Overview
Alomone Labs Trimethylapigenin inhibits KV1.5 channels expressed in Xenopus oocytes.A. Time course of KV1.5 plateau current amplitude elicited by 150 ms voltage step from holding potential of -80 mV to +50 mV, delivered every 10 seconds. Application of 150 µM Trimethylapigenin (#T-145) inhibits KV1.5 currents in a reversible manner (indicated by the horizontal bar). B. Representative current traces before and during application of 150 µM Trimethylapigenin as indicated.
- Liu, Y. et. al. (2012) Biochem. Pharmacol. 84, 498.
Trimethylapigenin is a natural flavone and a fully methylated derivate of apigenin, present in citrus, kaempferia parviflora, etc. Trimethylapigenin inhibits cardiac potassium currents. This compound blocks KV1.5 current in HEK 293 cell line (IC50 = 6.4 μM), and the ultra-rapid delayed rectify K+ current (IKur) in human atrial myocytes (IC50 = 8.0 μM) by binding to the open channels. In addition, trimethylapigenin decreased transient outward K+ current (Ito) in human atrial myocytes, inhibited acetylcholine-activated K+ current (IC50 = 6.8 μM) in rat atrial myocytes1.
It has been demonstrated that trimethylapigenin is effective in modulating bacterial drug resistance, and in α-glycosidase inhibition, anti-adipogenesis, anti-carcinoma, anti-inflammation, and chemoprevention. In addition, trimethylapigenin has been found to activate CFTR Cl− channels1.
