Tertiapin-Q

Pricing Availability   Qty
Description: Selective blocker of inward-rectifier K+ channels
Purity: ≥95% (HPLC)
Datasheet
Citations (10)
Reviews (2)

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

Certificate of Analysis / Product Datasheet
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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.

View Related Products by Product Action

View all Inward Rectifier Potassium (Kir) Channel Blockers

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:

Chu et al (2013) Effects of stresscopin on rat hypothalamic paraventricular nucleus neurons in vitro. PLoS One 8 e53863 PMID: 23349753

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

Aguilar-Sanchez et al (2019) Transmural Autonomic Regulation of Cardiac Contractility at the Intact Heart Level. Front Physiol 10 773 PMID: 31333477

Llamosas et al (2017) Inactivation of GIRK channels weakens the pre- and postsynaptic inhibitory activity in dorsal raphe neurons. Physiol Rep 5 PMID: 28196855


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.

PMID: 30795004
review image

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.

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