sk channels

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

ICA (N-[4-(2-Pyridinyl)-2-thiazolyl]-2-pyridinamine) is a SK channel inhibitor and exhibits antileishmanial activity (IC50: 2.1 µM).

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.

CyPPA, a subtype-selective positive modulator of SK channels, decreased spontaneous firing rate, increased the duration of the apamin-sensitive afterhyperpolarization.

NS4591 is a modulator of SK-IK channels.

Bicuculline is an alkaloid extracted from Corydalis decumbens, acting as a competitive antagonist of the neurotransmitter GABAA receptor (IC50 = 2 μM). It also blocks Ca2+-activated potassium (SK) channels and inhibits slow afterhyperpolarization (slow AHP). Bicuculline has anticonvulsant effects and is commonly used to establish mouse seizure models.

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).

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

Bupivacaine is a BK SK, Kv1, Kv3, TASK-2 K Channel and voltage-gated Na channel blocker used as an anesthetic. It maybe neurotoxic at high does, inducing apoptosis in neuroblastoma cells. It acts by binding to the intracellular portion of voltage-gated sodium channels and blocking sodium influx into nerve cells.

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.

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).

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.

Apamin (Apamine) is an 18 amino acid peptide neurotoxin found in apitoxin (bee venom) that selectively blocks Ca2+-activated K+ (SK) channels and exhibits anti-inflammatory and anti-fibrotic activity. This component of bee venom is strongly basic in nature.

Apamin acetate (Apamine acetate) is a selective Ca2+-activated blocker of K+ (SK) channels, an 18-amino acid peptide neurotoxin found in bee toxins.Apamin acetate enhances synapse growth and regeneration following laceration injury to cortical neurons.Apamin acetate has anti-inflammatory and anti-fibrotic effects.