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Tertiapin

TPN

A Blocker of Inward Rectifier (Kir) K+ Channels

Cat #: STT-250
Alternative Name TPN
Lyophilized Powder yes
  • Bioassay Tested
    • Origin Synthetic peptide
    MW: 2455 Da
    Purity: >98% (HPLC)
    Effective concentration 10-100 nM.
    Sequence ALCNCNRIIIPHMCWKKCGKK.
    Modifications Disulfide bonds between Cys3-Cys14, and Cys5-Cys18. Lys21 - C-terminal amidation.
    Structure
    Molecular formula C106H176N34O23S5.
    CAS No.: 58694-52-3
    Activity Tertiapin blocks a range of inward rectifier K+ channels (Kir) in particular ROMK1 and GIRK but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine induced K+ currents in the heart2,3.
    References-Activity
    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) Pharmacol. Exp. Therap. 293, 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.
    Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to two weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Tertiapin inhibits Kir3.2 channels expressed in Xenopus oocytes.
      Alomone Labs Tertiapin inhibits Kir3.2 channels expressed in Xenopus oocytes.
      A continuous current trace recorded at a holding potential of -80 mV. Channel activation was achieved by high K+ solution perfusion. 50 nM Tertiapin (#STT-250) was applied during the period (2 minutes each) marked as a green trace.
    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. Therap. 293, 196.
    4. Jin, W. et al. (1999) Biochemistry 38, 14294.
    Scientific background

    Tertiapin is a 21 amino acid long toxin, originally isolated from Apis mellifera bee venom. Native and synthetic Tertiapin block 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 is 8.6 nM) but with no effect on Kir2 family members1. In addition, it was shown to inhibit acetylcholine-induced K+ currents in the heart2,3.

    Tertiapin is as active as Tertiapin-Q (#STT-170), a derivative of Tertiapin in which the oxidation-liable methionine is replaced by a glutamine residue4.

    Target Kir1.1, Kir3.2 K+ channels
    Peptide Content: 100%
    Lyophilized Powder
    Last update: 02/01/2022

    Tertiapin (#STT-250) is a highly pure, synthetic, and biologically active peptide toxin.

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    For research purposes only, not for human use

    Applications

    Citations

    Citations
    Product citations
    1. Skov, J. et al. (2011) Cell. Mol. Neurobiol. 31, 587.
    2. Farhang, B. et al. (2010) Neuropharmacology 59, 190.
    3. Leuranguer, V. et al. (2008) Br. J. Pharmacol. 153, 57.
    4. Russo, M.J. et al. (2008) J. Neurophysiol. 100, 3351.
    5. Witkowski, G. et al. (2008) Neuroscience 155, 53.

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