An Inward Rectifier K+ Channel Blocker Conjugated to the Fluorescent Dye ATTO-633
    Cat #: STT-170-FR
  • Lyophilized Powder
  • Bioassay Tested
  • Origin Synthetic peptide
    MW: 3159.6 Da.
    Purity: >95%
    Effective concentration 50-200 nM.
    Modifications Disulfide bonds between Cys3-Cys14, Cys5-Cys18. Lys21- C-terminal amidation.
    Label ATTO-633. ATTO dyes are characterized by strong absorption (high extinction coefficient), high fluorescence quantum yield, and high photo-stability. ATTO-633 has a maximum absorption at 629 nm and  a maximum fluorescence at 657 nm. The fluorescence is excited most efficiently in the range 610 to 645 nm. This label is analogous to the well known dye Alexa 647, Alexa 633 and Cy5. The extent of labeling is one molecule of dye per molecule of Tertiapin-Q.
    • Tertiapin-Q-ATTO-633
    Activity Tertiapin-Q blocks a range of inward rectifier K+ channels (Kir), in particular ROMK1 and GIRK, but with no effect on Kir2 family members1,2. In addition, it was shown to inhibit acetylcholine induced K+ currents in the heart3,4.
    1. Jin, W. and Lu, Z. (1998) Biochemistry 37, 13291.
    2. Jin, W. et al. (1999) Biochemistry 38, 14294.
    3. Drici, M.D. et al. (2000) Br. J. Pharmacol131, 569.
    4. Kitamura, H. et al. (2000) Pharmacol. Exp. Ther293, 196.
    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. Avoid exposure to light.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min). Avoid exposure to light. The product is lyophilized in 0.5 ml conical vial.
    Storage of solutions Up to two weeks at 4°C or three months at -20°C. Avoid exposure to light.
    Our bioassay
    • Tertiapin-Q-ATTO-633
      Alomone Labs Tertiapin-Q-ATTO-633 binds GIRK1/GIRK4-GFP transfected HEK293T cells.
      Living cells were incubated in the presence of 100 nM Tertiapin-Q-ATTO-633 (#STT-170-FR). A. Visible light of cells. B. GIRK1/GIRK4-GFP transfected cells (green). C. Tertiapin-Q-ATTO-633 (red).  
      The pictures are a kind gift from the lab of Prof. Eithan Reuveny, Weizmann Institute, Israel.
    • Tertiapin-Q-ATTO-633
      Alomone Labs Tertiapin-Q-ATTO-633 inhibits Kir3.2 channel heterologously expressed in Xenopus oocytes.
      A continuous current trace recorded at a holding potential of -80 mV. Kir3.2 currents are downward reflections activated by high Kcontaining solution. While activated, 50 nM and 100 nM of Tertiapin-Q-ATTO-633 (#STT-170-FR) were applied for 2 min (indicated as bars).
    References - Scientific background
    1. Jin, W. and Lu, Z. (1998) Biochemistry 37, 13291.
    2. Drici, M.D. et al. (2000) Br. J. Pharmacol. 131, 569.
    3. Kitamura, H. et al. (2000) J. Pharmacol. Exp. Ther. 293, 196.
    4. Peleg, S. et al. (2002) Neuron 33, 87.
    5. Kanjhan, R. et al. (2005) J. Pharmacol. Exp. Ther. 314, 1353.
    Scientific background

    Tertiapin, the native toxin, was originally isolated from European honey bee Apis mellifera venom. Native and synthetic Tertiapin blocks a range of inward rectifier K+ channels (Kir), in particular ROMK1 (Kir1.1, IC50 = 2 nM) and GIRK (Kir3 family, IC50 for the Kir3.1/3.4 heteromer was 8.6 nM) but with no effect on the Kir2 family member1. In accordance, it was shown to inhibit acetylcholine induced K+ currents in mammalian cardiomyocytes2,3.

    Tertiapin-Q is a derivative of Tertiapin in which Met13 is substituted by a Gln residue. However, unlike native Tertiapin, Tertiapin-Q is non-oxidizable and therefore is more stable4.

    Tertiapin-Q inhibits the above-mentioned channels with similar affinities and also inhibits Ca2-activated large conductance BK-type K+ channels in a concentration and voltage-dependent manner5.

    Target Kir1.1, Kir3.2 Kchannels
    Net Peptide Content: 100%
    Last update: 24/01/2020

    Tertiapin-Q-ATTO-633 (#STT-170-FR) is a highly pure, synthetic, and biologically active conjugated peptide toxin.

    We gladly take on collaboration projects. Please Contact Us.

    For research purposes only, not for human use
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