kca2.3

SKA-121 is a selective KCa3.1 activator (EC50s: 109 nM and 4.4 μM for KCa3.1 and KCa2.3, respectively).

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

AP14145 hydrochloride is a potent negative allosteric modulator of K Ca 2 (SK) channels, specifically targeting K Ca 2.2 (SK2) and K Ca 2.3 (SK3) channels with an IC 50 of 1.1 μM. Inhibition of AP14145 hydrochloride is highly influenced by S508 and A533 amino acids present in the channel. This compound effectively extends the atrial effective refractory period (AERP) in rats and exhibits antiarrhythmic properties in a Vernakalant-resistant porcine model of atrial fibrillation (AF).

SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) 是一种钾离子通道激活剂，作用于 KCa3.1，KCa2.2，KCa2.1和 KCa2.3的 EC50分别为 260 nM，1.9 μM，2.9 μM，2.9 μM. SKA31增强内皮源性超极化因子反应，降低血压。

KCa2 channel modulator 1 (compound 2o) 是有效的亚型选择性的K Ca 通道的正调节剂，其增强大鼠 KCa2.2 通道亚型的EC50值为 0.99 μM 和人KCa2.3 通道亚型的EC50值为 0.19 μM。

KCa2 channel modulator 2 (compound 2q) 是有效的亚型选择性KCa2通道的正调节剂，对人KCa2.3 通道和大鼠 KCa2.2 通道亚型显示出相似的效力，EC50值分别为 0.6 μM 和 0.64 μM。

JNc-440 是一种有效的抗高血压剂。JNc-440 能够提高内皮细胞瞬时受体电位香草酸亚型 4 (TRPV4) 和钙离子激活钾通道 3 (KCa2.3) 的相互作用。JNc-440 也可以提高小鼠血管扩张，具有降压活性。

AP14145 是一种针对小电导钙激活的钾离子通道 (small conductance calcium-activated potassium channel) 的抑制剂,有效抑制 KCa2.2 通道 (KCa2.2 channel) 和 KCa2.3 通道 (KCa2.3 channel),其 IC50 值均为 1.1 μM.在生理研究中,AP14145 能有效延长大鼠心房有效不应期 (AERP),并在猪左心室功能障碍模型中实现房颤向窦性心律的转换,显示出显著的抗心律失常效果.

High affinity, selective KCa2.2 (SK2) channel blocker (Kd = 3.8 nM). Exhibits >200-fold selectivity for KCa2.2 over KCa2.1, KCa2.3, KCa3.1, IK, Kv and Kir2.1. Increases theta-burst responses and increases LTP in rat hippocampal slices in vitro. Convulsive