Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant (tau) of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6.

Zilvetrigine is a sodium channel blocker. Zilvetrigine can be used as analgesics.

Quinacainol dihydrochloride (PK 10139 dihydrochloride) is the dihydrochloride salt form of Quinacainol.

Olisutrigine bromide is a sodium channel blocker, which can be used as analgesics.

N-Hydroxy riluzole is a metabolite of the antiglutamatergic agent Riluzole.

ETD001 is a long-acting ENaC inhibitor, with an IC50 of 57.5 nM in cultured HBE cells. ETD001 can be used in the study for cystic fibrosis.

ErSO-TFPy activates the sodium channel TRPM4, causes an imbalance of intracellular calcium and sodium ions. ErSO-TFPy exhibits low nanomolar cytotoxicity in ERα+ breast cancer cell lines (IC50 = 5-25 nM) through induction of necrosis. ErSO-TFPy exhbits antitumor efficacy in mouse models.

DAPI (Compound 3) is an acid-sensing ion channel 3 (ASIC3) inhibitor. DAPI binds to ASIC3 and blocks the channel function. DAPI can be used in the study of chronic pain treatment.

CL-424032 is a sodium channel inhibitor.

CAY10568 is a compound based on QX-314 and a linker. MC-PEG2-VA-PAB-Exatecan can be used for synthesis of ADCs.

10,11-Dihydroxycarbamazepine is a metabolite of the anticonvulsant Carbamazepine. Carbamazepine is an orally active pressure-sensitive sodium ion channel blocker.

(R)-(+)-Bupivacaine hydrochloride is a voltage-gated sodium channel inhibitor. (R)-(+)-Bupivacaine hydrochloride can selectively block the voltage-gated sodium channels on nerve cell membranes, inhibit the influx of sodium ions, and thus prevent the generation and conduction of nerve impulses, exerting local anesthetic activity. (R)-(+)-Bupivacaine hydrochloride can be used in research of acute pains.

Lacosamide (Vimpat; Erlosamide) is a medication developed for the adjunctive treatment of partial-onset seizures and diabetic neuropathic pain.

Ethacizine hydrochloride (Ethacizin; NIK-244) is a Class Ic antiarrhythmic agent, which means it is part of a group of drugs that primarily act by blocking sodium channels in the heart. This class of antiarrhythmic agents is known for their potent effects on slowing conduction in the heart, particularly in the atria, ventricles, and the His-Purkinje system.

ABBV-318 is a potent Nav1.7/ Nav1.8 blocker, with IC50s of 2.8 μM and 3.8 μM for hNav1.7 and hNav1.8, respectively. ABBV-318 can be used for the research of pain.

SSCI-2 is a highly potent, selective NaV1.7 inhibitor with IC50 of 9 and 17 nM on human and rhesus Nav1.7 channels, respectively.SSCI-2 showed robust selectivity over other human and rhesus Nav channel paralogs, with the exception of Nav1.2 channels (IC50 183 nM for hNaV1.2), shows no other channels and receptors in 114 enzymatic, radioligand binding, and cellular assays.SSCI-2 also exhibits high potency in manual patch clamp experiments (IC50=24/62 nM for huma/rhesus Nav1.7 channels).SSCI-2 inhibits withdrawal responses to noxious heat in rhesus monkeys.

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.

LTGO-33 is a potent, selective inhibitor of voltage-gated sodium channel NaV1.8 with IC50 of 44 nM (hNaV1.8), 600-fold selectivity against NaV1.1-NaV1.7 and NaV1.9.

Ancistrotecine B (Compound 2) is a Nav1.7 channel inhibitor (IC50: 0.73 μM). Ancistrotecine B relieves inflammatory pain in mice.

XPC-7224 is a potent, selective NaV1.6 inhibitor with IC50 of 78 nM and 130 nM for human and mouse NaV1.6, respectively, interacts with the inactivated state of the channel.

XPC-5462 is a potent, selective dual inhibitor of NaV1.6 and NaV1.2 with IC50 of 10.9 nM and 10.3 nM, respectively.

UTX-143 is a potent, selective sodium-hydrogen exchange subtype 5 (NHE5) inhibitor with IC50 of 3.11 uM, 80-fold selective over NHE1.

DS43260857 is a potent, selective NaV1.7 inhibitor with IC50 of 15 nM (hNaV1.7), shows 440-fold and 930-fold selectivity over hNaV1.1 and hNaV1.5, respectively.

BW-031 iodide is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

BW-031 chloride is a potent cationic sodium channel inhibitor, inhibited Nav 1.7 (IC50=9.5 uM) and Nav 1.1 channels with approximately sixfold greater potency than QX-314.

Benzocaine is a local anesthetic.

Aneratrigine is a sodium channel protein type 9 subunit alpha blocker.

(-)-Sparteine sulfate pentahydrate is a class 1a antiarrhythmic agent and a sodium channel blocker.

PF-01247324 is an orally bioavailable, selective and potent NaV1.8 channel blocker that inhibits that exhibits analgesic efficacy in rodent behavioral models of pain.

GNE-131 is a novel NaV1.7 inhibitor with IC50 0.003uM,improving metabolic stability,efficacy in mouse IEM model at C-plasma <2.8uM.