Tertiapin-Q
Based on 3 publication(s) in Google Scholar
Tertiapin-Q is a highly selective blocker of GIRK1/4 heterodimer and ROMK1 (Kir1.1).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.81%
- CAS 番号: 910044-56-3
- 分子式: C106H175N35O24S4
- 分子量:2452.00
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保管条件:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
MedChemExpress(MCE)の使用を引用している文献 Tertiapin-Q
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生物活性
Potassium channel[1]
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 910044-56-3
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性状 Solid
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分子量 2452.00
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分子式 C106H175N35O24S4
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Color White to off-white
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配列
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)
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シーケンスの短縮
ALCNCNRIIIPHQCWKKCGKK-NH2 (Disulfide bridge: Cys3-Cys14, Cys5-Cys18)
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Chem Biol
Photo-cross-linking-assisted deorphanization deciphers GPR50-L-LEN pairing in metabolism. [Abstract]2026 Jan 6. PMID: 41495223 -
Psychopharmacology (Berl)
The effects of serotonergic psychedelics in synaptic and intrinsic properties of neurons in layer II/III of the orbitofrontal cortex. [Abstract]2023 Jun;240(6):1275-1285. PMID: 37071130 -
Physiol Rep
Ivabradine increases the high frequency gain ratio in the vagal heart rate transfer function via an interaction with muscarinic potassium channels. [Abstract]2021 Dec;9(23):e15134. PMID: 34889074
溶剤 & 溶解度
H2O : 50 mg/mL (20.39 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
プロトコル
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
純度とドキュメンテーション
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データシート (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Picton LD, et al. Mechanisms underlying the endogenous dopaminergic inhibition of spinal locomotor circuit function in Xenopus tadpoles. Sci Rep. 2016 Oct 20;6:35749. [Content Brief]
[2]. Günther T, et al. Research Resource: Real-Time Analysis of Somatostatin and Dopamine Receptor Signaling in Pituitary Cells Using a Fluorescence-Based Membrane Potential Assay. Mol Endocrinol. 2016 Apr;30(4):479-90. [Content Brief]
[3]. Chiba T, et al. Influences of rapid pacing-induced electrical remodeling on pharmacological manipulation of the atrial refractoriness in rabbits. J Pharmacol Sci. 2016 Mar;130(3):170-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 0.4078 mL | 2.0392 mL | 4.0783 mL | 10.1958 mL |
| 5 mM | 0.0816 mL | 0.4078 mL | 0.8157 mL | 2.0392 mL | |
| 10 mM | 0.0408 mL | 0.2039 mL | 0.4078 mL | 1.0196 mL | |
| 15 mM | 0.0272 mL | 0.1359 mL | 0.2719 mL | 0.6797 mL | |
| 20 mM | 0.0204 mL | 0.1020 mL | 0.2039 mL | 0.5098 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.