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Trimethylapigenin

A Blocker of KV1.5 and KV11.1 and an Activator of CFTR Channels

Cat #: T-145
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 312.3
    Purity: >96%
    Form Lyophilized powder.
    Effective concentration 1-200 µM.
    Structure
    Chemical name 5,7-dimethoxy-2-(4-methoxyphenyl)chromen-4-one.
    Molecular formula C18H16O5.
    CAS No.: 5631-70-9
    Activity Trimethylapigenin blocks KV1.5 and hERG channels with IC50 ~ 8 and 30 μM respectively. It also activates CFTR channels1.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 50 mM in DMSO. Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Trimethylapigenin inhibits KV1.5 channels expressed in Xenopus oocytes.
      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.
    References - Scientific background
    1. Liu, Y. et. al. (2012) Biochem. Pharmacol. 84, 498.
    Scientific background

    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.

    Target KV1.5, KV11.1, CFTR channels
    Lyophilized Powder
    Last update: 02/03/2021

    Trimethylapigenin (#T-145) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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