kca2.3

SKA-31 (Naphtho[1,2-d]thiazol-2-ylamine) is an activator of KCa3.1 and KCa2 channels (EC50s: 260, 2900, 2900 nM for KCa3.1, KCa2.1 and KCa2.2 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

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

JNc-440 is a potent anti-hypertensive agent. jNc-440 enhances the interaction between the transient receptor potential vanilloid subtype 4 (TRPV4) and calcium-activated potassium channel 3 (KCa2.3) in endothelial cells. jNc-440 also increases vasodilation and has hypotensive activity in mice.

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.

KCa2 channel modulator 1 (compound 2o) is an effective, subtype-selective K Ca2 channel positive modulator that potentiates rat KCa2.2 channels with an EC50 value of 0.99 μM and human KCa2.3 channels with an EC50 value of 0.19 μM [1].

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

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).

KCa2 channel modulator 2 (compound 2q) is an effective, subtype-selective K Ca 2 channel positive modulator with similar potency on the human K Ca 2.3 channel and rat K Ca 2.2a subtypes, exhibiting EC50 values of 0.60 μM and 0.64 μM, respectively [1].