Sodium Channel

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),

Nisoxetine hydrochloride is a noradrenaline transporter (NET) inhibitor

Sodium Channel Inhibitor 4 is a compound that functions as a sodium channel inhibitor [1].

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),

Pilsicainide HCl (SUN 1165) is a pure sodium channel blocker

Mebeverine hydrochloride (Colofac Hydrochloride), a β-phenylethylamine derivative, is a potent α1 repector inhibitor, relaxing the muscles in and around the gut

SLC13A5-IN-1 is a selective inhibitor of sodium-citrate co-transporter (SLC13A5),completely blocks the uptake of 14C-citrate(IC50 : 0.022 μM in HepG2 cells).

VX-150 is a highly selective NaV1.8 inhibitor relative to the other sodium channel subtypes (>400-fold).

Meticrane (Arresten) is a sulphonamide-derivative with thiazide-like diuretic activity.

PF-06869206 is an oral selective inhibitor of the sodium-phosphate cotransporter NaPi2a (SLC34A1, IC50: 380 nM).

Applications 4,4'-DDE - d8 is a metabolite of DDT - d8 (D434197), a synthetic organochlorine insecticide that functions by opening sodium ion channels in the insects’ neurons, causing them to fire spontaneously which in turn leads to death. 4,4'-DDE - d8 has shown to have endocrine disrupting effects on gonadotropin hormones in pituitary gonadotrope cells. References Saschenbrecker, P.W.: Can. J. Comp. Med., 37, 203 (1973); 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); Zhou, J., et. al.: Environ. Toxicol. Phar., 37, 1194 (2014)

Applications Used as a local anesthetic. References Chawla, H.P.S., et al.: J. Med. Chem., 13, 3, 480 (1970)

Dibucaine (Cinchocaine), a local anesthetic of the amide type, is now usually used for surface anesthesia.

Applications 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. Neuroprotective & Neuroresearch Product. 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),

Applications 3-Hydroxy-4-phenylbenzoic Acid is a useful reagent for the preparation of spiro[3,4-dihydro-2H-pyrrolo[1,2-a]pyrazine-1,4'-piperidine] derivatives as modulators of sodium ion channel. References Hadida Ruah, S. S., et al.: U.S. Pat. Appl. Publ. (2012), US 20120196869 A1

Tocainide hydrochloride (2-amino-n-(2,6-dimethylphenyl)propanamide hydrochloride) is a sodium channel blocker.

Propafenone: a drug for ventricular arrhythmias with mild beta-blocker activity, prolongs refractory period, and reduces heart automaticity.

GX 201 is a selective NaV1.7 inhibitor, IC50 of < 3.2 nM for hNaV1.7.

Stability Hygroscopic Applications A centrally-acting cough suppressant. It has local anesthetic and antihistamine properties, and may have anticholinergic effects at high doses. References Yuizono, T., et al.: Yakugaku Zasshi, 87, 915 (1967), Nomura, A., et al.: Oyo Yakuri, 8, 119 (1974),

Flunarizine dihydrochloride: a calcium blocker also targeting calmodulin and histamine H1, used for migraine, vertigo, vascular disease, and epilepsy aid.

Flecainide acetate (R-818) is a class Ic antiarrhythmic agent used to prevent and treat tachyarrhythmias (abnormal fast rhythms of the heart).

Orphenadrine hydrochloride (Mephenamin) is a muscarinic antagonist used to treat drug-induced parkinsonism and to relieve pain from muscle spasm.

Aneratrigine is a blocker of the sodium channel protein type 9 subunit alpha, utilized in research on neuropathic pain diseases [1].

Amiloride hydrochloride (Amiloride HCl) 是上皮钠通道和尿激酶型纤溶酶原激活物受体的抑制剂,也是 polycystin-2通道阻断剂。

Applications 1,2,4-oxadiazol-3-amine (cas# 39512-64-6) is a useful research chemical.

Transcainide (R 54718), an oral lidocaine-like antiarrhythmic, blocks BTX-activated Na+ channels in heart/muscle.

Articaine hydrochloride (Hoe-045) is a thiophene-containing local anesthetic pharmacologically similar to MEPIVACAINE.

Nav1.7-IN-18 (Compound 31) is a Nav1.7 inhibitor with a Ki value of 4.9 nM and an IC50 of 13 nM, demonstrating analgesic effects in transgenic mice with inherited erythromelalgia (IEM).

PF-04856264 is a Nav1.7 blocker.,modulates intracellular Ca 2+ signaling and chondrocyte secretome, raises the threshold of mechanical pain analgesic.

Applications 2,2’-Iminobis(N-(2,6-Dimethylphenyl)acetiamide is an impurity in the synthesis of Lidocaine Hydrochloride (L397800), an anesthetic local agent and antiarrythmic class IB agent. 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),

DPI 201-106: cardioselective h1 Na channel inhibitor, enhances heart contraction, blocks potassium and calcium currents.

N-Depropylpropafenone, an active metabolite of Propafenone, is produced through the metabolism by the CYP450 enzyme system (primarily CYP2D6). It functions by blocking sodium ion channels, thereby delaying the depolarization process in myocardial cells and exhibiting antiarrhythmic properties.

Applications Propoxycaine is used as a local anaesthetic, an analogue of Procaine (P755150), a local anesthetic of the amino ester group that is primarily used as a topical anesthetic. Procaine is also used to control the pain of intramuscular injection of penicillin as well as in dentistry. References Kania, B.H. et al.: Pol. J. Vet. Sci., 6, 279 (2003); Jussi, L. et al.: Cont. Derm., 60, 150 (2009); Gangarosa, L.P. Sr.: J. Dent. Res., 60, 1471 (1981); Torrens, F. et al.: Int. J. Mol. Sci., 7, 12 (2006);

Indenebart is a humanized IgG1λ2 monoclonal antibody targeting SNCA, with HumanIgG1lambda2, Isotype Control serving as the corresponding isotype control.

Applications Articaine-d7 Hydrochloride 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)

Methocarbamol (AHR 85) is a centrally acting muscle relaxant whose mode of action has not been established.

Bulleyaconitine A, an analgesic and antiinflammatory drug isolated from Aconitum plants, has several potential targets, such as voltage-gated Na+ channels.

ETD001 is a long-acting ENaC inhibitor with an IC50 value of 57.5 nM in HBE cells. It is applicable for research in cystic fibrosis.

Co 102862 is a voltage-gated sodium channel blocker. Co 102862 can be used for anticonvulsant studies.

Zilvetrigine is a sodium channel (sodium channel) blocker. It can be used as an analgesic.

Mexiletine hydrochloride is a lidocaine-like antiarrhythmic (Class IB) and anesthetic, stabilizing heartbeats by inhibiting sodium in cardiac cells.

Applications Anesthetic (local). References Padmanabhan, G.R., et al.: Anal. Profiles Drug Subs., 12, 105 (1983), Curto, E., et al.: Biochem. Pharmacol., 57, 663 (1999), Hall, A., et al.: Pigment Cell Res., 18, 122 (2005), Yamaguchi, Y., et al.: J. Biol. Chem., 282, 27557 (2007),

Applications Ralfinamide mesylate is a mixed sodium and N-type calcium channel protein inhibitor. Inhibitory activity of Ralfinamide mesylate is voltage dependent, with higher potency towards inactivated channels. Ralfinamide mesylate is useful in preventing, alleviating and curing a wide range of pathologies, including pain, migraine, peripheral diseases, cardiovascular diseases, inflammatory processes affecting all body systems, disorders affecting skin and related tissues, disorders of the respiratory system, disorders of the immune and endocrinol. systems, gastrointestinal, urogenital, metabolic and seizure disorders. References Bayes, M., et al.: Methods. Find. Exp. Clin. Pharmacol., 27, 411 (2005); Pevarello, P., et al.: J. Med. Chem., 41, 579 (1998); Bauer, M., et al.: Pharmacol., 85, 297 (2010);

DS-1971a is a highly potent and selective NaV1.7 inhibitor. DS-1971a exhibits a favorable toxicological profile and analgesic effects.

Applications Veratridine is a voltage dependent Na+ channel opening agent. Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package

QX-222 chloride (Lidocaine N-Methyl Hydrochloride) is a sodium channel blocker.

Raxatrigine (CNV 1014802) has been investigated for the treatment of Bipolar Disorder and Bipolar Depression.

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.