Tertiapin-Q

Research use only, not for human use.

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 also available.

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 also available.

Tertiapin-Q is a highly selective blocker of G protein-coupled inwardly rectifying potassium (GIRK1/4) heterodimer and renal outer medullary potassium channel (ROMK1, Kir1.1). Tertiapin-Q is a potent and selective blocker for Kir1.1 renal outer medullary potassium, Kir3.1-Kir3.4 channels and calcium activated large conductance potassium channels (big potassium channels). The somatostatin (SS-14)-activated current is almost completely blocked (93.2±2.9%, n=5; P<0.01) by preincubation with the G protein-coupled inwardly rectifying potassium (GIRK) channel blocker Tertiapin-Q (TPN-Q).

Tertiapin-Q is a muscarinic acetylcholine receptor-operated K+ current (IK,Ach) blocker. After the cessation of rapid atrial pacing, the atrial effective refractory period (AERP) is unchanged during the experimental period in the rapid atrial pacing (RAP) rabbits (n=6). Bepridil (1 mg/kg, n=5 for each group), Amiodarone (10 mg/kg, n=5 for each group), Vernakalant (3 mg/kg, n=5 for each group), Ranolazine (10 mg/kg, n=6 for each group) or Tertiapin-Q (0.03 mg/kg, n=5 for each group) on the AERP in the control and RAP rabbits. Tertiapin-Q significantly prolongs the AERP at each pacing cycle length both in the control and RAP rabbits. The extents of prolonging effect of Tertiapin-Q on the AERP in the RAP rabbits are greater than those in the control animals.

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Cell Cycle/DNA Damage

Potassium Channel

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910044-56-3

2452

C106H175N35O24S4

>98% (HPLC)

water:2 mg/mL

[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

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(-20℃)

With Ice Pack

≥ 2 years