Potassium
Potassium channels are a diverse and ubiquitous family of membrane proteins present in both excitable and non-excitable cells. Members of this channel family play critical roles in cellular signaling processes regulating neurotransmitter release, heart rate, insulin secretion, neuronal excitability, epithelial electrolyte transport, smooth muscle contraction, and cell volume regulation. Over 50 human genes encoding various potassium channels have been cloned during the past decade[1]. Based on the structure of the potassium channels, four main classes can be identified. The basis of all channels consists of four subunits that are clustered to form the ion-permeation pathway across the membrane. Each of the four subunits is build up of two transmembrane helices and a short loop between them. Distinct features characterize the four main classes[2]: inwardly rectifying potassium channels (2TM/P channels), voltage and/or ligand gated ion channels (6TM/P channels), hybrid channels made from the two previously mentioned classes (8TM/2P channels), and dimer channels (4TM/2P channels) made from two repeats of the inwardly rectifying channels, and are often referred to as ‘leakage channels’. Also the hyperpolarization-activated and cyclic nucleotide-gated (HCN) channels belong to the superfamily of voltage-gated K+ (Kv) and cyclic nucleotide-gated (CNG) channels. They are sometimes referred to as “pacemaker channels” because they help to generate rhythmic activity within groups of heart and brain cells.
Axon Medchem offers a variety of potassium channel openers and blockers, including the racemate and optically pure enantiomers of BMS204352 (Axon 1112, Axon 1308, and Axon 1309), modulators of the Maxi-K channel (or BK channel, member of 6TM/P channel class), and Zatebradine HCl (Axon 1248, HCN channel blocker).
[1] Potassium Channels: Molecular Defects, Diseases, and Therapeutic Opportunities. C.C. Shieh, M. Coghlan, J.P. Sullivan, M. Gopalakrishnan. Pharmacological Reviews, 2000, 52, 557-594.
[2] Ion conduction pore is conserved among potassium channels. Lu, Z., Klem, A. M. & Ramu, Y. Nature 2001, 413, 809–813.
Axon ID | Name | Description | From price | |
---|---|---|---|---|
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 | |
1294 | Chromanol 293B | KCNQ1 channel blocker | €120.00 | |
1322 | DMP 543 | K+ channel blocker; Ach release stimulator | €90.00 | |
2103 | Dofetilide | Kv11.1 (hERG) channel blocker | €85.00 | |
3450 | Dronedarone hydrochloride | Ca2+/K+/Na+ channel blocker; Antiarrhythmic agent | €100.00 | |
4173 | Ebio1 | Potent and highly selective KCNQ2 activator | Recently added | €130.00 |
1437 | Flupirtine maleate | Analgesic | €65.00 | |
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 | |
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 | |
2747 | ML 213 | KCNQ2/KCNQ4 channel opener | €75.00 | |
2615 | ML252 | Selective and brain penetrant KCNQ2 inhibitor | €95.00 | |
3196 | ML277 | Potent and selective KCNQ1 channel activator | €80.00 | |
3644 | Propafenone hydrochloride | Ca2+/K+/Na+ channel blocker; Antiarrhythmic agent | €60.00 | |
3507 | Ranolazine | Ca2+/K+/Na+ channel blocker; Anti-anginal agent | €70.00 | |
1525 | Retigabine | KCNQ channel opener; Anti-convulsant | €90.00 | |
2252 | Retigabine dihydrochloride | KCNQ channel opener; Anti-convulsant | €90.00 | |
1657 | S 9947 | Ikur/Kv1.5 channel Inhibitor | €125.00 | |
3265 | XAF-1407 | Potent and highly selective IKACh inhibitor | €140.00 | |
1987 | XE 991 | KCNQ channel and M-current blocker | €90.00 | |
1305 | XE 991 dihydrochloride | KCNQ channel and M-current blocker | €90.00 | |
1248 | Zatebradine hydrochloride | HCN channel blocker | €110.00 |