potassium ion channel

Yoda 1 is an agonist of the Piezo1 channel that agonizes human- and mouse-derived Piezo1 (EC50=17.1 26.6 μM). Yoda 1 is also an inhibitor of glycine transporter protein 2 (GlyT2).

Sodium dichloroacetate (BCA) , a specific inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50 values of 183 and 80 μM for PDK2 and PDK4 respectively, has been shown to derepress a mitochondrial potassium-ion channel axis, trigger apoptosis in cancer cells, and inhibit tumor growth.

Dofetilide (UK 68789) is a sulfonamide class III antiarrhythmic agent and potassium channel blocker. Dofetilide selectively blocks cardiac ion channels of the rapid component of the delayed rectifier potassium current Ikr. This antiarrhythmic agent prolongs cardiac action potential duration and effective refractory period due to delayed repolarization without affecting conduction velocity. This results in a normal sinus rhythm. Dofetilide is used in the treatment of atrial fibrillation and flutter.

Ropivacaine hydrochloride monohydrate (LEA-103 HCl) is an anaesthetic agent and blocks impulse conduction in nerve fibres through inhibiting sodium ion influx reversibly.

Cholesterol Myristate (Cholesteryl Myristate) is a natural steroid found in traditional Chinese medicine that interacts with various ion channels, including the GABAA receptor, nicotinic acetylcholine receptor, and the inward-rectifier potassium ion channel.

Gramicidin (Gramicidine) is an antimicrobial peptide. Gramicidin dimers form ion channel-like pores in the cell membranes and organelles of bacterial and animal cells, allowing inorganic monovalent ions, such as potassium and sodium ions, to pass freely through the pores by diffusion, disrupting the important ionic gradient between membranes and thus killing the cells by various actions. Gramicidin is effective against Gram-positive bacteria such as Bacillus subtilis and Staphylococcus aureus, but is not as effective against Gram-negative bacteria such as Escherichia coli.

NS3623 is an activator of human ether-a-go-go-related gene (hERG) potassium channels with a dual mode of action, also acting as an inhibitor of hERG1 channels. It activates the IKr and Ito currents and exhibits an antiarrhythmic effect.

GSK369796 Dihydrochloride (N-tert-butylisoquine),is an anti-malaria drug candidate. is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization(IC50 of 7.5 μM)

GLP-1 receptor agonist 15 (Example 4) is a GLP receptor agonist with an EC50 of 0.74 nM. It exhibits an IC50 of 10.1 μM against the hERG potassium ion channel. This compound is applicable for research in the diabetes field.

Ebio3 is a selective potassium ion channel (KCNQ2) inhibitor with an IC50 of 1.2 nM. It binds to the KCNQ2 channel via its hydrophobic tail, causing the inward movement of the S6 helix, which results in the closure of the internal gate. The inhibitory effect of Ebio3 is equally effective on pathogenic KCNQ2 mutants, such as R75C and I238L, reducing their outward current by approximately 80%. Ebio3 holds potential for research in neurological disorders like epilepsy.

(BrMT)2 is an activator of the Kv1.1 potassium ion channel.

Photoswitchable Kv channel blocker (IC50 values are 2 and 64 μM at 500 nm and 380 nm respectively). Switches conformation from cis to trans at 500 nm and trans to cis at 380 nm. Exhibits minimal activity at Nav1.2 and L-type Ca2+ channels. Stimulates action potential firing of hippocampal neurons in vitro at 500 nm and restores visual responsiveness in blind mice at 380 nm. Fortin et al (2008) Photochemical control of endogenous ion channels and cellular excitability. Nat.Methods 5 331 PMID:18311146 |Polosukhina et al (2012) Photochemical restoration of visual responses in blind mice. Neuron 75 271 PMID:22841312 |Banghart et al (2009) Photochromic blockers of voltage-gated potassium channels. Angew.Chem.Int.Ed. 48 9097 PMID:19882609

Ropivacaine mesylate, a long-acting amide local anaesthetic, is used for spinal block and effectively mitigates neuropathic pain. It achieves analgesia by reversibly inhibiting sodium ion influx in nerve fibers, thus blocking impulse conduction. Additionally, Ropivacaine acts as an inhibitor of the K2P (two-pore domain potassium channel) TREK-1, exhibiting an IC50 of 402.7 μM in COS-7 cell membranes.

DAD is an ion channel blocker (blocks voltage-gated potassium channels) and is a third generation photoelectric switch that responds to visible light.

DAD dichloride is an ion channel blocker that blocks voltage-gated potassium channels, a third-generation photoelectric switch that responds to visible light, and can be used to study visual function.

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

κM-Conotoxin RIIIK is a potassium channel antagonist that inhibits voltage-activated potassium ion channels [1].

CVN293 is a selective and brain-permeable potassium ion (K+) channel KCNK13 inhibitor with IC50 values of 41 nM for hKCNK13 and 28 nM for mKCNK13, respectively. CVN293 potently inhibits the NLRP3-inflammasome-mediated production of the pro-inflammatory cytokine IL-1β in microglia [1].