IKCa Related Drug Discovery Products
Membrane protein stable cell lines are widely used in many areas of biomedical research. Creative Biolabs can offer membrane protein stable cell lines to stablish in vitro models for High Throughput Screening.
Creative Biolabs offers high-quality, innovative tools to help research groups accelerate membrane protein drug discovery. They can be found by targets. If there is no product that meets your needs, please contact us.
According to their membrane architecture, potassium channels, the biggest and most diverse grouping of ion channels, are divided into four subgroups. The KCa channel family is divided into two sub-families: the large conductance BKCa subfamily and the small conductance (SKCa) and intermediate (IKCa) conductance KCa subfamily, which includes KCa2.1, KCa2.2, KCa2.3 (also known as SK1, SK2, and SK3) and KCa3.1 (also known as IK1) subunits. IKCa channels and calcium-activated potassium channels with tiny conductances are voltage-independent, and the association with calmodulin is thought to be the cause of their calcium sensitivity.
As a leader in drug discovery, Creative Biolabs offer a series of IKCa drug discovery in vitro assays and products with the best quality:
Overview of IKCa
KCa3.1 is the major Ca2+-activated K+ channel in human T lymphocytes and in other immune cells. Additional nonexcitable tissues where KCa3.1 is important include fibroblasts, dedifferentiated vascular smooth muscle cells, secretory epithelia, and the vascular endothelium. KCa3.1 controls membrane potential and Ca2+ signaling in each of these organs. While two recent research suggested that KCa3.1 may be produced in neurons and that it may help explain the gradual afterhyperpolarization that occurs in hippocampus-related neurons after a burst of action potentials, a third study found that KCa3.1 is not involved in this slow AHP. Therefore, it is currently unknown what the channel's possible function in neurons might be.
Due to the importance of KCa3.1 and KCa2.3 in the endothelium-derived hyperpolarization vasodilator response, many of the pharmacological drugs that activate KCa2 channels are also positive modulators of KCa3.1 and are being investigated as novel endothelialtargeted antihypertensives. However, compared to the KCa2 family, KCa3.1 current suppressing drugs have a different pharmacology. Until far, treating sickle cell anemia has been the only clinical use of KCa3.1 blockers.
IKCa Drug Discovery
The endothelial intracellular calcium Ca2+ concentration is increased by antagonists that stimulate G protein-coupled receptors, calcium ionophores, thapsigargin, and cyclopiazonic acid, which activates SK3 and IK1 channels. As a result, the endothelial cells become hyperpolarized, and vascular smooth muscle cells also become hyperpolarized in an endothelium-dependent manner. By boosting the driving power for this ion, the endothelial cells' hyperpolarization favors calcium entry. As a result, endothelial KCa play a crucial role in EDHF-mediated responses and help to activate calcium-sensitive enzymes like the NOS and cause the production of NO. The buildup of potassium ions in the intercellular space and direct electrical interaction through myo-endothelial gap junctions can both induce the endothelium-dependent hyperpolarizations of vascular smooth muscle cells.
