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Ion Channels

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  • 1-EBIO | K+ channel activator; Promotes cardiomyocyte differentiation
    1-EBIO (10045-45-1) is a direct activator of small-conductance Ca2+-activated K+ channels (SK) which dose-dependently relaxes rat mesenteric vessels.1  Reverses ischemia-induced cognitive impairment2 and displays...

  • 2-APB | 524-95-8 | Structure | Supplier
    2-APB (524-95-8) is an IP3 receptor antagonist (IC50=42 μM).1 Inhibits store-operated Ca2+ channels at high concentrations (50 μM) but stimulates at low concs. (<10 μM).2 Modulates TRP channels,...

  • 2GBI | Hv1 channel blocker
    2GBI (5418-95-1) is a selective and state-dependent blocker of voltage-gated proton channels (Hv1).1 2GBI blocks the channel by binding to the voltage-sensing domain from its intracellular side.2,3  Inhibition of Hv1 is...

  • 4,9-Anhydrotetrodotoxin | Selective sodium channel blocker
    4,9-Anhydrotetrodotoxin (13072-89-4) is a highly selective blocker of the Na(v1.6) sodium channel. (IC50's: Na(v1.2) = 260 nM, Na(v1.3) = 341 nM, Na(v1.4) = 988 nM, Na(v1.5) = 11.6 μM, Na(v1.6) = 7.8 nM, Na(v1.7) = 1.27...

  • A-803467 | 944261-79-4 | Structure | Supplier
    A-803467 (944261-79-4) is a potent, selective inhibitor of the TTX-resistant voltage-gated sodium channel Nav1.8. Nav1.8 is preferentially expressed in sensory neurons, and inhibition attenuates both inflammatory and...

  • A-967079 | 1170613-55-4 | Structure | Supplier
    A-967079 (1170613-55-4) is a TRPA1 antagonist. Active in rat models.1 Cell permeable References/Citations1) McGaraughty et al. (2010), TRPA1 modulation of spontaneous and mechanically evoked firing of spinal neurons in...

  • AM-404 | 198022-70-7 | Structure | Supplier
    AM-404 (198022-70-7) inhibits anandamide transport (IC50 = 1 μM) without inhibiting anandamide amidase or activating cannabinoid receptors.1,2 Vanilloid receptors are activated by AM-404.3 Active in vivo...

  • Ambroxol HCl | Free radical scavenger
    Ambroxol HCl (18683-91-5) is a radical scavenger with anti-inflammatory activity. Blocks the generation of reactive oxygen species by bronchoalveolar lavage cells, inhibits doxorubicin-induced lipid peroxidation (70 mg/kg in...

  • Amlodipine | 88150-42-9 | Structure | Supplier
    Amlodipine (88150-42-9) is an anti-hypertensive L-type calcium channel blocker, which also benefits the cardiovascular system by stimulating nitric oxide synthase, inhibiting angiotension-induced oxidative stress and...

  • AP-18 | 552244-94-7 | Structure | Supplier
    AP-18 (55224-94-7) is a selective TRPA1 (transient receptor potential A1) channel blocker (IC50 = 3.1 and 4.5 μM at human and mouse TRPA1 respectively). References/Citations1) Petrus et al. (2007) A role of TRPA1 in...

  • BAPTA-AM | 126150-97-8 | Structure | Supplier
    BAPTA-AM (126150-97-8) is a selective cell permeable Ca2+ chelator. It is a widely used intracellular calcium sponge1,2. Rapidly taken up by cells where it is irreversibly hydrolyzed to BAPTA by intracellular esterases...

  • BAY K8644 | L-type calcium channel activator
    BAY K8644 (71145-03-4) is an L-type Ca2+-channel activator with positive inotropic and vasoconstrictive effects.1-4 References/Citations1) Schramm et al. (1983) Novel Dihydropyridines with positive inotropic action through...

  • BCTC | 393514-24-4 | Structure | Supplier
    BCTC (393514-24-4) is a vanilloid receptor I (TRPV1) antagonist, IC50 = 35 nM for capsaicin-induced and 6 nM for acid-induced TRPV1 activation. Displays analgesic activity in rat models of neuropathic pain. BCTC is orally...

  • Benzamil HCl | Sodium channel blocker
    Benzamil HCl (2898-76-2) is a derivative of amiloride. Potent sodium channel blocker

  • Capsaicin (natural) | TRPV1 agonist
    Capsaicin (404-86-4) is a vanilloid agonist known to activate the transient receptor potential channel vanilloid subfamily member 1 (TRPV1)1,2 and to possess analgesic3, anti-inflammatory4 and hypolocomotor effects5. SEVERE...

  • CGP-37157 | MPTP inhibitor
    CGP-37157 (75450-34-9) inhibits the mitochondrial Na+-Ca2+ exchanger (NCX) in isolated heart mitochondria, IC50=0.36 mM.1 Does not inhibit the plasmalemmal NCX.2  Also inhibits voltage-gated Ca2+ channels in intact...

  • Cyclothiazide | AMPA receptor positive allosteric modulator
    Cyclothiazide (2259-96-3) is a positive allosteric modulator of AMPA receptors acting at a site distinct from that of 2,3-benzodiazepines.1,2 Clinically useful diuretic and antihypertensive agent.3 Induces robust...

  • Deltamethrin | Calcineurin inhibitor; displays neurotrophic activity
    Deltamethrin (52918-63-5) is reported to be an inhibitor of calcineurin (PP2B), IC50~100 pM1 but this activity has been disputed2. Markedly enhances the expression of BDNF in cultured rat cortical neurons and displays...

  • Diazoxide | K-ATP channel activator
    Activates ATP-dependent K+ channels1 via inducing translocation of PKC-epsilon from the cytosol to the mitochondria2. Hyperglycemic agent. Induces powerful protective effects against cardiac ischemia via multiple mechanisms...

  • Dofetilide | 115256-11-6 | Structure | Suplier
    Dofetilide (115256-11-6) is a clinically useful class III antiarrhythmic that inhibits the rapid component of the delayed rectifier outward potassium current (IKr) via selective blockage of the Kv11.1 (hERG) channel...

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