bkca-channel

GAL-021 an intravenous BKCa-channel blocker.

GAL-021 sulfate is a BKCa channel blocker that inhibits the analgesic effects of opioids and is used in the study of respiratory control diseases.

(±)-Naringenin (Naringenine) is a natural product. It displays vasorelaxant effect on endothelium-denuded vessels via the activation of BKCa channels in myocytes.

NS19504 is an activator of Ca2+-activated K+ channel with EC50 of 11.0 µM. NS19504 shows relaxing effect on bladder smooth muscle spontaneous phasic contractions[1].

Paxilline is an indole alkaloid mycotoxin from *Penicillium paxilli*, acting as a potent BK channel inhibitor via an almost exclusively closed-channel block mechanism. Paxilline possesses significant anticonvulsant activity.

KS176 is a potent and selective inhibitor of the breast cancer resistance protein (BCRP) multidrug transporter, exhibiting no inhibitory activity against P-gp or MRP1.

NS1619 have cardio-protective effects after ischemia-reperfusion injury.

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

17R(18S)-EpETE is an oxylipin and a cytochrome P450 metabolite of eicosapentaenoic acid. 17R(18S)-EpETE activates large-conductance calcium-activated potassium (BKCa) channels, increasing potassium current amplitude by 15-fold in isolated rat cerebral artery vascular smooth muscle cells at +60 mV at 50 nM. 17R(18S)-EpETE also exerts negative chronotropic effects in neonatal rat cardiomyocytes with an EC50 of ~1–2 nM and prevents calcium-induced increases in spontaneous beating. 17R(18S)-EpETE is therefore used in cardiovascular electrophysiology research systems to investigate ion channel modulation, lipid mediator signaling, and cardiac excitability regulation in cellular models.

BMS-191011 (BMS-A) is an activator of large-conductance calcium-activated potassium (BKCa) channels ,effective in stroke models

Eicosapentaenoic acid (EPA) is metabolized into epoxyeicosatetraenoic acids (EpETE) by multiple cytochrome P450 isoforms. The predominant compound of this epoxygenase pathway, (±)17(18)-EpETE, induces relaxation in vascular and airway smooth muscles through its action on large conductance Ca2+-activated K+ (BKCa) channels, specifically by binding to the BKα channel subunits. Another notable epoxygenase pathway derivative, (±)11(12)-EpETE, also generated from EPA via CYP450 activity in both in vitro and in vivo studies, has biological and physiological roles that are yet to be fully elucidated.

Martentoxin is a polypeptide toxin with a molecular weight of 4,046 Da, acting as an inhibitor of the large conductance Ca2+-activated K+ channel (BKCa channel). It can reduce TNF-α-induced NO release in HUVECs, inhibit iNOS activation, and upregulate eNOS mRNA expression. Martentoxin is applicable for vascular disease research.