kca1.1

GAL-021 an intravenous BKCa-channel blocker.

KCa1.1 Channel Activator-1, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels while also blocking CaV1.2 channels. Additionally, it demonstrates weak myorelaxant activity.

KCa1.1 channel activator-2, a hybrid derivative of Quercetin, selectively stimulates the vascular KCa1.1 channels. This compound demonstrates significant myorelaxant activity.

NS 11021 (NS11021) , a novel opener of large-conductance Ca(2+)-activated K(+) channels

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

Flufenamic acid-d4 is intended for use as an internal standard for the quantification of flufenamic acid by GC- or LC-MS. Flufenamic acid is a non-steroidal anti-inflammatory drug (NSAID) and COX inhibitor (IC50s = 3 and 9.3 µM for human COX-1 and COX-2, respectively). Flufenamic acid inhibits TNF-α-induced increases in COX-2 levels and NF-κB activation in HT-29 colon cancer cells in a concentration-dependent manner. It inhibits calcium influx induced by fMLP or A23187 in human polymorphonuclear leukocytes (PMN) with IC50 values of 29 and 14 µM, respectively. Flufenamic acid also activates various ion channels, including transient receptor potential canonical 6 (TRPC6) and the large-conductance calcium-activated potassium channel (KCa1.1). It also inhibits various ion channels, including TRPC3 and the cystic fibrosis transmembrane conductance regulator (CFTR). Flufenamic acid (20 mg kg) reduces increases in intestinal fluid secretion and intestinal barrier disruption in mice ......

(±)13,14-EDT, an oxylipin metabolite derived from adrenic acid through the cytochrome P450 (CYP) pathway, acts as a potent activator of large-conductance calcium-activated potassium channels (KCa1.1/BK) in isolated rat coronary small arterial smooth muscle cells at 50 nM, promoting dilation. Additionally, it induces arteriole dilation in isolated porcine samples with an EC50 of 12 pM and relaxes isolated bovine coronary arteries previously contracted by TP receptor agonist U-46619.

5(6)-DiHET is a racemic compound synthesized through the action of epoxide hydrolases on 5(6)-EET, encompassing both enantiomeric forms. It serves as a quantitative marker for 5(6)-EET, facilitating its measurement by utilizing the compound's conversion to 5(6)-δ-lactone in solution. Additionally, 5(6)-DiHET activates large-conductance calcium-activated potassium (KCa1.1/BK) channels in rat small coronary artery smooth muscle cells, supporting its biological significance in vascular regulation. It also acts as a substrate for sheep seminal vesicle COX, leading to the in vitro production of 5,6-dihydroxy prostaglandin E1 and F1α metabolites. Notably, its levels diminish in the plasma of rats subjected to a high-fat diet, indicating a potential role in the pathophysiology of hyperlipidemia.