ARN 23746 (ARN-23746) is a potent, selective inhibitor of Na+-K+-Cl- importer NKCC1, shows NKCC1 inhibition 31.8% at 10 uM, and 95.2% at 100 uM in the Cl− influx assay on NKCC1-transfected HEK293 cells.ARN23746 did not show significant NKCC2 inhibition and KCC2 inhibition at 10 uM.ARN23746 selectively blocks NKCC1 in a human cell line and restore the physiological [Cl−]i in murine DS neurons in culture, has excellent solubility and metabolic stability, and displays no issues with off-target activity in vitro.ARN23746 demonstrated in vivo efficacy in rescuing cognitive impairment in a DS mouse model and social deficits and repetitive behaviors in an autism mouse model.

IPPQ is a small molecule that selectively target the interface between the N-type calcium (CaV2.2) channel and CaVβ, specifically binds to CaVβ2a and inhibits CaVβ2's interaction with CaV.2-AID (alpha interacting domain).

HZS60 is a NMDAR/TRPM4 inhibitor with brain permeability that can improve cerebral ischemia. HZS60 has significant neuroprotective effects on primary neuronal ischemic damage caused by NMDA and oxygen-glucose deprivation/reoxygenation. HZS60 exhibits good pharmacokinetic characteristics and can inhibit cerebral ischemia-reperfusion injury. HZS60 can be used as a potential inhibitor of ischemic stroke.

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.

ZQMT-10 is an orally active and potent antagonist of TRPA1, with the Kd of 1.04 μM. ZQMT-10 plays an important role in cancer research.

Davasaicin (KR 25018), Capsaicin derivative and a δ-opioid receptor agonist. AZ 12488024 is available for research into major depressive disorder.

CMP233 is a potent antagonist of TRPM4, with the IC50 of 0.15 μM. CMP233 plays an important role in neurodegenerative disorders research.

(S)-AMG-628 (Compound 16q) is the S-isomer of AMG-628. (S)-AMG-628 is the orally active antagonist for TRPV1, that inhibits the Capsaicin- and acid-induced Ca2+-influx with IC50 of 7 nM and 5 nM in CHO cell. (S)-AMG-628 ameliorates Capsaicin-induced rats flinching, and reverses the thermal hypersensitivity in CFA-induced inflammatory pain models.

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.

rel-Licogliflozin is a relative configuration of Licogliflozin.

Olorigliflozin is a sodium glucose co-transporter inhibitor with anti-hyperglycemic effects.

Pantoprazole sulfone is a metabolite of the gastric H+/K+ ATPase pump inhibitor Pantoprazole. AR-13503 is the hydrolytic metabolite of AR-13324 mesylate. AR-13324 is a ROCK kinase and PKC inhibitor with anti-angiogenic and retinal health-improving effects, showing potential for use in retinal disease research.

N3-Methyl pantoprazole is an impurity of Pantoprazole-induced stereotyped behaviors and emesis, inhibits discriminative avoidance behavior, and induces catalepsy in rats models.

4-Hydroxy omeprazole sulfide is a metabolite of the proton pump inhibitor Omeprazole.

2-(Trifluoromethyl)cinnamic acid is a cinnamic acid derivative that inhibits the proton pump (H+/K+-ATPase), thereby reducing gastric acid secretion. 2-(Trifluoromethyl)cinnamic acid also improves delayed gastric emptying and can be used in research on gastric diseases such as acute gastritis and gastric ulcers.

Tetramisole is an orally active, selective inward rectifier potassium channel agonist with an EC50 of approximately 30 μM for the Kir2.1 subunit. Tetramisole is also an anti-nematode agent that blocks neuromuscular transmission by non-competitive depolarization. Tetramisole promotes the forward transport of Kir2.1 channels, hyperpolarizes the resting potential (RP), shortens the action potential duration (APD), inhibits intracellular calcium overload and the PKA signaling pathway, and exerts anti-arrhythmic and anti-myocardial remodeling activities. Tetramisole can be used in cardiac electrophysiology research and research related to myocardial ischemia and heart failure.

SKP-451 is an ATP-sensitive potassium (K+) channel agonist. SKP-451 activates the ATP-sensitive K+ channels, promotes the efflux of K+, causes membrane hyperpolarization, and inhibits the influx of Ca2+, thereby relaxing the vascular smooth muscle. SKP-451 relaxs the canine coronary artery, rabbit basilar artery, and vertebral artery. SKP-451 also reduces the mean arterial blood pressure of conscious spontaneously hypertensive rats (SHR). SKP-451 is promising for research of cardiovascular diseases.

Opakalim is the activator for potassium channel and exhibits antiepileptic activity.

ONO-TR-772 (VU6018042) is a selective TREK inhibitor (IC50: 15 nM). ONO-TR-772 enhances recognition memory in the MK-801-stimulated NOR mouse model. ONO-TR-772 can be used in the study of diseases related to cognitive impairment.

ONO-2920632 is an orally active and central nervous system (CNS)-penetrant TREK activator, with EC50 values of 0.3 µM and 2.8 μM for TREK-1 and TREK-2, respectively. ONO-2920632 exhibits selectivity for other K2P channels (>91-fold selective versus TASK1, TASK2, TASK3, TRAAK, and TWIK2; 31-fold selective versus TRESK). ONO-2920632 possesses analgesic effects and can be used in research on pain, migraine, and neurological disorders.