Sodium Channel

SYM2206 is a low affinity non-competitive AMPA receptor antagonist with an IC50 value of 1.6 μM.SYM2206 exhibits anticancer activity by blocking Nav1.6-mediated

Eslicarbazepine Acetate (Zebinix) is an anticonvulsant medication approved for use as an adjunctive therapy for partial-onset seizures.

Applications 3-Deoxyyunaconitine is a metabolite of Aconitine (A189875), a neurotoxin that binds, activates tetrodotoxin-sensitive Na+ channels and prolongs the opening of the sodium-ion channel by suppressing conformational changes. References Derbre, S., et al.: Anal. Bioanal. Chem., 398, 1747 (2010), Li, M., et al.: J. Pharm. Biomed. Anal., 53, 1063 (2010),

Mepivacaine hydrochloride (Mepivacaine HCl) is the hydrochloride salt form of mepivacaine, an amide derivative with local anesthetic properties.

Stability Hygroscopic Applications Antiepileptic; increases levels of GABA in the brain. References Chang, Z.L., et al.: Anal. Profiles Drug Subs., 8, 529 (1979), Nau, H., et al.: Pharmacol. Toxicol., 69, 310 (1991), Loscher, W., et al.: Prog. Neurobiol., 58, 31 (1999)

Dibucaine hydrochloride (Cinchocaine hydrochloride), a long-acting local amide anestheticsis, is usually used for surface anesthesia.

Benzocaine is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and at nerve endings.

Lamotrigine (BW430C) is an Anti-epileptic Agent and Mood Stabilizer.

Zoniporide (CP-597396) is an NHE-1 inhibitor that inhibits platelet swelling and can be used in the study of cardiovascular diseases.

Stability Light Sensitive Applications 2-Chloro-2',6'-dimethyl-d6-acetanilide is the labeled analogue of 2-Chloro-2',6'-dimethylacetanilide (C365375), an intermediate of Lidocaine (L397800), a local anesthetic; antiarrhythmic (class IB). Long-acting, membrane stabilizing agent against ventricular arrhythmia. Originally developed as a local anesthetic. References Moen, A., et al.: Biocatal. Biotransform., 23, 45 (2005); Yogeeswari, P., et al.: Bioorg. Med. Chem. Lett., 17, 3712 (2007); 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)

Applications Antiepileptic triazole derivative which decreases firing by neurons at sodium channels. Anticonvulsant. Neuroprotective & Neuroresearch Product. References Cheung, W.K., et al.: Pharm. Res., 12, 1878 (1995), Cardot, J.-M., et al.: Biopharm. Drug Dispos., 19, 259 (1998), Palhagen, S., et al.: Epilepsy Res., 43, 115 (2001),

Phenytoin sodium (Diphantoine) is an inactive stabilizer for voltage-gated sodium channel .

Levobupivacaine is an amino-amide local anaesthetic drug belonging to the family of n-alkylsubstituted pipecoloxylidide.

Olorigliflozin is a sodium glucose co-transporter (SGLT) inhibitor with antihyperglycemic properties.

NHE3-IN-1 是钠/质子交换剂 3 (NHE-3) 的抑制剂。

Trapencaine is a newly synthesized carbamate type local anesthetic that induces conformational changes in sodium channels on hypertrophic cell membranes.

Applications Labelled Rufinamide (R701552). Antiepileptic triazole derivative which decreases firing by neurons at sodium channels. Anticonvulsant. References Cheung, W.K., et al.: Pharm. Res., 12, 1878 (1995), Cardot, J.-M., et al.: Biopharm. Drug Dispos., 19, 259 (1998), Palhagen, S., et al.: Epilepsy Res., 43, 115 (2001),

Applications Labelled analogue of 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);

Flecainide is a medication used to prevent and treat abnormally fast heart rates. This includes ventricular and supraventricular tachycardias.

Applications 4,4'-Dichlorodiphenyltrichloroethane - D8 is a synthetic organochlorine insecticide. 4,4'-Dichlorodiphenyltrichloroethane - D8 functions by opening sodium ion channels in the insects’ neurons, causing them to fire spontaneously which in turn leads to death. 4,4'-Dichlorodiphenyltrichloroethane - D8 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).

Eleclazine hydrochloride (GS 6615 hydrochloride) is a novel inhibitor of late Na+ current (IC50: 0.7 uM).

AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

Applications 4-Methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiophenecarboxylic Acid is an impurity of Articaine (A777900), an amide based short-acting local anesthetic use for regional anaesthesia in day-case settings such arthroscopy, hand , food surgery and in dentistry. References Grossman, M., et al.: J. Clin. Pharmacol., 44, 1282 (2004); Oertel, R., et al.: Pharmazie., 53, 646 (1998); Vree, T.B., et al.: Brit. J. Clin. Pharmacol., 44, 29 (1997);

Brompheniramine maleate (Dimotane) is an antagonist against histamine H1 receptors.

Applications Benzocaine is used as an anesthetic (local). References Kholod, Y., et al.: Environ. Sci. Technol., 43, 9208 (2009), Fliri, A., et al.: J. Med. Chem., 52, 8038 (2009), Perez-Garrido, Alfonso; Helguera, A., et al.: J. Pharm. Sci., 98, 4557 (2009), Onoue, S., et al.: J. Pharm. Sci., 98, 3647 (2009),

Vilobelimab (CaCP-29) is a human-mouse chimeric IgG antibody targeting human complement component 5a, a C5a inhibitor that inhibits neutrophil activation.

Applications A labelled metabolite of the sodium channel blocker Propafenone (P757500). References Hege, H.G. et al.: Arzneim.-Forsch., 34, 972 (1984); Hollmann, M., et al.: Arzneim.-Forsch., 33, 763 (1983); Bryson, H. M., et al.:Drugs, 45, 85 (1993);

Applications A local anesthetic used topically in opthalmology. 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 Fliri, A., et al.: J. Med. Chem., 52, 8038 (2009), Gohil, V., et al.: Nat. Biotechnol., 28, 249 (2010),

Cariporide (HOE-642), an NHE1 inhibitor, reduces human platelet degranulation, platelet-leukocyte aggregates, and GPIIb/IIIa activation.

Ranolazine (RS 43285-003) inhibits calcium uptake, treats chronic angina by targeting sodium/calcium channels to modulate intracellular sodium.

N-Me-aminopyrimidinone9 is a sodium channel antagonist

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

Topiramate (RWJ 17021) is a unique antiseizure medication that is used in the treatment of partial and generalized seizures.

Applications Flecainide is an antiarrhythmic (class IC). References Hodess, A.B., et al.: J. Cardiovasc. Pharmacol., 1, 427 (1979), Somani, P., et al.: Clin. Pharmacol. Ther., 27, 464 (1980), Alessi-Severini, S., et al.: Anal. Profiles Drug Subs. Excip., 21, 169 (1992)

Applications Butanilicaine Hydrochloride, is a local anesthetic. References Gall, H., et al.: J. Allergy and Clinical immunology, 97, 933 (1996)

Veratridine is a benzoate-cevane found in Veratrum and Schoenocaulon. It activates sodium channels to stay open longer than normal.

PF-05661014, a demethylated analogue of PF-06526290, selectively inhibits Nav1.3 and Nav1.7 currents by stabilizing the inactivated state through interaction with the D4 VSD. This compound is utilized in research focused on sodium channel modulation.

CL-424032 is an inhibitor of sodium channels (sodium channel).

Stability Hygroscopic Applications 5,5-Diphenyl Hydantoin Sodium salt reduces incidence of grand mal seizures; appears to stabilize excitable membranes perhaps through effects on Na+, K+, and Ca2+ channels. 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 Faucette, S., et al.: J. Pharmacol. Exp. Ther., 320, 72 (2007), Guo, D., et al.: J. Biol. Chem., 282, 36766 (2007), Merrell, M., et al.: Drug Metab. Dispos., 36, 1716 (2008),

Fosphenytoin disodium (ACC-9653) is a prodrug of phenytoin that is rapidly converted to phenytoin, a voltage-gated sodium channel blocker

Rilmakalim is a potassium channel opener. Rilmakalim shows antivasoconstrictor effect.

Suzetrigine (VX-548) is an oral NaV1.8 inhibitor with analgesic properties for acute pain research.

Benzonatate (PEGn) is a unique non-narcotic cough suppressant featuring sodium channel blocking properties and anesthetic effects on respiratory tract stretch receptors.

Ranolazine 2HCl, an antianginal, treats arrhythmia by inhibiting sodium current without changing blood pressure or heart rate.

Carbamazepine: a tricyclic with anticonvulsant and analgesic effects, treats trigeminal neuralgia.

A-803467 is a selective NaV1.8 channel blocker.

Myomodulin is a neuropeptide present in molluscs, insects, and gastropods.Myomodulin is present in two identified aplysia neurons that contain myomodulin A the

(R)-Duloxetine, an isomer of Duloxetine, induces tonic and use-dependent blockade of neuronal Na+ channels. This compound is utilized in pain research.

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.