Sodium Channel

Applications Deacetamide Acetonitrile-pentisomide is an intermediate in the synthesis of Pentisomide (P275600). 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)

Stability Moisture Sensitive Applications Mesaconine is an Aconine (A190245) derivative, which is an Aconitine (A189875), a neurotoxin which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction. 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 Derbre, S., et al.: Anal. Bioanal. Chem., 398, 1747 (2010), Li, M., et al.: J. Pharm. Biomed. Anal., 53, 1063 (2010),

Applications Neurotoxin. Activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction. Aconitine also blocks norepinephrine reuptake. In the heart, aconitine induces ventricular tachycardia after intracoronary injection. In cultured ventricular myocytes, aconitine increases the duration of the action potential and induces the appearance of early after depolarization.Used in producing heart arrhythmia in experimental animals. 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 Derbre, S., et al.: Anal. Bioanal. Chem., 398, 1747 (2010), Li, M., et al.: J. Pharm. Biomed. Anal., 53, 1063 (2010),

Applications Yunnaconitine 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. Yunnaconitine is a deiterpene alkaloid, known to exhibit cytotoxic activity in human leukemic cell. 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 He, Y.Q., et al.: J. Pharma. Analysis., 1, 57 (2011); Derbre, S., et al.: Anal. Bioanal. Chem., 398, 1747 (2010); Li, M., et al.: J. Pharm. Biomed. Anal., 53, 1063 (2010);

Applications Bupivacaine is a 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),

AZD 7009 is a novel antiarrhythmic compound that inhibits the sodium current of hNav1.5 in CHO K1 cells with an IC50 of 11 uM.

EIPA (L593754) is a TRPP3 channel inhibitor and an inhibitor of Na+/H+ exchange (NHE). EIPA inhibits megacytosis, promotes autophagy. Cost-effective and quality-assured.

Butamben (Butyl 4-aminobenzoate) is a long-duration local anesthetic used for the treatment of chronic pain.

Applications Isotope labelled 4,4'-Dichlorodiphenyltrichloroethane 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);

Sodium Channel inhibitor 2 is a blocker of sodium channel.

Impurity Lidocaine EP impurity I Applications 2-(Diethylamino)-N-(2,4-dimethylphenyl)acetamide is a Lidocaine (L397800) derivative with reduced local anesthetic action. 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 Costa, J.C.S., et al.: Bioorg. Med. Chem. Lett., 18, 1162 (2008); Magee, P.S., et al.: J. Org. Chem., 19, 168 (1954);

Vormatrigine effectively inhibits sodium channels (sodium channel).

Benzocaine hydrochloride (Ethyl 4-aminobenzoate hydrochloride) is a surface anesthetic that acts by preventing transmission of impulses along nerve fibers and

BIIB 722 Mesylate is a sodium-hydrogen exchange inhibitor with cardioprotective properties and can be used to study myocardial ischemia.

Tolperisone hydrochloride (Muscalm) is a muscle relaxant for treating muscle tone disorders from neurological diseases.

Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction through inhibiting sodium ion influx reversibly.

Cyfluthrin binds to voltage-sensitive sodium channel such as Nav 1.8 sodium channel and modify their gating kinetics, thereby disrupting nerve function of pests

Applications 4-Hydroxylidocaine, is a metabolite of Lidocaine (L397800), a common local anesthetic and antiarrhythmic drug. 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),

Primidone (NCI-C56360) is a potent anticonvulsant agent.

PF 05089771 is a Selective inhibitor of Nav1.7 (IC50 = 11 nM) that interacts with the voltage-sensor domain of domain IV.

λ-Cyhalothrin (Icon) is a type II synthetic pyrethroid insecticide featuring a high-efficiency, broad-spectrum formula with an α-cyano group.

Applications 4-Descarboxamido Rufinamide 4-Methyl Ester is an impurity in the synthesis of Rufinamide (R701550), an 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 3-(2-Chloropropionyl)amino-4-methyl-2-methoxycarbonylthiophene is an intermediate in the synthesis of Articaine-d7 Hydrochloride which is the labelled form of Articaine Hydrochloride (A777905). Articaine Hydrochloride is the Hydrochloride Salt of Articaine (A777900). Articaine is an amide based short-acting local anesthetic use for regional anaesthesia in day-case settings such arthroscopy, hand, food surgery and in dentistry. References Malamed, S.F., et al.: J. Am. Dent. Assoc., 132, 177 (2001); Luan, F., et al.: Bioorg. Med. Chem., 21, 1870 (2013)

Impurity Ripovacaine EP Impurity C Applications (S)-(+)-Mepivacaine Hydrochloride (Ripovacaine EP Impurity C) is an optical isomer of the local anesthetic Mepivacaine (M225060) that is slightly less active than its (-)-isomer. 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 Luduena, F.P. et al.: Arch. Int. Pharmacodyn. Ther., 200, 359 (1972); Jeske, A.H. et al.: Meth. Find. Exp. Clin. Pharmacol., 3, 33 (1981);

Orphenadrine is a noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist that inhibits clonal HERG channels in a concentration-dependent manner,

GX-585 is a novel potent inhibitor of NaV1.7 and highly selective against NaV1.5, having limited selectivity against NaV1.1 and NaV1.2.

Benzamil blocks ENaC, inhibiting sodium transport (IC50=4 nM) and binds with Kd=5 nM to bovine kidney membranes.

(+)-Kavain ((R)-KAWAIN) is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.

Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a reversible neuronal sodium channel inhibitor, used as a long-acting local anesthetic.

Applications Used in the preparation of bicycloamine derivatives as sodium channel inhibitors for treatment of pain, epilepsy and insomnia.

DSP-2230 is a selective blocker of Nav1.7/Nav1.8.

Triamterene is a barosensitive epithelial sodium channel (ENaC) blocker with a diuretic effect. It can also act as an inhibitor of the TGR5 receptor, reducing GLP-1 secretion and cAMP level increases induced by TGR5 activation in a dose-dependent manner.

Ethacizine hydrochloride (NIK-244) has antiarrhythmic activity and can be used to study arrhythmias and myocardial infarction.

Stability Hygroscopic Applications The N-Glucoside of Benzocaine (B202970) with anesthetic activity. A potential sun-screening agent. References Rybczynska, B. et al.: Parfum. Kosm., 48, 125 (1967); Nikolin, A. et al.: Glas. Hemi. Tehnol. Bosne Herceg., 16, 93 (1968);

Rimeporide (EMD-87580) (EMD-87580) is a potent and selective Sodium hydrogen exchange 1 (NHE-1) inhibitor.

Zoniporide hydrochloride: selective NHE-1 inhibitor, IC50 14 nM, >150x selectivity over other NHEs, inhibits platelet swelling (IC50 59 nM).

Dyclonine hydrochloride (Dyclonine HCl) , an over the counter throat lozenge, is found in Sucretswith local anesthetic effect .

Applications 2-Diisopropylaminoethyl Chloride Hydrochloride-d14 is an intermediate in synthesizing Disopyramide-d14 Tosylate Salt (D493452). Antiarrhythmic (class IA). Sodium channel blocker. References Adelstein, et al.: J. Med. Chem., 16, 309 (1973); Czeisler, J.L., et al.: J. Pharm. Sci., 74, 750 (1985); Taylor, E.H., et al.: Ann. Clin. Lab. Sci., 16, 289 (1986);

Dronedarone (SR 33589) is an amiodarone analogue which has an effective and promising treatment for Atrial fibrillation.

Applications 3-​Deoxyaconitine is a derivative of Aconitine (A189875), which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus blocking the nerve action potential which, in turn, blocks the release of neurotransmitters and decreases the end plate potential at the neuromuscular junction. 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 Derbre, S., et al.: Anal. Bioanal. Chem., 398, 1747 (2010), Li, M., et al.: J. Pharm. Biomed. Anal., 53, 1063 (2010),

Bupivacaine (AH-250) is a NMDA receptor inhibitor.Bupivacaine can block sodium, L-calcium, and potassium channels.Bupivacaine potently blocks SCN5A channels

Halofuginone specifically inhibits collagen type I and MMP-2 gene expression, which may result in the suppression of angiogenesis and tumor cell growth.

Phenytoin: a non-sedative hydantoin, antiepileptic with anticonvulsant effects, stabilizes neurons, prevents seizure spread, and relaxes muscles.

Aneratrigine hydrochloride is a Nav 1.9 blocker that may be used to prevent or treat sodium channel blocker-related disorders.

Ralfinamide (Priralfinamide) is an orally available Na-channel blocker for the treatment of neuropathic pain and other pain conditions.

Dimethyl lithospermate B (dmLSB) is a selective Na+ channel agonist.