small-conductance

Rimtuzalcap (CAD-1883) (CAD-1883), a pioneering selective positive allosteric modulator of small-conductance calcium-activated potassium channels (SK channels), is employed in the study of movement disorders such as spinocerebellar ataxia (SCA) and essential tremor (ET).

Tezacaftor (VX-661) is a cystic fibrosis transmembrane conductance regulator (CFTR) corrector. Tezacaftor increases the number of functional CFTR proteins by promoting the proper folding and transport of mutant CFTR proteins to the cell surface, thereby restoring chloride channel function. Tezacaftor is commonly used in cystic fibrosis research.

NS8593 hydrochloride (NS8593 HCl) is a potent and selective inhibitor of small conductance Ca2+-activated K+ channels (SK channels) .

NS13001 (N-(4-Chlorophenyl)-2-(3,5-dimethyl-1H-pyrazol-1-yl)-9-methyl-9H-purin-6-amine) is a potent, selective, orally active allosteric positive modulator of SK channels (small conductance calcium-activated potassium channels). The EC50s are 1.8 and 0.14 μM for SK2 and SK3, respectively. NS13001 holds promise as a potential therapeutic agent for treatment of spinocerebellar ataxia type 2 (SCA2) and possibly other cerebellar ataxias.

KCa2 (small conductance Ca2+-activated potassium) channel negative allosteric modulator (IC50 = 1.1 μM). Increases the EC50 of Ca2+ on KCa2.3 channels by ~3-fold. Prolongs atrial effective refractory period (AERP) in rats. Reduces atrial fibrillation (AF) duration and prolongs atrial refractoriness without affecting ventricular refractory period in an animal AF model. Diness et al (2017) Termination of vernakalant-resistant atrial fibrillation by inhibition of small-conductance Ca2+-activated K+ channels in pigs. Circ.Arrhythm.Electrophysiol. 10 e005125 PMID:29018164 |Simó-Vicens et al (2017) A new negative allosteric modulator, AP14145, for the study of small conductance calcium-activated potassium (KCa2) channels. Br.J.Pharmacol. 174 4396 PMID:28925012

NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hE

Scyllatoxin (Leiurotoxin I), a peptide toxin derived from the venom of the scorpion (Leiurus quinquestriatus hebraeus), acts as a blocker of small-conductance K Ca (SK) channels. It notably enhances the release of norepinephrine (NE) and epinephrine (Epi) in vivo [1].

Tamapin, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small-conductance Ca(2+)-activated K(+) (SK) channels, particularily SK2 (Potassium Channel). It inhibits SK channel-mediated currents in the pyramidal neurons of the hippocampus.

Tamapin TFA, a venom peptide isolated from the Indian red scorpion (Mesobuthus tamulus) [1], selectively targets and blocks small conductance Ca(2+)-activated K(+) (SK) channels, particularly the SK2 subtype (Potassium Channel). It is known to inhibit SK channel-mediated currents in the hippocampal pyramidal neurons.

(±)13,14-EDT, an oxylipin metabolite derived from adrenic acid through the cytochrome P450 (CYP) pathway, acts as a potent activator of large-conductance calcium-activated potassium channels (KCa1.1/BK) in isolated rat coronary small arterial smooth muscle cells at 50 nM, promoting dilation. Additionally, it induces arteriole dilation in isolated porcine samples with an EC50 of 12 pM and relaxes isolated bovine coronary arteries previously contracted by TP receptor agonist U-46619.

5(6)-DiHET is a racemic compound synthesized through the action of epoxide hydrolases on 5(6)-EET, encompassing both enantiomeric forms. It serves as a quantitative marker for 5(6)-EET, facilitating its measurement by utilizing the compound's conversion to 5(6)-δ-lactone in solution. Additionally, 5(6)-DiHET activates large-conductance calcium-activated potassium (KCa1.1/BK) channels in rat small coronary artery smooth muscle cells, supporting its biological significance in vascular regulation. It also acts as a substrate for sheep seminal vesicle COX, leading to the in vitro production of 5,6-dihydroxy prostaglandin E1 and F1α metabolites. Notably, its levels diminish in the plasma of rats subjected to a high-fat diet, indicating a potential role in the pathophysiology of hyperlipidemia.

AP14145 functions as an inhibitor of the small conductance calcium-activated potassium channels (small conductance calcium-activated potassium channel), specifically blocking the KCa2.2 channel (KCa2.2 channel) and KCa2.3 channel (KCa2.3 channel) with an IC50 of 1.1 μM for both. It prolongs the atrial effective refractory period (AERP) in rats and has been shown to convert atrial fibrillation to sinus rhythm in a porcine model of left ventricular dysfunction, demonstrating antiarrhythmic properties.

Tezacaftor-D4 is a deuterated compound of Tezacaftor. Tezacaftor (T2263) has a CAS number of 1152311-62-0. VX-661 is a small molecule that can be used as a corrector of the cystic fibrosis transmembrane conductance regulator (CFTR) gene function.

Apamin TFA (Apamine TFA) is a toxin found in bee venom. It is a potent blocker of small conductance Ca2+-activated K+ (SK, KCa2) channels that is more effective at SK2 than SK1 and SK3.

Chlorotoxin is a 36-amino acid peptide found in the venom of the deathstalker scorpion (Leiurus quinquestriatus) which blocks small-conductance chloride channels.