Name: Tertiapin-Q
Brand: Alomone Labs
SKU: STT-170

Cat #: STT-170

Lyophilized Powder yes

Bioassay Tested

Origin Synthetic peptide

MW: 2452 Da

Purity: >98% (HPLC)

Effective concentration 2-200 nM.

Sequence ALCNCNRIIIPHQCWKKCGKK.

Modifications Disulfide bonds between Cys³-Cys¹⁴, Cys⁵-Cys¹⁸. Lys²¹ - C-terminal amidation.

Structure

Molecular formula C₁₀₆H₁₇₅N₃₅O₂₄S₄.

CAS No.: 910044-56-3

Activity Tertiapin-Q blocks a range of inward rectifier K⁺ channels (K_ir), in particular ROMK1 and GIRK, but with no effect on K_ir2 family members¹. In addition, it was shown to inhibit acetylcholine induced K⁺ currents in heart^2,3. Tertiapin-Q is a derivative of Tertiapin in which Met¹³ is replaced by Gln. Tertiapin-Q inhibits the above-mentioned channels with similar affinities⁴.

References-Activity

Jin, W. and Lu, Z. (1998) Biochemistry 37, 13291.
Drici, M.D. et al. (2000) Br. J. Pharmacol. 131, 569.
Kitamura, H. et al. (2000) J. Pharmacol. Exp. Ther. 293, 196.
Jin, W. et al. (1999) Biochemistry 38, 14294.

Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.

Solubility Any aqueous buffer. Centrifuge all product preparations before use (10000 x g 5 min).

Storage of solutions Up to one week at 4°C or three months at -20°C.

Our bioassay

Alomone Labs Tertiapin-Q inhibits K_ir3.2 channel heterologously expressed in Xenopus oocytes.
A continuous current trace recorded at a holding potential of -80 mV. K_ir3.2 currents are downward reflections activated by high K⁺ containing solution. While activated, increasing concentrations of Tertiapin-Q (#STT-170) were applied (arrows at the bottom of the trace).

Scientific background

Tertiapin, the native toxin, was originally isolated from European honey bee Apis mellifera venom. Native and synthetic Tertiapin blocks a range of inward rectifier K⁺ channels (K_ir), in particular ROMK1 (K_ir1.1, IC₅₀= 2 nM) and GIRK (K_ir3 family, IC₅₀ for the K_ir3.1/3.4 heteromer was 8.6 nM) but with no effect on the K_ir2 family member¹. In accordance, it was shown to inhibit acetylcholine induced K⁺ currents in mammalian cardiomyocytes^2,3.

Tertiapin-Q is a derivative of Tertiapin in which Met¹³ is substituted by a Gln residue. However, unlike native Tertiapin, Tertiapin-Q is non-oxidizable and therefore is more stable⁴.

Tertiapin-Q inhibits the above-mentioned channels with similar affinities and also inhibits Ca²-activated large conductance BK-type K⁺ channels in a concentration and voltage-dependent manner⁵.

Target K_ir1.1, K_ir3.2 K⁺channels

Peptide Content: 100%

Lyophilized Powder

Image & Title

Alomone Labs Tertiapin-Q blocks time-dependent hyperpolarization-activated current (I_KH) in rat atrial cardiomyocytes.Whole-cell voltage-clamp was performed on neonatal rat atrial cardiomyocyte (NRAM) primary cultures. A. The voltage-clamp recordings depict large inward currents evoked by hyperpolarizations (5 sec), whereas, very little current is activated during steps to -50 mV and more positive potentials. Na⁺ current (I_Na) and T-type Ca²⁺ current (I_CaT) are inactivated by holding the cells at the potential of -40 mV. B. In the presence of Tertiapin-Q (#STT-170) (100 nM), which selectively suppresses the constitutively active acetylcholine (ACh)-mediated K⁺ current I_KACh-c component of I_KH, only inward rectifier current (I_K1) is left with K⁺ leak.Adapted from Majumder, R. et al. (2016) PLoS Comput. Biol. 12, e1004946. with permission of PLoS.

Last update: 11/12/2022

For research purposes only, not for human use

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Scientific Background

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Tertiapin-Q

Specifications

Citations

Applications

Scientific Background

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