Tertiapin-Q

Name: Tertiapin-Q
Brand: Tocris Bioscience
SKU: 1316
Rating: 5 (2 reviews)

Catalog # 1316 | Tocris Bioscience a Bio-Techne Brand

(2)

Citations (10)

COA / SDS

Selective blocker of inward-rectifier K+ channels

Key Product Details

Description:	Selective blocker of inward-rectifier K⁺ channels
Purity:	≥95% (HPLC)
Molecular Weight:	2452

View Full Technical Details for Tertiapin-Q

Technical Data
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 (K_ir1.1) and GIRK1/4 (K_ir3.1/3.4) channels with high affinity (K_i values are 1.3 and 13.3 nM respectively) and is selective over K_ir2.1 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
Single Letter 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 for Tertiapin-Q

Solubility

Soluble to 2mg/ml in water

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References for Tertiapin-Q

References are publications that support the biological activity of the product.

Bidaud 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. 2020 PMID: 32555258
Jin Mechanisms of inward-rectifier K⁺ channel inhibition by tertiapin-Q. Biochemistry 1999 PMID: 10572004
Jin and Lu Synthesis of a stable form of tertiapin: a high-affinity inhibitor for inward-rectifier K⁺ channels. Biochemistry 1999 PMID: 10572003

Citations for Tertiapin-Q (10)

Showing 1 - 10 of 10 citations Showing All

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Citations are publications that use Bio-Techne products. Selected citations for Tertiapin-Q include:

Patel et al. (2020) Structural Determinants Mediating Tertiapin Block of Neuronal Kir3.2 Channels. Biochemistry. 59:836
PMID: 31990535
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
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
Stott et al. (2015) Contribution of Kv7 channels to natriuretic peptide mediated vasodilation in normal and hypertensive rats. Hypertension. 65:676
PMID: 25547342
Marcott et al. (2014) Phasic DA 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) Modulation by endothelin-1 of spontaneous activity and membrane currents of atrioventricular node myocytes from the rabbit heart. PLoS One. 7:e33448
PMID: 22479400
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
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

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Customer Reviews for Tertiapin-Q (2)

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Works as expected.

Name: Anonymous

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
Tertiapin-Q is a very potent Kir channel blocker even at low concentrations

Name: Anonymous

Species: Human

Assay Type: In Vitro

The product shows great Kir channel blocking properties even at very small cocentrations, the data was reproducible every time.

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