Sodium Channel

Applications An anti-inflammatory and analgesic agent. Anesthetic (local). 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);

Nav1.8-IN-4 is a potent Nav1.8 channel inhibitor with potential analgesic activity.Nav1.8-IN-4 can be used for pain and neurological related disorders.

Applications N-(Methoxymethyl)-N-[(trimethylsilyl)methyl]benzenemethanamine is used in the synthesis of pyrrolidine derivatives as novel sodium channel blockers used to treat ischemic related ailments. References Seki, M. et al.: Bioorg. Med. Chem. Lett., 23, 4230 (2013);

RY785 is a potent and selective inhibitor of voltage-gated potassium channel such as KV2.2 (IC50 = 50 nM). RY785 may be used in pain relief studies.

E 0747 is an antiarrhythmic agent of class 1C type. E-0747 suppresses arrhythmia by inhibiting the Na channels of cardiac cells.

Applications Lidocaine-d6 Hydrochloride is the labeled analogue of Lidocaine Hydrochloride, 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 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),

GS967 is a potent, and selective inhibitor of cardiac late sodium current (late INa ).

Lidocaine, an amide local anesthetic, reduces pain and inflammation by dampening ICAM-1, cytokines, and neutrophil influx.

Besipirdine (HP 749 free base) is a non-receptor-dependent cholinomimetic compound with alpha-adrenergic activity and cardiovascular activity.

Olisutrigine bromide is a sodium channel blocker used as an analgesic.

Applications A potent local anesthetic that is active even in acidic conditions. It is used (usually in combination with an antacid) for the relief of pain associated with peptic ulcer disease or esophagitis. References Detrain, M. et al.: Acta. Gastro-Enterol. Belg., 28, 360 (1965); Barbezat, G.O. et al.: Scand. J. Gastroenterol., 13, 321 (1978); Masuda, Y. et al.: Biochem. Pharmacol., 64, 677 (2002);

Metaflumizone (BAS-320I) is a sodium channel blocker insecticide.

CRMP2-Ubc9-NaV1.7 inhibitor 194, is a CRMP2-Ubc9-NaV1.7 inhibitor.

Lidocaine Hydrochloride hydrate is an amide local anesthetic, has anti-inflammatory property.

Amlenetug is a humanized IgG1κ antibody targeting SNCA, with its corresponding isotype control being HumanIgG1kappa, Isotype Control.

Ropivacaine hydrochloride (Ropivacaine monohydrochloride) is the hydrochloride salt of ropivacaine, a local anesthetic of the amide type with analgesic activity

Applications Lorcainide Hydrochloride is an inhibitor of sodium voltage-gated channels. Effective anti-arrhythmic agents in patients. References Lynch, J. J., et al.: J. Pharm. Exp. Ther., 273, 554-560 (1995); Heykants, J.: Int. Congr. Symp., 49, 35-39 (1981)

Analgesic Agent-2, a selective orally active inhibitor of the NaV1.8 channel, demonstrates an IC50 of 50.18 nM in HEK293 cells that stably express the human

Applications 6-Chlorohexanoic Acid is used as the starting material in the synthesis of 2,6-Dichloro-N-(2,6-dimethylphenyl)hexanamide (D434225); an impurity of the local anesthetic Levobupivacaine (B689546). 6-Chlorohexanoic Acid is also used as a reagent in the synthesis of novel types of polyester glycodendrimers as potential inhibitors of urinary tract infections. 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 Tullar, B., et al.: J. Med. Chem., 14, 891 (1971); Schmidt, A., et al.: Pharm. Res., 22, 2121 (2005); Twibanire, J.K., et al.: New J. Chem., 39, 4115 (2015)

Ralitoline (Ralitolinum) is an anticonvulsant with anticancer activity and sodium channel blocking activity.

Ambroxol hydrochloride (Mucosolvan) is a metabolite of BROMHEXINE that stimulates mucociliary action and clears the air passages in the respiratory tract.

Applications Labelled Benzocaine (B202970). Benzocaine is used as an anesthetic (local). References Ali, S.L., et al.: Anal. Profiles Drug Subs., 12, 73 (1983),

Applications Ethyl N-Boc-piperidine-4-carboxylate is used as a reagent to synthesize 3-amino-1-(5-indanyloxy)-2-propanol derivatives as sodium channel blockers to treat stroke patients. Ethyl N-Boc-piperidine-4-carboxylate is also used as a reagent to prepare inhibitors of tumour necrosis factor alpha-converting enzyme. References Levin. J.: Heterocycles, 70, 691 (2006); Seki, M., et al.: Chem. Pharm. Bull., 60, 488 (2012)

Bupivacaine hydrochloride (Vivacaine) is a long-lasting, amide local anesthetic that blocks sodium channels, inhibiting nerve impulses and sensation.

Applications 6-(Propylamino)-2-hydroxy-N-(2,6-dimethylphenyl)-hexanamide is a derivative of Bupivacaine (B689560), a sodium channel blocker, local anesthetic. References Wilson, T.D., et al.: Anal. Profiles Drug Subs., 19, 59 (1990), McClellan, K.J., et al.: Drugs, 56, 355 (1998),

Applications Anesthetic (local). References Cederholm. I., et al.: Reg. Anesth., 19, 18 (1994), Johansson, B., et al.: Anesth. Analg., 78, 210 (1994), Oda, Y., et al.: Anesthesiology, 82, 214 (1995),

GNE-131 is a potent and specific inhibitor of human sodium channel NaV1.7 (IC50: 3 nM).

PF-04885614 is a potent inhibitor of NaV1.8, has potential for neurological and neurodevelopmental diseases treatment.

Applications Labelled 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),

GX-674 is a highly potent and selective voltage-gated sodium channel 1.7 (Nav1.7) antagonist with an IC50 value of 0.1 nM measured at -40 mV for the study of

LTGO-33 is a voltage-gated sodium channel NaV1.8 inhibitor that inhibits NaV1.8, NaV1.1-NaV1.7, and NaV1.9.

PF 04531083 is a selective blocker of the NaV1.8 channel. PF 04531083 can be used for neuropathic and inflammatory pain studies.

Applications 4,4'-Dichlorodiphenyltrichloroethane is a synthetic organochlorine insecticide. 4,4'-Dichlorodiphenyltrichloroethane functions by opening sodium ion channels in the insects’ neurons, causing them to fire spontaneously which in turn leads to death. 4,4'-Dichlorodiphenyltrichloroethane is banned for agricultural use in North America, it is still commonly used in some countries and particularly as a means of malaria control. 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 Balkew, M. et al.: Paras. Vect., 3, No pp. given (2010); Kikankie, C.K. et al.: Malaria J., 9, No pp. given. (2010); Battu, R.S. et al.: Sci. Total Environ., 78, 173 (1989);

Applications N-(Chloroacetyl)-2,5-dimethylaniline is an intermediate in the synthesis of impurities of Lidocaine (L397800), an anesthetic local agent and antiarrythmic class IB agent. References Groningsson, K., et al.: Anal. Profiles Drug Subs., 14, 207 (1985), Davies, P.S., et al.: Drugs, 64, 937 (2004),

Applications Hemin chloride is a porphyrin complex heme oxygenase-1 inducer with acts in cellular protection and control. At a concentration of 20 mM Hemin chloride demonstrated the significance of heme in myotube maturation by increasing size, number, cross-striations, and contraction frequency and strength of myotubes. The compound has been observed to induce cGMP formation through induction of guanylate cyclase. Hemin chloride has been noted to stimulate calcium-dependent K+ channels and modulate fluid transport and Na+ in the loop of henle in rat studies. Hemin has also been documented to give rise to active chloride secretion in Caco-2 cells. In cadmium injured rat testes, hemin chloride demonstrated anti-apoptotic, antiinflamatory and antioxidant properties. Through reactive oxygen species of ERK References Vanova, K. et al.: BMC Cancer., 16, 309 (2016); Wang, X. et al.: ACS App. Mat. Inter., 9, 25387 (2017);

Evenamide (NW-3509) is a sodium channel blocker. Which shows efficacy in a broad spectrum of rodent models of psychosis, mania, depression, and aggressiveness.

Stability Hygroscopic Applications Nigericin Sodium Salt is a polyether antibioitc K+ and Na+ ionophore. 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 Graven, S.N., et al.: Proc. Natl. Acad. Sci., 56, 654-8 (1966);

Tenapanor (RDX 5791), an NHE3 inhibitor, regulates sodium in the gut and kidney with a strong preclinical safety record and minimal side effects.

Applications Ethyl 3-Aminobenzoate Methanesulfonate is used as anesthetic for broodfish such as rainbow trout and red pacu. Ethyl 3-Aminobenzoate Methanesulfonate also acts as the sodium channel blocker which reverses the degenerative effects of fipronil insecticide. References Sladky, K., et al.: Am. J. Vet. Res., 62, 337 (2001); Wagner, E., et al.: Aquaculture, 211, 353 (2002); Stehr, C., et al.: Toxicol. Sci., 92, 270 (2006);

Psora 4 (5-(4-Phenylbutoxy)psoralen) is a Kv1.3 blocker and a caloric restriction mimetic.

Applications Labelled Bupivacaine (B689560). Sodium channel blocker, 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 Wilson, T.D., et al.: Anal. Profiles Drug Subs., 19, 59 (1990), McClellan, K.J., et al.: Drugs, 56, 355 (1998),

Pramocaine hydrochloride (Pramoxine HCl), a topical anesthetic, is served as an antipruritic.

PF-05089771 inhibits Nav1.7 channels (IC50: 11-33 nM), selective over Nav1.1-1.6/1.8, Ca+, K+ channels, TRPV1; 1000x affinity for half-inactivated state.