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Tertiapin

TPN
A Blocker of Inward Rectifier (Kir) K+ Channels
    Cat #: STT-250
    Alternative Name TPN
  • Lyophilized Powder
  • 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.
      • Tertiapin
    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.
    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.
      • Tertiapin
        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.

      • 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
    Net Peptide Content: 100%
    Lyophilized Powder
    receive a 0.1 mg free trial sample!
    Last update: 18/02/2020

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

    For research purposes only, not for human use
    Citations
      • Skov, J. et al. (2011) Cell. Mol. Neurobiol. 31, 587.
      • Farhang, B. et al. (2010) Neuropharmacology 59, 190.
      • Leuranguer, V. et al. (2008) Br. J. Pharmacol. 153, 57.
      • Russo, M.J. et al. (2008) J. Neurophysiol. 100, 3351.
      • Witkowski, G. et al. (2008) Neuroscience 155, 53.
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