bkca α

BKCa activator-1 (Compound 51b) is an orally active activator of BKCa calcium-activated potassium channels with an EC50 of 2.82 μM. It promotes K+ efflux, leading to cell membrane hyperpolarization and inhibition of smooth muscle contraction. In a spontaneous hypertensive rat (SHR) model, it alleviates urinary incontinence and exhibits antitussive effects in a guinea pig cough model.

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.

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.