1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Tertiapin-Q

Tertiapin-Q 

Cat. No.: HY-P1275 Purity: 97.46%
Handling Instructions

Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).

For research use only. We do not sell to patients.

Tertiapin-Q Chemical Structure

Tertiapin-Q Chemical Structure

CAS No. : 910044-56-3

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1 mg USD 330 In-stock
Estimated Time of Arrival: December 31
5 mg USD 850 In-stock
Estimated Time of Arrival: December 31
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Description

Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).

IC50 & Target

Potassium channel[1]

In Vitro

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)[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)[2].

In Vivo

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[3].

Molecular Weight

2452.00

Formula

C₁₀₆H₁₇₅N₃₅O₂₄S₄

CAS No.

910044-56-3

Sequence

Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile-Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys-Lys-NH2 (Disulfide bridge: Cys3-Cys14, Cys5-Cys18)

Sequence Shortening

ALCNCNRIIIPHQCWKKCGKK-NH2 (Disulfide bridge: Cys3-Cys14, Cys5-Cys18)

SMILES

[Ala-Leu-Cys-Asn-Cys-Asn-Arg-Ile-Ile-Ile- Pro-His-Gln-Cys-Trp-Lys-Lys-Cys-Gly-Lys- Lys-NH2(Disulfide bridge: Cys3-Cys14, Cys5-Cys18)]

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -80°C 2 years
  -20°C 1 year
In solvent -80°C 6 months
  -20°C 1 month
References
Animal Administration
[3]

Rabbits[3]
Male New Zealand White rabbits weighing 3.0-3.5 kg are used for this study. Effects of Vernakalant, Ranolazine and Tertiapin-Q on the atrial effective refractory period (AERP) in the control and rapid atrial pacing (RAP) rabbits. Vernakalant (left panels, 3 mg/kg, n=5 for each group), Ranolazine (middle panels; 10 mg/kg, n=6 for each group) or Tertiapin-Q (right panels; 0.03 mg/kg, n=5 for each group) is intravenously administered to the control or RAP rabbits. AERP is measured before and 10 min after the administration of each drug, which are shown in the lower panels.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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