Cat. No. 1316
Biological ActivityA 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.
Licensing InformationSold under license granted by the University of Pennsylvania
(Modifications: Disulfide bridge between 3 - 14, 5 - 18, Lys-21 = C-terminal amide)
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.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Jin et al (1999) Mechanisms of inward-rectifier K+ channel inhibition by tertiapin-Q. Biochemistry 38 14294. PMID: 10572004.
Jin and Lu (1999) Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K+ channels. Biochemistry 38 14286. PMID: 10572003.
If you know of a relevant reference for this product please let us know.
Citations are publications that use Tocris products. Selected citations for Tertiapin-Q include:
Workman et al (2015) Rapid antidepressants stimulate the decoupling of GABAB receptors from GIRK/Kir3 channels through increased protein stability of 14-3-3η. Mol Psychiatry 20 298. PMID: 25560757.
Marcott et al (2014) Phasic dopamine release drives rapid activation of striatal D2-receptors. Neuron 84 164. PMID: 25242218.
Chu et al (2013) Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro. PLoS One 8 e53863. PMID: 23349753.
Choisy et al (2012) Acute desensitization of acetylcholine and endothelin-1 activated inward rectifier K+ current in myocytes from the cardiac atrioventricular node. Biochem Biophys Res Commun 423 496. PMID: 22683635.
Choisy et al (2012) Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart. PLoS One 7 e33448. PMID: 22479400.
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Keywords: Tertiapin-Q, supplier, Potent, selective, blockers, inward-rectifier, K+, channels, Potassium, KIR, Channels, Tocris Bioscience, Inward Rectifier Potassium (Kir) Channel Blocker products
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