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.

14 Item(s)

per page
Axon ID Name Description From price
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
2552 Adjudin Non-hormonal male contraceptive with anti-proliferative activity €125.00
2979 ASP 2905 Potent, selective and orally active KCNH3 (Kv12.2) inhibitor €125.00
3036 BI 749327 Potent, selective and orally bioavailable TRPC6 inhibitor €160.00
2572 GlyH 101 Highly potent and selective CFTR inhibitor €105.00
3495 Ivabradine hydrochloride Selective sinus node I(f) channel inhibitor €50.00
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
3349 NMDAR-TRPM4 blocker C19 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €130.00
3348 NMDAR-TRPM4 blocker C8 dihydrochloride NMDAR/TRPM4 interaction interface inhibitor €120.00
2295 PPQ 102 CFTR inhibitor that acts by a mechanism involving stabilization of the channel closed-state €100.00
3593 VU0468554 Selective cardiac GIRK inhibitor €110.00
3265 XAF-1407 Potent and highly selective IKACh inhibitor €165.00

14 Item(s)

per page
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