Catalog Number: 1316
Biological Activity
A high affinity blocker for inward-rectifier K+ channels, this compound is a stable derivative of the bee venom toxin tertiapin. Binds to ROMK1 (Kir1.1) and GIRK1/4 (Kir3.1/3.4) channels with high affinity (Ki values are 1.3 and 13.3 nM respectively) and is selective over Kir2.1 channels. Derivative tertiapin LQ (Cat. No. 4339) also available.
Technical Data
  • M.Wt:
    2452
  • Formula:
    C106H175N35O24S4
  • Sequence:
    ALCNCNRIIIPHQCWKKCGKK

    (Modifications: Disulfide bridge between 3 - 14, 5 - 18, Lys-21 = C-terminal amide)

  • Solubility:
    Soluble to 2 mg/ml in water
  • Storage:
    Desiccate at -20°C
  • CAS No:
    910044-56-3
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Additional Information
Licensing Caveats:
Sold under license granted by the University of Pennsylvania
Background References
  1. Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q.
    Jin et al.
    Biochemistry, 1999;38:14294
  2. Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels.
    Jin and Lu
    Biochemistry, 1999;38:14286
Citations:

The citations listed below are publications that use Tocris products. Selected citations for Tertiapin-Q include:

5 Citations: Showing 1 - 5
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  1. Rapid antidepressants stimulate the decoupling of GABAB receptors from GIRK/Kir3 channels through increased protein stability of 14-3-3η.
    Authors: Workman Et al.
    Mol Psychiatry 2015;20:298
  2. Phasic dopamine release drives rapid activation of striatal D2-receptors.
    Authors: Marcott Et al.
    Neuron 2014;84:164
  3. Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro.
    Authors: Chu Et al.
    PLoS One 2013;8:e53863
  4. Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart.
    Authors: Choisy Et al.
    PLoS One 2012;7:e33448
  5. Acute desensitization of acetylcholine and endothelin-1 activated inward rectifier K+ current in myocytes from the cardiac atrioventricular node.
    Authors: Choisy Et al.
    Biochem Biophys Res Commun 2012;423:496
Tocris Peptides
Description Application Cat# Citations Images  

Tertiapin LQ

4339  
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