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Sodium Channel Na Channels; Na+ Channels

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Sodium Channel Na Channels; Na+ Channels 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, Agonists, Antagonists, Activators & Modulators (+)-Kavain (-)-Sparteine sulfate pentahydrate Cat. No.: HY-B1671 ((-)-Lupinidine sulfate pentahydrate) Cat. No.: HY-B1304 (+)-Kavain, a main kavalactone extracted from Piper (-)-Sparteine sulfate pentahydrate ((-)-Lupinidine methysticum, has anticonvulsive properties, sulfate pentahydrate) is a class 1a antiarrhythmic attenuating vascular smooth muscle contraction agent and a sodium channel blocker. It is an through interactions with voltage-dependent Na+ alkaloid, can chelate the bivalents calcium and and Ca2+ channels. magnesium. Purity: 99.98% Purity: ≥98.0% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg Size: 10 mM × 1 mL, 50 mg (Rac)-AMG8379 20(S)-Ginsenoside Rg3 ((Rac)-AMG8380) Cat. No.: HY-108425B (20(S)-Propanaxadiol; S-ginsenoside Rg3) Cat. No.: HY-N0603 (Rac)-AMG8379 ((Rac)-AMG8380) is a racemate of 20(S)-Ginsenoside Rg3 is the main component of Red AMG8379. AMG8379 is a potent, orally active and ginseng. Ginsenoside Rg3 inhibits Na+ and selective sulfonamide antagonist of NaV1.7, with hKv1.4 channel with IC50s of 32.2±4.5 and 32.6±2.2 IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, μM, respectively. 20(S)-Ginsenoside Rg3 also respectively . inhibits Aβ levels, NF-κB activity, and COX-2 expression. Purity: >98% Purity: 98.10% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg 5-(N,N-Hexamethylene)-amiloride A-317567 (Hexamethylene amiloride; HMA) Cat. No.: HY-128067 Cat. No.: HY-122135 5-(N,N-Hexamethylene)-amiloride (Hexamethylene A-317567 is a potent acid-sensing ion channel 3 amiloride) derives from an amiloride and is a (ASIC-3) inhibitor with an IC50 of 1.025 μM. potent Na+/H+ exchanger inhibitor, which A-317567 has antidepressant and antinociception decreases the intracellular pH (pHi) and induces effects. apoptosis in leukemic cells. Purity: 98.42% Purity: >98% Clinical Data: Phase 3 Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg Size: 1 mg, 5 mg A-803467 A-887826 Cat. No.: HY-11079 Cat. No.: HY-100080 A 803467 is a selective Nav1.8 sodium channel A-887826 is a potent, selective, oral bioavailable blocker with an IC50 of 8 nM; over 100-fold more and voltage-dependent Na(v)1.8 sodium channel selective vs. human Nav1.2, 1.3, 1.5 and 1.7. blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo. Purity: 98.51% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 10 mg, 50 mg Size: 1 mg, 5 mg Ajmaline AM-2099 (Cardiorythmine; (+)-Ajmaline) Cat. No.: HY-B1167 Cat. No.: HY-100727 Ajmaline (Cardiorythmine) is a sodium channel AM-2099 is a potent and selective inhibitor of blocking, class 1A anti-arrhythmic agent. Ajmaline voltage-gated sodium channel Nav1.7 with an IC50 blocks HERG currents with an IC50 of 1 μM in HEK of 0.16 μM for human Nav1.7. cells and 42.3 μM in Xenopus oocytes. Ajmaline can be used for the research of the ventricular tachyarrhythmia. Purity: 99.84% Purity: 98.02% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg 2 Tel: 609-228-6898 Fax: 609-228-5909 Email: [email protected] AMG8380 Amiloride Cat. No.: HY-108425A (MK-870) Cat. No.: HY-B0285 AMG8380, an orally active and less active Amiloride (MK-870) is an inhibitor of both enantiomer of AMG8379, can serves as a negative epithelial sodium channel (ENaC) and control. AMG8380 inhibits human and mouse urokinase-type plasminogen activator receptor voltage-gated sodium channel NaV1.7 with IC50s of (uTPA). Amiloride is a blocker of polycystin-2 0.907 and 0.387 μM, respectively. (PC2; TRPP2) channel. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: Launched Size: 1 mg, 5 mg Size: 1 mg, 5 mg Amiloride hydrochloride Amiloride hydrochloride dihydrate (MK-870 hydrochloride) Cat. No.: HY-B0285A (MK-870 hydrochloride dihydrate) Cat. No.: HY-B0285B Amiloride hydrochloride (MK-870 hydrochloride) is Amiloride hydrochloride dihydrate (MK-870 an inhibitor of both epithelial sodium channel hydrochloride dihydrate) is an inhibitor of both (ENaC) and urokinase-type plasminogen activator epithelial sodium channel (ENaC) and receptor (uTPA). Amiloride hydrochloride is a urokinase-type plasminogen activator receptor blocker of polycystin-2 (PC2; TRPP2) channel. (uTPA). Amiloride hydrochloride dihydrate is a blocker of polycystin-2 (PC2; TRPP2) channel. Purity: 99.71% Purity: 99.50% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 100 mg, 500 mg Size: 10 mM × 1 mL, 100 mg Amitriptyline hydrochloride Annonacin Cat. No.: HY-B0527A Cat. No.: HY-N2877 Amitriptyline hydrochloride is an inhibitor of Annonacin is an Acetogenin and promotes serotonin reuptake transporter (SERT) and cytotoxicity via a pathway inhibiting the noradrenaline reuptake transporter (NET), with Kis mitochondrial complex. Annonacin is the active of 3.45 nM and 13.3 nM for human SERT and NET, agent found in Graviola leaf extract to act as an respectively. inhibitor of sodium/potassium (NKA) and sarcoplasmic reticulum (SERCA) ATPase pumps. Purity: 99.56% Purity: >98% Clinical Data: Launched Clinical Data: No Development Reported Size: 10 mM × 1 mL, 500 mg, 1 g, 5 g Size: 5 mg APETx2 APETx2 TFA Cat. No.: HY-P1346 Cat. No.: HY-P1346A APETx2, a sea anemone peptide from Anthopleura APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses its external side. APETx2 could reverses acidinduced and inflammatory pain. acidinduced and inflammatory pain. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg AZD-3161 Benzamil Cat. No.: HY-117714 (Benzylamiloride) Cat. No.: HY-B1546 AZD-3161 is a potent and selective blocker of Benzamil (Benzylamiloride), an Amiloride analogue, + 2+ NaV1.7 channel, with a pIC50 of 7.1. AZD-3161 can is a Na /Ca exchanger (NCX) inhibitor be used for the research of neuropathic and (IC50~100 nM). Benzamil also is a non-selective inflammatory pain. Deg/epithelial sodium channels (ENaC) blocker, and can potentiate myogenic vasoconstriction. Purity: >98% Purity: >98% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 1 mg, 5 mg www.MedChemExpress.com 3 Benzamil hydrochloride Benzocaine (Benzylamiloride hydrochloride) Cat. No.: HY-B1546A Cat. No.: HY-Y0258 Benzamil hydrochloride (Benzylamiloride Benzocaine shares a common receptor with all othe hydrochloride), an Amiloride analogue, is a rLAs in the voltage-gated Na+ channel, with an + 2+ Na /Ca exchanger (NCX) inhibitor (IC50~100 IC50 of 0.8 mM tested with a potential of +30 mV. nM). Purity: 99.60% Purity: 99.98% Clinical Data: Launched Clinical Data: Launched Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 500 mg BI 01383298 BI-9627 Cat. No.: HY-124738 Cat. No.: HY-18071 BI 01383298 is a potent inhibitor of the BI-9627 is potent sodium-hydrogen exchanger sodium-citrate co-transporter (SLC13A5) that isoform 1 (NHE1) inhibitor, with IC50s of 6 and is highly expressed in the liver. 31 nM in intracellular pH recovery (pHi) and human platelet swelling assays, respectively. Purity: 99.96% Purity: ≥99.0% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg Size: 10 mM × 1 mL, 5 mg BI-9627 hydrochloride Bifenthrin Cat. No.: HY-18071A Cat. No.: HY-B0824 BI-9627 hydrochloride is potent sodium-hydrogen Bifenthrin is a synthetic pyrethroid insecticide exchanger isoform 1 (NHE1) inhibitor, with IC50s that prolongs opening of sodium channels resulting of 6 and 31 nM in intracellular pH recovery (pHi) in membrane depolarization and conductance block and human platelet swelling assays, respectively. in the insect nervous system. Purity: >98% Purity: 99.51% Clinical Data: No Development Reported Clinical Data: No Development Reported Size: 1 mg, 5 mg Size: 10 mM × 1 mL, 10 mg, 25 mg, 50 mg Brevetoxin B Brevetoxin-3 (Brevetoxin-2; PbTx-2) Cat. No.: HY-12546 (PbTx-3) Cat. No.: HY-12545 Brevetoxin B (Brevetoxin-2; PbTx-2) is a Brevetoxin-3 (PbTx-3) is a potent allosteric polyketide neurotoxin produced by Karenia species voltage-gated Na+ channel activator and has and other dinoflagellates.
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