Home / Inward Rectifier Potassium Channel Blockers / Tertiapin-Q

Tertiapin-Q

Catalog #: 1316
10 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
1316/1
Tertiapin-Q
1 Image
Description: Selective blocker of inward-rectifier K+ channels

Purity: ≥95%

Product Details
Citations (10)
Reviews
Biological Activity Technical Data Additional Information Background Product Datasheets Calculators

Biological Activity

Tertiapin-Q is a high affinity blocker for inward-rectifier K+ channels. Tertiapin-Q is a stable derivative of the bee venom toxin tertiapin. Tertiapin-Q 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. Tertiapin-Q improves heart rate and atrioventricular conduction in a mouse model of bradycardia. Derivative Tertiapin LQ (Cat. No. 4339) also available.

Technical Data

M.Wt:
2452
Formula:
C106H175N35O24S4
Sequence:
ALCNCNRIIIPHQCWKKCGKK

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

Solubility:
Soluble to 2 mg/ml in water
Purity:
≥95%
Storage:
Store 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Additional Information

Licensing Caveats:
Sold under license granted by the University of Pennsylvania

Background References

  1. Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart.
    Choisy SC, Cheng H, Smith GL, James AF, Hancox JC
    PLoS ONE, 2012;7(3):e33448.
  2. Acute desensitization of acetylcholine and endothelin-1 activated inward rectifier K+ current in myocytes from the cardiac atrioventricular node.

    Biochem. Biophys. Res. Commun., 2012;423(3):496-502.
  3. Nociceptin induces hypophagia in the perifornical and lateral hypothalamic area.
    Parsons, Matthew, Burt, Julia, Cranford, Amanda, Alberto, Christia, Zipperlen, Katrin, Hirasawa, Michiru
    PLoS ONE, 2012;7(9):e45350.
  4. Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q.
    Jin et al.
    Biochemistry, 1999;38:14294
  5. Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels.
    Jin and Lu
    Biochemistry, 1999;38:14286

Product Datasheets

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Citations for Tertiapin-Q

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

10 Citations: Showing 1 - 10

  1. Structural Determinants Mediating Tertiapin Block of Neuronal Kir3.2 Channels.
    Authors: Patel Et al.
    Biochemistry  2020;59:836
  2. Transmural Autonomic Regulation of Cardiac Contractility at the Intact Heart Level.
    Authors: Aguilar-Sanchez Et al.
    Front Physiol  2019;10:773
  3. Inactivation of GIRK channels weakens the pre- and postsynaptic inhibitory activity in dorsal raphe neurons.
    Authors: Llamosas Et al.
    Physiol Rep  2017;5
  4. Contribution of Kv7 channels to natriuretic peptide mediated vasodilation in normal and hypertensive rats.
    Authors: Stott Et al.
    Hypertension  2015;65:676
  5. 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
  6. Phasic DA release drives rapid activation of striatal D2-receptors.
    Authors: Marcott Et al.
    Neuron  2014;84:164
  7. Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro.
    Authors: Chu Et al.
    PLoS One  2013;8:e53863
  8. 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
  9. 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
  10. Sperm GIRK2-containing K+ inward rectifying channels participate in sperm capacitation and fertilization.
    Authors: Yi Et al.
    Syst Biol Reprod Med  2011;57:296

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