sodium channel inhibitor 2

Sodium Channel Inhibitor 2 [Sodium Channel inhibitor 2] is a blocker of sodium channels.

Valproic Acid (2-Propylpentanoic Acid) is an HDAC inhibitor that suppresses HDAC1 activity and induces HDAC2 degradation, exhibiting oral bioavailability. Valproic Acid activates Notch1 signalling and inhibits the proliferation of small cell lung carcinoma cells, making it applicable for research into epilepsy and bipolar disorder.

Camostat mesylate (FOY-S980) is a trypsin-like protease inhibitor and inhibits airway epithelial sodium channel (ENaC) function.

Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use in Europe, the United States and Canada as an adjunctive therapy for partial-onset seizures that are not adequately controlled with conventional therapy.

Taurochenodeoxycholic acid sodium (Sodium taurochenodeoxycholate) is one of the main bioactive substances of animals' bile acid. Taurochenodeoxycholic acid sodium induces apoptosis and shows obvious anti-inflammatory and immune regulation properties. It can increase glucose-induced insulin secretion and stimulate the electrical activity of α2-cells and enhance cytosolic Ca(2+) concentration ([Ca(2+)](c)).

DPP8/9-IN-2 (Compound 21) is an inhibitor targeting DPP8 and DPP9 with IC50 values of 0.22 nM and 3 nM, and Ki values of 2.9 nM and 6 nM, respectively. It exhibits certain cardiac toxicity, with IC50 values against the hERG potassium channel, Nav1.5 sodium channel, and Cav1.2 calcium channel of 0.7 μM, 29.0 μM, and 27.7 μM. DPP8/9-IN-2 is applicable for research into diseases such as cancer.

Nav1.7-IN-22 (P58 13-2) is a selective inhibitor of the voltage-gated sodium channel Nav1.7. By blocking the activity of the Nav1.7 channel, Nav1.7-IN-22 suppresses the generation and transmission of abnormal electrical signals in sensory neurons. This compound is applicable for research related to pain.

Eslicarbazepine (Stedesa) can be used for adjunctive therapy for adults with partial-onset seizures.

Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide (T0267) is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium current.3 Zonisamide (T0267) inhibits H. pylori recombinant carbonic anhydrase (CA) and the human CA isoforms I, II, and V with Ki values of 218, 56, 35, and 21 nM, respectively.4,5 In mice, it has anticonvulsant activity against maximal electroshock seizure (MES) and pentylenetetrazole-induced maximal, but not minimal, seizures (ED50s = 19.6, 9.3, and >500 mg/kg, respectively). Zonisamide (T0267) (40 mg/kg, p.o.) prevents MPTP-induced decreases in the levels of dopamine , but not homovanillic acid or dihydroxyphenyl acetic acid , and increases MPTP-induced decreases in the dopamine turnover rate in mouse striatum in a model of Parkinson's disease.6 Formulations containing zonisamide have been used in the treatment of partial seizures in adults with epilepsy.

Amiloride (MK-870) is an inhibitor of the epithelial sodium channel (ENaC) and the urokinase-type plasminogen activator receptor (uPAR). It also acts as a blocker of the polycystin-2 (PC2; TRPP2) channel.

TRPC6-IN-3 ((4-(6-Aminopyridazin-3-yl)piperidin-1-yl)(5-(4-fluorophenoxy)-4-methoxypyridin-2-yl)methanone) is an orally active inhibitor of the transient receptor potential canonical 6 (TRPC6) ion channel. It regulates intracellular calcium concentration and influences membrane potential by modulating the flux of cations, including calcium and sodium ions. TRPC6-IN-3 can be used for research on respiratory system-related diseases.

ICA-121431 (2,2-Diphenyl-N-[4-(thiazol-2-ylsulfamoyl) is a nanomolar potent small molecule Nav1.7 channel inhibitor with IC50 of 19 nM for rat Nav1.7, with little or no activity against human Nav1.5 or Nav1.7 channels.

Licarbazepine (10,11-hydroxy-10,11 Dihydrocarbamezer) is the pharmacologically active metabolite of oxcarbazepine, a drug indicated for the treatment of partial seizures and bipolar disorders.

Ceratotoxin-2 (CcoTx2) is a voltage-gated sodium channel inhibitor with half maximal inhibitory concentrations (IC50) of 8 nM for Na v 1.2/β 1 and 88 nM for Na v 1.3/β 1 [1].

Pterinotoxin-2 is a peptide toxin that acts as a sodium channel inhibitor [1].

Myr-Tat-CBD3 is a chemical compound that serves as an inhibitor of the protein-protein interaction between the N-type voltage-gated calcium channel Cav2.2 and collapsin response mediator protein 2 (CRMP2). This compound effectively disrupts the Cav2.2-CRMP2 interaction by about 81% at a 10 µM concentration and demonstrates an inhibitory concentration 50 (IC50) value of approximately 2.8 µM against potassium-induced calcium influx in primary rat dorsal root ganglion (DRG) neurons. Furthermore, at a concentration of 20 µM, Myr-Tat-CBD3 specifically inhibits calcium currents without affecting sodium currents in primary DRG neurons. Additionally, intrathecal administration of 20 µg/5 µl of Myr-Tat-CBD3 effectively mitigates carrageenan-induced declines in paw withdrawal latencies in rats, indicating its potential for pain relief. The compound also notably reduces cue-induced reinstatement of cocaine-seeking behavior in rats, suggesting therapeutic potential in addiction treatment.

LTGO-33 is a species-specific inhibitor of the voltage-gated sodium channel NaV1.8, inhibiting NaV1.8, NaV1.1-NaV1.7, and NaV1.9.LTGO-33 inhibits wild-type and multiple NaV1.8 variants associated with human pain disorders and can be used for the study of pain.hBChE-IN-2 is a low affinity Nurr1 agonist.

Nav1.8-IN-1 (CHEMBL1270208) is an inhibitor of human NaV1.8