Chromanol 293B is a blocker of slowly activating delayed-rectifier K+ current (IKs) with an IC50 value of 6.89 μM in Xenopus oocytes expressing rat IKs channels. It is selective, having no activity at rat Kv1.1 or Kir2.1 channels at a concentration of 30 μM. Chromanol 293B increases the rate and extent of IKs in guinea pig ventricular cells in a dose-dependent manner. It also inhibits cystic fibrosis transmembrane conductance regulator (CTFR) Cl- currents (ICTFR) with an IC50 value of 19 μM in Xenopus oocytes expressing human CTFR.
용도
Chromanol 293B has been used in the inhibition of calcium and cyclic adenosine monophosphate (cAMP)-activated potassium channels in human epithelial cell lines. Chromanol 293B has been used in patch-clamp electrophysiology studies in cardiomyocytes.
일반 설명
Chromanol 293B enantiomer is a potent inhibitor of potassium channel protein (KvLQT1). In human atrial myocytes, chromanol 293B inhibits repolarization potassium currents. Chromanol 293B improves glucose-stimulated insulin secretion (GSIS) in pancreas by modulating potassium voltage-gated channel (KCNQ1).
생물학적 활성
Blocker of the slow delayed rectifier K + current (I Ks ) (IC 50 = 1-10 μ M). Also blocks the CFTR chloride current (I CFTR ) (IC 50 = 19 μ M).