1a, exhibits a dramatic leftward shift under pH 6.7 activation of ASIC1a as compared to pH 6.0.ASIC1a inhibitor 5b protected neurons from ASIC1a-dependent cell death and is blood-brain barrier permeable.ASIC1a inhibitor 5b (5 mg/kg) attenuated neurological impairment and alleviated infarct volume in mouse MCAO model of ischemic stroke.

BI 1265162 is a potent ENaC inhibitor, inhibits Na+ transport with IC50 3 nM and 8 nM in M1 and NCI-H441 cells, respectively.BI 1265162 dose-dependently inhibited Na+ transport and decreased water resorption in cell line models.BI 1265162 reduced liquid absorption in rat lungs and increased MCC in sheep, with no effects on renal function in the animal models.BI 1265162 alone and in combination with CF transmembrane conductance regulator (CFTR) modulators decreased water transport and increased MCC in both normal and CF airway human epithelial models.

BI-8668 (BI 8668) is a highly potent and selective epithelial sodium channel (ENaC) inhibitor, inhibits Na+ current with IC50 of 17 nM (Ussing chamber assay); BI-8668 inhibits ENaC-mediated water permeability through cell monolayers of the cell line M-1 (M-1 cells: mouse kidney tubules cells) with 81% inhibition at 3 uM.