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Submit ReviewTertiapin-Q
Description: Selective blocker of inward-rectifier K+ channels
Purity: ≥95% (HPLC)
Biological Activity for Tertiapin-Q
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.
Licensing Information
Sold under license granted by the University of Pennsylvania
Technical Data for Tertiapin-Q
| M. Wt | 2452 |
| Formula | C106H175N35O24S4 |
| Sequence |
ALCNCNRIIIPHQCWKKCGKK (Modifications: Disulfide bridges: 3-14, 5-18, Lys-21 = C-terminal amide) |
| Storage | Store at -20°C |
| Purity | ≥95% (HPLC) |
| CAS Number | 910044-56-3 |
| PubChem ID | 90479782 |
| InChI Key | GMZAXHIZSCRCHM-MIPBWYARSA-N |
| Smiles | [H]N[C@@H](C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H]1CSSC[C@@H]2NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC3=CNC=N3)NC(=O)[C@@H]3CCCN3C(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC3=CNC4=C3C=CC=C4)NC2=O)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCCCN)C(N)=O)NC(=O)[C@H](CC(N)=O)NC1=O)[C@@H](C)CC)[C@@H](C)CC)[C@@H](C)CC |
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.
Solubility Data for Tertiapin-Q
| Solubility | Soluble to 2 mg/ml in water |
Product Datasheets for Tertiapin-Q
References for Tertiapin-Q
References are publications that support the biological activity of the product.
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
Bidaud et al (2020) Inhibition of G protein-gated K + channels by tertiapin-Q rescues sinus node dysfunction and atrioventricular conduction in mouse models of primary bradycardia Sci.Rep. 10 9835 PMID: 32555258
If you know of a relevant reference for Tertiapin-Q, please let us know.
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Keywords: Tertiapin-Q, Tertiapin-Q supplier, Potent, selective, blockers, inward-rectifier, K+, channels, Potassium, KIR, Channels, venoms, Inward, rectifier, 1316, Tocris Bioscience
10 Citations for Tertiapin-Q
Citations are publications that use Tocris products. Selected citations for Tertiapin-Q include:
Llamosas et al (2017) Inactivation of GIRK channels weakens the pre- and postsynaptic inhibitory activity in dorsal raphe neurons. Physiol Rep 5 PMID: 28196855
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
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 DA release drives rapid activation of striatal D2-receptors. Neuron 84 164 PMID: 25242218
Patel et al (2020) Structural Determinants Mediating Tertiapin Block of Neuronal Kir3.2 Channels. Biochemistry 59 836 PMID: 31990535
Chu et al (2013) Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro. PLoS One 8 e53863 PMID: 23349753
Yi et al (2011) Sperm GIRK2-containing K+ inward rectifying channels participate in sperm capacitation and fertilization. Syst Biol Reprod Med 57 296 PMID: 22054410
Aguilar-Sanchez et al (2019) Transmural Autonomic Regulation of Cardiac Contractility at the Intact Heart Level. Front Physiol 10 773 PMID: 31333477
Stott et al (2015) Contribution of Kv7 channels to natriuretic peptide mediated vasodilation in normal and hypertensive rats. Hypertension 65 676 PMID: 25547342
Do you know of a great paper that uses Tertiapin-Q from Tocris? Please let us know.
Reviews for Tertiapin-Q
Average Rating: 5 (Based on 2 Reviews.)
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Works as expected..
By
Anonymous on 05/26/2020
Species: Mouse
Cell Line/Tissue: Bed nucleus of the stria terminalis
We performed ex-vivo slice physiology and pre-incubated the slices in tertiapin-Q (200 nM). Pre-incubation blocked inward rectifying channels.
Tertiapin-Q is a very potent Kir channel blocker even at low concentrations.
By
Anonymous on 10/31/2018
Assay Type: In Vitro
Species: Human
The product shows great Kir channel blocking properties even at very small cocentrations, the data was reproducible every time.
