Tertiapin-Q

Pricing Availability   Qty
Cat.No. 1316 - Tertiapin-Q | Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2 (Disulfide bridges: 3 - 14, 5 - 18) | CAS No. 910044-56-3
Description: Selective blocker of inward-rectifier K+ channels
Datasheet
Citations (8)
Reviews (1)
Literature

Biological Activity

A 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 Information

Sold under license granted by the University of Pennsylvania

Technical Data

M. Wt 2452
Formula C106H175N35O24S4
Sequence ALCNCNRIIIPHQCWKKCGKK

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

Storage Desiccate at -20°C
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

Solubility Soluble to 2 mg/ml in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

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


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

8 Citations for Tertiapin-Q

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

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

Stott et al (2015) Contribution of Kv7 channels to natriuretic peptide mediated vasodilation in normal and hypertensive rats. Hypertension 65 676 PMID: 25547342

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

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

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

Marcott et al (2014) Phasic dopamine release drives rapid activation of striatal D2-receptors. Neuron 84 164 PMID: 25242218


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Reviews for Tertiapin-Q

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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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Literature in this Area

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