Ion Channels

Ion channels are pore-forming membrane proteins that act as gated pathways for the movement of ions across cell membranes. They are found in both surface and intracellular membranes, and play essential roles in the physiology of all cell types. Ion channels are especially prominent components of the nervous system as they underlie the nerve impulse and because "transmitter-activated" channels mediate conduction across the synapses of a nerve cell’s axon. In addition, ion channels are key components in a wide variety of biological processes that involve rapid changes in cells, such as cardiac, skeletal, and smooth-muscle contraction, epithelial transport of nutrients and ions, T-cell activation and pancreatic beta-cell insulin release. Many human diseases are caused by defects in ion channel function, which can lead to disease in a number of different ways: Gain, or loss, of channel function (channel-pathies), defective regulation of channel activity by intracellular or extracellular ligands or by channel modulators, by autoantibodies binding to ion channel proteins, or even by ion channels that act as lethal agents[1]. Ion channels can be categorized based upon multiple characteristics, e.g. their selectivity in permeability for a certain type of ion, the number of pores, or by their mechanism of activation.  The wide range of Axon Ligands™  targeting ion channels has been categorized into ligand gated ion channels and voltage gated ion channels (and more). Categories are subdivided on the basis of their selectivity towards activating ligand or the type of ion. In addition, sections are created for specific members of the family of potassium channels that are characterized by their deviant ways of activation (e.g. calcium-activated, and ATP-sensitive potassium channels).


[1] Taken from Oxford Textbook of Medicine, fifth edition, 2010. ISBN 9780470987261.

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Axon ID Name Description From price
1309 (R)-(-)-BMS 204352 Potassium channel opener; Less active enantiomer of Axon 1112 €145.00
1308 (±)-BMS 204352 Potassium channel opener; racemate of Axon 1112 Inquire
1313 1-EBIO K+ channel opener (Ca2+ activated) €50.00
3019 A2764 dihydrochloride Selective inhibitor of the TRESK potassium channel €105.00
3060 A2793 Inhibitor of the TRESK and TASK-1 potassium channel €95.00
2979 ASP 2905 Potent, selective and orally active KCNH3 (Kv12.2) inhibitor €125.00
2243 AVE 0118 hydrochloride Potassium channel blocker (Kv1.5 (IKur), Kv4.3 (Ito), Kir3.4 (IKAch), and IKr currents) €120.00
1112 BMS 204352 Maxi K+ channel opener €110.00
1294 Chromanol 293B KCNQ1 channel blocker €95.00
1322 DMP 543 K+ channel blocker; Ach release stimulator €90.00
2103 Dofetilide Kv11.1 (hERG) channel blocker €85.00
1437 Flupirtine maleate Analgesic €65.00
2064 Glibenclamide potassium salt KATP channel blocker; inhibits SUR1 €50.00
3503 Glipizide KATP channel blocker; inhibits SUR1 €50.00
1757 HMR 1098 K+ channel blocker (SUR1/Kir6.2 selective) €95.00
2724 ICA-069673 KCNQ2/KCNQ3 channel opener; Anti-convulsant €90.00
3091 ICA-110381 KCNQ2/KCNQ3 channel opener; Anti-convulsant €80.00
3495 Ivabradine hydrochloride Selective sinus node I(f) channel inhibitor €50.00
3516 KCa modulator RA-2 Potent and selective KCa2/3 pan inhibitor €110.00
1735 Kv1.3 Channel blocker 42 Kv1.3 potassium channel blocker €110.00
3032 LUF7244 Potent negative allosteric modulator (NAM) of the Kv11.1 (hERG) channel €140.00
3490 Minoxidil K+ channel opener (ATP sensitive, vascular) €50.00
2747 ML 213 KCNQ2/KCNQ4 channel opener €75.00
2436 ML 297 First potent and selective activator of the GIRK potassium channel €95.00
2872 ML 335 Selective activator of the TREK-1 and TREK-2 potassium channel €115.00
2840 ML 365 Potent and selective inhibitor of the TASK-1 potassium channel €135.00
2615 ML252 Selective and brain penetrant KCNQ2 inhibitor €95.00
3196 ML277 Potent and selective KCNQ1 channel activator €80.00
3641 Nateglinide KATP channel blocker; inhibits SUR1 €60.00
1647 NN 414 K+ channel opener (SUR1/Kir6.2 selective) €110.00

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