Sodium Channel

GDC-0276 is an orally active, selective, and potent NaV1.7 inhibitor that can be used for the study of pain-related diseases.

Applications 2-Butoxyquinoline-4-carboxylic Acid is used in the organic synthesis of o-(β-diethylaminoethyl)cinchoninaldoxime with local anesthetic activity References Rossi, S., et al.: Farmaco, Edizione Scientifica, 34, 486 (1979)

Propoxycaine hydrochloride is an ester local anesthetic that inhibits voltage-gated sodium channels, modulates nerve impulses, and induces loss of sensation.

Applications The N-oxide of the local anesthetic Ropivacaine (R675000).

Applications Labelled Tributyl O-Acetylcitrate (T772950). Topical pharmaceutical formulation anesthetic surfactant ester. References Cherian., et al.: Br. J. Anaesthesia, 87, 502 (2001),

Applications 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),

Mepivacaine (Carbocaine) is an amide local anesthetic, blocking sodium channels for nerve blocks and epidurals.

Applications BMS 204352 is a potassium channel opener that can be used to treat stroke. References Jensen, S. B.: CNS Drug. Rev. 8, 353 (2002); Gribkoff, V. K., et al.: Nat Med 7, 471 (2001)

Funapide (TV 45070) is a potent Nav1.7 inhibitor, potentially treating inflammation and various pains.

Licarbazepine (10,11-hydroxy-10,11 Dihydrocarbamezer) is the pharmacologically active metabolite of oxcarbazepine, a drug indicated for the treatment of partial

Applications Sodium channel blocker. Diuretic. References Paterson, J., et al.: Br. Med. J., 1, 422 (1968), Khan, K., et al.: J. Pharm. Pharmacol., 27, 48 (1975), Frank, S., et al.: J. Pharm. Sci., 64, 1585 (1975), Vidt, D., et al.: Pharmacotherapy, 1, 179 (1981),

Indazole, a heterocyclic compound, offers diverse biological activities.

Metergoline (Methergoline) is a dopamine agonist and serotonin antagonist.

Diphenidol hydrochloride (Difenidol hydrochloride), a muscarinic antagonist, is employed as an anti-vertigo and as an antiemetic drug.

Stability Hygroscopic Applications Labelled Ropivacaine (R675000). 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),

NaV1.2/1.6 channel blocker-1 is a NaV1.2/1.6 channel blocker that inhibits rNaV1.6 and can be used to study generalised epilepsy and movement disorders.

Oxcarbazepine (GP 47680), an anti-epileptic, reduces CNS disorganized electrical activity.

ProTx-II TFA is a potent and highly selective Nav1.7 sodium channel blocker, exhibiting an IC50 of 0.3 nM and demonstrating at least 100-fold selectivity over

BI-9627 is an inhibitor of sodium-hydrogen exchanger isoform 1 (NHE1) (EC50: 31 nM).

VGSCs-IN-1, a VGSC inhibitor and Riluzole analog, exhibits good blocking activity on Nav1.4 and can be used to study cellular excitability disorders.

Impurity Lidocaine EP impurity J Applications 2-(Diethylamino)-N-(2,5-dimethylphenyl)acetamide Hydrochloride is an impurity in the synthesis of Lidocaine Hydrochloride (L397800), an anesthetic local agent and antiarrythmic class IB 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 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),

Halazone (Pantocid) is fine white powder with an odor of chlorine. It has been widely used to disinfect drinking water.

Applications Anesthetic (topical). References Olson, L., et al.: J. Imaging Sci. Technol., 51, 217 (2007),

Applications 4-Methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiophenecarboxylic Acid-d7 is the labelled form of 4-Methyl-3-[[1-oxo-2-(propylamino)propyl]amino]-2-thiophenecarboxylic Acid (M326815). 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)

(Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of AMG8379 which is an orally active and selective sulfonamide NaV1.7 antagonist.

Impurity Ropivacaine EP Impurity H Applications 2,6-Dimethylaniline Hydrochloride (Ropivacaine EP Impurity H) is chemical reagent frequently used in the synthesis of pharmaceutical compounds. Impurity of Ropivacaine (R675000), anesthetic (local). References Li, H. et al.: J. Polym. Sci. A. Poly. Chem., 44, 2665 (2006); 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); Lv, C. et al.: Chem. A Eur. J., 19, 1174 (2013);

Applications Antiarrhythmic (class IB). References Singh, E.M., et al.: Br. J. Pharmacol., 44, 1 (1972); Scott, K.N., et al.: Drug Metab. Dispos., 1, 506 (1973); Chew, C.Y.C., et al.: Drugs, 17, 161 (1979); Abounassif, M.A., et al.: Anal. Profiles Drug Subs., 20, 433 (1991);

BI 01383298 is a selective inhibitor of the sodium-citrate co-transporter (SLC13A5).

Applications The N-oxide derivative of the local anesthetic Mepivacaine (M225060).

Elpetrigine (GW273293) is a potential sodium channel blocker with antiepileptic activity that can be used to study epilepsy.

3- Deoxyaconitine is a derivative of Aconitine (A189875), which activates tetrodotoxin-sensitive Na+ channels, inducing presynaptic depolarization, thus

Applications 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);

Riluzole (RP-54274) is an anticonvulsant, glutamate antagonist, and prolongs ALS patient survival.

Impurity Lidocaine EP Impurity D (HCl) Applications Nor Lidocaine Hydrochloride is a hydrochloride salt metabolite of Lidocaine (L397800), an 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 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);

Permethrin (NRDC-143) is a pyrethroid insecticide commonly used in the treatment of LICE INFESTATIONS and SCABIES.

Nav1.3 Channel Inhibitor 1 (Compound 15b) is a state-dependent inhibitor of the voltage-gated sodium channel Na v 1.3, with an IC50 value of 20 nM.

Applications N-Formyl Benzocaine is a degradation product of Benzocaine (B202970); a compound that 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); Helguera, A., et al.: J. Pharm. Sci., 98, 4557 (2009); Onoue, S., et al.: J. Pharm. Sci., 98, 3647 (2009); Koellmer, M., et al.: AAPS PharmSciTech., 14, 1333 (2013)

Tocainide is a blocker of the sodium channel and used for the treatment of tinnitus.

PF-01247324 is a selective and orally bioavailable Nav1.8 channel blocker (IC50: 196 nM).

Applications N-(4-Bromo-2,6-dimethylphenyl)-2-chloroacetamide is a useful synthetic intermediate in the synthesis of 4-Hydroxylidocaine (H943825); a metabolite of Lidocaine (L397800) which is 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)

Benzocaine shares a common receptor with all othe rLAs in the voltage-gated Na+ channel(IC50 of 0.8 mM tested with a potential of +30 mV).

Nav1.7 inhibitor is a Nav1.7 inhibitor for research in the field of pain and anesthesia.

PF-05186462 (PF-05150122) is a potent, state-dependent, subtype selective Nav1.7 inhibitor with IC50 of 21 nM, no significant activity against Nav1.5.

Applications 5-Hydroxy Propafenone Hydrochloride-d5 is a labeled analogue of 5-Hydroxy Propafenone Hydrochloride (H952450), a metabolite of Propafenone (P757500), a sodium channel blocker. Antiarrhythmic (class IC). References Hege, H.G., et al.: Eur. J. Drug Metab. Pharmacokinet., 9, 41 (1984); 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)

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

solpecainol is a sodium channel blocker used in the study of neurological and cardiovascular diseases.

E 0747 FA is an antiarrhythmic compound that inhibits the voltage of action potential Vmax in Purkinje fibers of porcine heart.E 0747 FA inhibits Na channels in cardiac cells.

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),