Sodium Channel

Etidocaine Hydrochloride (W19053) is a long-acting anesthetic and a blocker of the voltage-gated sodium channel.

Stability Hygroscopic Applications N-Despropyl Propafenone Hydrochloride is a metabolite of Propafenone (P757500), a sodium channel blocker. Antiarrhythmic (class IC). References Hollmann, M., et al.: Arzneim.-Forsch., 33, 763 (1983); Bryson, H. M., et al.:Drugs, 45, 85 (1993); Rae, A. P., et al.: Am. J. Cardiol., 82, 59N (1998)

Applications Nor Lidocaine-d6 Hydrochloride is the labeled analogue of Nor Lidocaine Hydrochloride (N713500), a hydrochloride salt metabolite of Lidocaine (L397800), a local anesthetic; antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Fukuda, S., et al.: Anesthesiology, 53, 106 (1980); Duce, R., et al.: J. Pharmacol. Exp. Ther., 179, 580 (1971); Kronberg, G.H., et al.: J. Med. Chem., 16, 739 (1973); Groningsson, K., et al.: Anal. Profiles Drug Subs., 14, 207 (1985); Davies, P.S., et al.: Drugs, 64, 937 (2004)

Disopyramide, or Triombrin, a class I anti-arrhythmic with membrane-stabilizing effects, has heart depressant, anticholinergic, and anesthetic properties.

ErSO-TFPy activates the sodium ion channel TRPM4, resulting in an imbalance of intracellular calcium and sodium ions. It exhibits low nanomolar-level cytotoxicity (IC50 = 5-25 nM) by inducing necrosis in ERα+ breast cancer cell lines. Additionally, ErSO-TFPy shows antitumor activity in mouse models.

Benzonatate is an antagonist of sodium channel protein.

R 56865 is a weak potential-operated channel inhibitor that inhibits the late sodium current in human isolated cardiomyocytes.

(5R)-BW-4030W92 is the R-type of BW-4030W92, the active enantiomer.

Lidocaine HCl: local anesthetic, antiarrhythmic, stronger & longer-lasting than procaine but shorter than bupivacaine/prilocaine.

Stability Hygroscopic Applications Anesthetic (local); antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Duce, R., et al.: J. Pharmacol. Exp. Ther., 179, 580 (1971), Kronberg, G.H., et al.: J. Med. Chem., 16, 739 (1973), Groningsson, K., et al.: Anal. Profiles Drug Subs., 14, 207 (1985), Davies, P.S., et al.: Drugs, 64, 937 (2004),

Halofuginone (RU-19110) inhibits prolyl-tRNA synthetase (Ki=18.3 nM), down-regulates Smad3, and blocks TGF-β at 10 ng/ml.

Applications The N-oxide of the local anesthetic Bupivacaine (B689546). Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

Tizolemide, a sulfonamide diuretic compound with alkaline properties, is cleared through the tubular transport system. It induces changes in the passive transport components across the basolateral membrane of isolated frog skin.

Vinpocetine (RGH-4405) is a selective inhibitor of cyclic GMP phosphodiesterase (PDE).

Applications Metaflumizone is a semicarbazone insecticide that works by blocking sodium channel in target insects resulting in paralyzation associated with blocking nerve activity. Metaflumizone is useful as a heartworm control treatment. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Zhang, Zhe,, et al.: J. Integrat. Agri. 11, 1145 (2012); Kuhn, D., et al.: Modern. Crop. Protect. Compound., 3, 1273 (2012);

KR-32568 is a sodium/hydrogen exchanger 1 (NHE-1) inhibitor (IC50: 230 nM).

Applications A selective vanilloid receptor antagonist (Ki=3.2uM) References Dickenson and Dray: Br. J. Pharmacol., 104, 1045 (1991), Kwak, et al.: Neuroscience, 86, 619 (1998), Szallasi and Blumberg: Pharmacol. Rev., 51, 159 (999)

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

Lubeluzole (dihydrochloride) acts as a neuroprotective agent by blocking neuronal voltage-gated sodium channels and also affects cardiac sodium channels, exhibiting both tonic and blocking effects. This compound is considered promising in the research of antiarrhythmic agents.

Propafenone hydrochloride (Arythmol8) is a classic anti-arrhythmic medication, which treats illnesses associated with rapid heartbeats such as atrial.

Applications Labelled Prilocaine (P725000). Prilocaine is a local anesthetic of the amino amide type. Prilocaine is often used in dentistry. Prilocaine is also often combined with lidocaine as a preparation for dermal anesthesia (lidocaine/prilocaine or EMLA), for treatment of conditions like paresthesia. References Caliaro, G., et al.: J. Pharm. Biomed. Anal., 26, 427 (2001), Ulmeanu, S., et al.: Pharm. Res., 20, 1317 (2003),

Phenazopyridine HCl, an oral urinary analgesic, may cause nausea, anemia, and liver/kidney toxicity. Possibly carcinogenic.

Silperisone HCl is a muscle relaxant and vasodilator, treating myoclonus, hypertonia, dystonia, and myospasm by blocking Na+ and Ca2+ channels.

Stability Very Hygroscopic Applications The labelled N-oxide of the local anesthetic Bupivacaine (B689546).

ICA-121431: a potent Nav1.7 inhibitor (IC50=19 nM for rat), minimal effect on human Nav1.5/Nav1.7.

Applications A local anesthetic with stimulant properties. Studies have shown its potency to be about half that of Cocaine (C633500). References Wppdward, J.J. et al.: Eur. J. Pharmacol., 277, 7 (1995); Rigon, A.R. et al.: Psychopharmacol., 127, 323 (1996); Wilcox, K.M. et al.: Synapse, 58, 220 (2005);

BS3 Crosslinker (Bis(sulfosuccinimidyl)suberate) is an ADC linker that can be used to synthesize antibody-coupled active molecules.

Stability Hygroscopic Applications Gitoxin acts as in inhibitor of the sodium and potassium ion channels, interfering with ATPase activity and used in cancer treatment as a growth inhibitor. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Colovic, M. et al.: Russ. J. Phys. Chem. A., 83, 1602 (2009); Banuls, L. et al.: Mol. Canc., 12, 33 (2013);

Applications An anti-inflammatory and analgesic agent. Anesthetic (local). Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package References Reynolds, et al.: Br. J. Anaesth., 43, 33 (1971), Tullar, et al.: J. Med. Chem., 14, 891 (1971), Aberg, G., et al.: Acta Pharmacol. Toxicol., 31, 273 (1972),

20(S)-Ginsenoside Rg3 (Rg3) possess an ability to inhibit the lung metastasis of tumor cells via inhibition of the adhesion and invasion of tumor cells.

Clopamide (Brinaldix) is a piperidine and sulfamoylbenzamide-based diuretic with thiazide-like diuretic activity.

NaV1.7 inhibitor-1, an efficacious inhibitor of voltage-gated sodium channel (NaV) 1.7 (IC50 of 0.6 nM for hNaV1.7).

Rufinamide (E 2080), a triazole derivative, is used as voltage-gated sodium channel blocker for the treatment of seizure disorders.

Lifarizine FA is a sodium channel blocker used in the treatment of neurological disorders and cardiovascular diseases, study of stroke.

Applications Zonisamide-13C2-15N is the labeled analogue of Zonisamide (Z700000), a sulfonamide antiseizure agent; blocks repetitive firing of voltagesensitive sodium channels and reduces voltage-sensitive T-type calcium currents. Heterocyclic methanesulfonide with anticonvulsant properties. The compound is under investigation for potential therapeutic use as an antiepileptic drug. Anticonvulsant. References Masuda, Y., et al.: Arzneim.-Forsch., 30, 477 (1980); Hammond, E.J., et al.: Gen. Pharmacol., 18, 303 (1987); Schmidt, D., et al.: Epilepsy Res., 15, 67 (1993); Sorkin, E.M., et al.: Drugs, 45, 760 (1993)

Stability Light and Moisture Sensitive Applications Isotope Labelled analogue of rac-Kavain (K145490), the main kavalactone found in the roots of the kava plant. Kavain is known to exhibit anticonvulsive properties by attenuating vascular smooth muscle contraction through interactions with voltage-dependent sodium and calcium channels. rac-Kavain was shown in recent research to exhibit protective properties on anaerobic glycolysis, ATP content and intracellular calcium and sodium of anoxic brain vesicles. References Gleitz, J., et al: Neuropharmacol., 35, 1743 (1997); Hashimoto, T., et al.: Phytomedicine, 10, 309 (2003); Mulholland, P.J., et al.: Brain. Res., 945, 106 (2002);

Applications A derivative of Vincamine with vasodilating activity. Vasodilator (cerebral). References Han, et al.: J. Biol. Chem., 274, 22337 (1999), O’Donnell, et al.: Pharmacol. Biochem. Behav., 63, 185 (1999)

TC-N 1752 is an orally active inhibitor of Nav1.7 channel with IC50 of 0.17 μM. TC-N 1752 shows analgesic activities.

Ralfinamide mesylate (FCE-26742A (mesylate)) is an orally available Na+ channel blocker.

Applications Pentisomide is a sodium channel blocker; derivative of disopyramide. Antiarrhythmic (class I). References Kuhlkamp, V., et al.: Int. J. Cardiol., 36, 69 (1992), Yuan, S., et al.: Cardiovasc. Drug Rev., 11, 74 (1993)

Ancistrotecine B (Compound 2), a Nav1.7 channel inhibitor (IC50: 0.73 μM), has been shown to alleviate inflammatory pain in mice [1].

5-Tridecanol blocks ion flux in sodium channels.

Applications 2,6-Dichloro-N-(2,6-dimethylphenyl)hexanamide is an impurity of the local anesthetic Levobupivacaine (B689546).

6-Iodoamiloride is a potent inhibitor of acid-sensing ion channel 1 (ASIC1), exhibiting an IC50 value of 88 nM.

Sodium ionophore III (ETH2120) is a Na+ ionophore suitable for the test of sodium activity in plasma, serum, and blood.

Ajmaline, a class Ia anti-arrhythmic, diagnoses Brugada syndrome and treats tachycardia; inhibits cardiac Kv1.5/Kv4.3 channels.

6-Benzoylheteratisine (Heteratisan-14-one, 6-(benzoyloxy)-20-ethyl-8-hydroxy-1-methoxy-4-meth) is a Aconitum alkaloid.

Nicainoprol (RU-42924) is a fast-sodium-channel blocking drug. Nicainoprol is a potent antiarrhythmic agent.

Oxybuprocaine hydrochloride (Oxybuprocaine HCl), a local anesthetic, is used especially in otolaryngology and ophthalmology.

Amitriptyline hydrochloride (Annoyltin) is the hydrochloride salt of the tricyclic dibenzocycloheptadiene amitriptyline with antidepressant and antinociceptive