Tertiapin-Q

Pricing Availability Delivery Time 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 (5)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 2 mg/ml in water

Preparing Stock Solutions

The following data is based on the product molecular weight 2452. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.41 mL 2.04 mL 4.08 mL
5 mM 0.08 mL 0.41 mL 0.82 mL
10 mM 0.04 mL 0.2 mL 0.41 mL
50 mM 0.01 mL 0.04 mL 0.08 mL

Molarity Calculator

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*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

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Dilution Calculator

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the products' biological activity.

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


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Keywords: Tertiapin-Q, supplier, Potent, selective, blockers, inward-rectifier, K+, channels, Potassium, KIR, Channels, venoms, Inward, rectifier, Potassium, Channels, Inward, rectifier, Potassium, Channels, Tocris Bioscience

5 Citations for Tertiapin-Q

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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