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Sodium Channel Na Channels;Na+ Channels

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Sodium Channel Na channels;Na+ channels Sodium channels are integral membrane proteins that form ion channels, conducting sodium ions (Na +) through a cell's plasma membrane. They are classified according to the trigger that opens the channel for such ions, i.e. either a voltage-change (Voltage-gated, voltage-sensitive, or voltage-dependent sodium channel also called VGSCs or Nav channel) or a binding of a substance (a ligand) to the channel (ligand-gated sodium channels). In excitable cells such as neurons, myocytes, and certain types of glia, sodium channels are responsible for the rising phase of action potentials. Voltage-gated Na+ channels can exist in any of three distinct states: deactivated (closed), activated (open), or inactivated (closed). Ligand-gated sodium channels are activated by binding of a ligand instead of a change in membrane potential. www.MedChemExpress.com 1 Sodium Channel Inhibitors & Modulators (+)-Kavain (-)-Sparteine sulfate pentahydrate Cat. No.: HY-B1671 ((-)-Lupinidine (sulfate pentahydrate)) Cat. No.: HY-B1304 Bioactivity: (+)-Kavain, a main kavalactone extracted from Piper Bioactivity: (-)-Sparteine sulfate pentahydrate ((-)-Lupinidine sulfate methysticum, has anticonvulsive properties, attenuating pentahydrate) is a class 1a antiarrhythmic agent and a sodium vascular smooth muscle contraction through interactions with channel blocker. It is an alkaloid, can chelate the bivalents voltage-dependent Na + and Ca 2+ channels [1]. (+)-Kav… calcium and magnesium. Purity: 99.98% Purity: 98.0% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 50 mg A-803467 Ajmaline Cat. No.: HY-11079 (Cardiorythmine; (+)-Ajmaline) Cat. No.: HY-B1167 Bioactivity: A 803467 is a selective Nav1.8 sodium channel blocker with an Bioactivity: Ajmaline is an alkaloid that is class Ia antiarrhythmic agent. IC50 of 8 nM; over 100-fold more selective vs. human Nav1.2, 1.3, 1.5 and 1.7. Purity: 97.51% Purity: 99.31% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 10 mg, 50 mg 50 mg, 100 mg AM-2099 Amiloride Cat. No.: HY-100727 (MK-870) Cat. No.: HY-B0285 Bioactivity: AM-2099 is a potent and selective inhibitor of voltage-gated Bioactivity: Amiloride is a relatively selective inhibitor of the sodium channel Nav1.7 with an IC50 of 0.16 μM for human epithelial sodium channel (ENaC), used in the management Nav1.7. of hypertension and congestive heart failure. Purity: 98.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 100 mg 2 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Amiloride hydrochloride Amiloride hydrochloride dihydrate (MK-870 hydrochloride) Cat. No.: HY-B0285A (MK-870 hydrochloride dihydrate) Cat. No.: HY-B0285B Bioactivity: Amiloride hydrochloride (MK-870 hydrochloride) is an epithelial Bioactivity: Amiloride hydrochloride dihydrate is an inhibitor of both sodium channel (ENaC) inhibitor and a competitive inhibitor Epithelial sodium channel ( ENaC) and urokinase-type of Urokinase-type plasminogen activator ( uPA). plasminogen activator receptor ( uTPA). Purity: 98.0% Purity: 98.56% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 100 mg Amitriptyline hydrochloride Benzamil hydrochloride Cat. No.: HY-B0527A (Benzylamiloride hydrochloride) Cat. No.: HY-B1546A Bioactivity: Amitriptyline Hydrochloride is a Bioactivity: Benzamil hydrochloride is a specific blocker of sodium dibenzocycloheptene-derivative tricyclic antidepressant (TCA). channel ( ENaC). Purity: 99.64% Purity: 99.46% Clinical Data: Launched Clinical Data: Launched Size: 10mM x 1mL in Water, Size: 10mM x 1mL in DMSO, 1 g, 5 g 5 mg, 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] Benzocaine BI 01383298 Cat. No.: HY-Y0258 Cat. No.: HY-124738 Bioactivity: Benzocaine shares a common receptor with all other local Bioactivity: BI 01383298 is a potent inhibitor of the sodium-citrate anesthetics (LAs) in the voltage-gated Na+ channel, with an co-transporter (SLC13A5) that is highly expressed in the liver [1]. IC50 of 0.8 mM tested with a potential of +30 mV. Purity: 99.98% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 mg, 10 mg, 25 mg, 50 mg, 100 mg BI-9627 Bulleyaconitine A Cat. No.: HY-18071 Cat. No.: HY-N0239 Bioactivity: BI-9627 is a sodium−hydrogen exchanger isoform 1 (NHE1) Bioactivity: Bulleyaconitine A is an analgesic and antiinflammatory drug [1] isolated from Aconitum plants; has several potential targets, inhibitor with an EC50 of 31 nM . including voltage-gated Na+ channels. Purity: 99.0% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10 mg, 50 mg 5 mg Carbamazepine Cariporide (CBZ; NSC 169864) Cat. No.: HY-B0246 (HOE-642) Cat. No.: HY-19693 Bioactivity: Carbamazepine, a sodium channel blocker, is an anticonvulsant Bioactivity: Cariporide (HOE-642) is a selective Na+/H+ exchange drug. Target: Sodium channel Carbamazepine inhibits the inhibitor. binding of [3H]batrachotoxinin A 20-α-benzoate (BTX-B) to a receptor site of voltage-sensitive sodium channel with IC50 of 131 μM, to decrease the activation of sodium channel ion flux… Purity: 99.35% Purity: 98.57% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 100 mg, 500 mg 5 mg, 10 mg, 50 mg, 100 mg Chlorpromazine D6 hydrochloride Chlorpromazine hydrochloride Cat. No.: HY-B0407AS Cat. No.: HY-B0407A Bioactivity: Chlorpromazine D6 hydrochloride is the deuterium labeled Bioactivity: Chlorpromazine Hydrochloride is an antagonist of the Chlorpromazine. Chlorpromazine is an inhibitor of dopamine dopamine D2, 5HT2A, potassium channel and sodium receptor, 5-HT receptor, potassium channel, sodium channel. channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively. Purity: 99.0% Purity: 99.83% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 1 g, 5 g 1 mg, 5 mg, 10 mg Dibucaine Dibucaine hydrochloride (Cinchocaine) Cat. No.: HY-B0552 (Cinchocaine hydrochloride) Cat. No.: HY-B0552A Bioactivity: Dibucaine is a local anesthetic of the amide type now Bioactivity: Dibucaine Hydrochloride is a local anesthetic of the amide generally used for surface anesthesia. type now generally used for surface anesthesia. Purity: 99.81% Purity: 99.67% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 g, 10 g www.MedChemExpress.com 3 Dyclonine hydrochloride EIPA (Dyclocaine hydrochloride) Cat. No.: HY-B0364A (L593754; MH 12-43; Ethylisopropylamiloride) Cat. No.: HY-101840 Bioactivity: Dyclonine is an oral anaesthetic found in Sucrets, an over the Bioactivity: EIPA is a TRPP3 channel inhibitor with an IC50 of 10.5 μM. counter throat lozenge. EIPA also inhibits Na+/H+-exchanger ( NHE) and macropinocytosis. Purity: 99.72% Purity: 99.73% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 g, 10 g 5 mg, 10 mg EIPA hydrochloride (L593754 hydrochloride; MH 12-43 Eleclazine hydrochloride hydrochloride; Ethylisopropylamiloride hydrochloride) Cat. No.: HY-101840A (GS 6615 hydrochloride) Cat. No.: HY-16738A Bioactivity: EIPA hydrochloride (L593754 hydrochloride) is a TRPP3 channel Bioactivity: Eleclazine hydrochloride is a novel late Na+ current inhibitor [1] with IC50 value of 0.7 uM. target: Na+ current. IC50: 0.7 uM. inhibitor with an IC50 of 10.5 μM . EIPA also inhibits In vitro: Eleclazine hydrochloride inhibits ATX-II enhanced + + [2] [3] Na /H -exchanger ( NHE) and macropinocytosis . late INa in ventricular myocytes, shorten the ATX-II induced prolongation of APD, MAPD, QT interval, and decreased… Purity: >98% Purity: 99.47% Clinical Data: No Development Reported Clinical Data: Phase 3 Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg 1 mg, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Eniporide hydrochloride Eslicarbazepine acetate (EMD-96785 hydrochloride) Cat. No.: HY-106150B (BIA 2-093) Cat. No.: HY-B0703 Bioactivity: Eniporide hydrochloride (EMD-96785 hydrochloride) is a potent Bioactivity: Eslicarbazepine acetate, an antiepileptic drug, is a dual a Na+/H+ exchange inhibitor. dual Inhibitor of β-Secretase and voltage-gated sodium channel. Purity: 99.31% Purity: 99.98% Clinical Data: No Development Reported Clinical Data: Launched Size: 10mM x 1mL in DMSO, Size: 10mM x 1mL in DMSO, 5 mg, 10 mg, 25 mg, 50 mg 10 mg, 50 mg, 100 mg, 500 mg Flecainide acetate FR183998 free base (R-818) Cat. No.: HY-17429 Cat. No.: HY-100302 Bioactivity: Flecainide acetate (R-818) is a class 1C antiarrhythmic drug Bioactivity: FR183998 free base is a potent Na+/H+-exchange inhibitor, especially used for the management of supraventricular with IC50s of 0.3 nM, 3.1 nM and 6.5 nM by measurement of pH i arrhythmia; works by blocking the Nav1.5 sodium channel in the change in rat lymphocytes, rat and human platelets, heart, causing prolongation of the cardiac action potential. respectively. Purity: 99.65% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10mM x 1mL in Water, Size: 1 mg, 5 mg, 10 mg 10 mg, 50 mg, 100 mg Funapide Ginsenoside Rg3 (TV 45070; XEN402) Cat. No.: HY-16723 (20(S)-Ginsenoside-Rg3; Rg3; S-Ginsenoside Rg3) Cat. No.: HY-N0603 Bioactivity: Funapide (TV 45070; XEN402) is a potent Sodium Channel Bioactivity: Ginsenoside Rg3 is the main component of Red ginseng. Nav1.7 inhibitor. Ginsenoside Rg3 inhibits Na+ and hKv1.4 channel with IC 50s of 32.2±4.5 and 32.6±2.2 μM, respectively.
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    1 abietic acid R abrasive silica for polishing DR acenaphthene M (LC) acenaphthene quinone R acenaphthylene R acetal (see 1,1-diethoxyethane) acetaldehyde M (FC) acetaldehyde-d (CH3CDO) R acetaldehyde dimethyl acetal CH acetaldoxime R acetamide M (LC) acetamidinium chloride R acetamidoacrylic acid 2- NB acetamidobenzaldehyde p- R acetamidobenzenesulfonyl chloride 4- R acetamidodeoxythioglucopyranose triacetate 2- -2- -1- -β-D- 3,4,6- AB acetamidomethylthiazole 2- -4- PB acetanilide M (LC) acetazolamide R acetdimethylamide see dimethylacetamide, N,N- acethydrazide R acetic acid M (solv) acetic anhydride M (FC) acetmethylamide see methylacetamide, N- acetoacetamide R acetoacetanilide R acetoacetic acid, lithium salt R acetobromoglucose -α-D- NB acetohydroxamic acid R acetoin R acetol (hydroxyacetone) R acetonaphthalide (α)R acetone M (solv) acetone ,A.R. M (solv) acetone-d6 RM acetone cyanohydrin R acetonedicarboxylic acid ,dimethyl ester R acetonedicarboxylic acid -1,3- R acetone dimethyl acetal see dimethoxypropane 2,2- acetonitrile M (solv) acetonitrile-d3 RM acetonylacetone see hexanedione 2,5- acetonylbenzylhydroxycoumarin (3-(α- -4- R acetophenone M (LC) acetophenone oxime R acetophenone trimethylsilyl enol ether see phenyltrimethylsilyl... acetoxyacetone (oxopropyl acetate 2-) R acetoxybenzoic acid 4- DS acetoxynaphthoic acid 6- -2- R 2 acetylacetaldehyde dimethylacetal R acetylacetone (pentanedione -2,4-) M (C) acetylbenzonitrile p- R acetylbiphenyl 4- see phenylacetophenone, p- acetyl bromide M (FC) acetylbromothiophene 2- -5-
  • 8–16–01 Vol. 66 No. 159 Thursday Aug. 16, 2001 Pages 42929

    8–16–01 Vol. 66 No. 159 Thursday Aug. 16, 2001 Pages 42929

    8–16–01 Thursday Vol. 66 No. 159 Aug. 16, 2001 Pages 42929–43064 VerDate 11-MAY-2000 19:13 Aug 15, 2001 Jkt 194001 PO 00000 Frm 00001 Fmt 4710 Sfmt 4710 E:\FR\FM\16AUWS.LOC pfrm11 PsN: 16AUWS 1 II Federal Register / Vol. 66, No. 159 / Thursday, August 16, 2001 The FEDERAL REGISTER is published daily, Monday through SUBSCRIPTIONS AND COPIES Friday, except official holidays, by the Office of the Federal Register, National Archives and Records Administration, PUBLIC Washington, DC 20408, under the Federal Register Act (44 U.S.C. Subscriptions: Ch. 15) and the regulations of the Administrative Committee of Paper or fiche 202–512–1800 the Federal Register (1 CFR Ch. I). The Superintendent of Assistance with public subscriptions 512–1806 Documents, U.S. Government Printing Office, Washington, DC 20402 is the exclusive distributor of the official edition. General online information 202–512–1530; 1–888–293–6498 Single copies/back copies: The Federal Register provides a uniform system for making available to the public regulations and legal notices issued by Paper or fiche 512–1800 Federal agencies. These include Presidential proclamations and Assistance with public single copies 512–1803 Executive Orders, Federal agency documents having general FEDERAL AGENCIES applicability and legal effect, documents required to be published Subscriptions: by act of Congress, and other Federal agency documents of public interest. Paper or fiche 523–5243 Assistance with Federal agency subscriptions 523–5243 Documents are on file for public inspection in the Office of the Federal Register the day before they are published, unless the issuing agency requests earlier filing.