Pirmenol
Based on 1 Customer Validation
Pirmenol is an orally active antiarrhythmic agent. Pirmenol inhibits IK.ACh (IC50: 0.1 μM) by blocking mAchR. Pirmenol can be used in the research of cardiovascular disease, such as atrial fibrillation.
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: 99.32%
- CAS 番号: 68252-19-7
- 分子式: C22H30N2O
- 分子量:338.49
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
生物活性
IC50: 0.1 μM (IK.ACh)[1]
Pirmenol (1 μM) inhibits the IK.ACh induced by carbachol or intracellular loading of GTPg S in in atrial cells[1].
Pirmenol (5 μM) depresses the early part of the plateau and lengthened the final repolarization of the action potentials in ventricular myocytes[3].
Pirmenol (1 μM) prolongs the action potential duration at 90% repolarization in atrial muscles and Purkinje fibers[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pirmenol (rats) shows LD50s of 359.9 mg/kg (p.o), 23.6 mg/kg (i.v.)[2].
Pirmenol (mice) shows LD50s of 215.5 mg/kg (p.o), 20.8 mg/kg (i.v.)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Conscious, coronary artery ligated dogs[4]
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Dosage:Oral administration (p.o.)
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Administration:2.5 and 5 mg/kg
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Result:Restored normal sinus rhythm, and showed a long duration of activity, wide safety margin.
化学情報
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CAS 番号 68252-19-7
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性状 Solid
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分子量 338.49
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分子式 C22H30N2O
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Color Off-white to light yellow
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SMILES
OC(C1=CC=CC=C1)(CCCN2[C@@H](C)CCC[C@H]2C)C3=CC=CC=N3
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別名
(±)-Pirmenol; CI-845 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 8.33 mg/mL (24.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (275 KB)
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SDS (393 KB)
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- Portuguese - PT (393 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Watanabe Y, et al. Pirmenol inhibits muscarinic acetylcholine receptor-operated K+ current in the guinea pig heart. Eur J Pharmacol. 1997 Oct 29;338(1):71-4. [Content Brief]
[2]. Schardein JL, et al. Preclinical toxicology studies with a new antiarrhythmic agent: Pirmenol hydrochloride (CI-845). Toxicol Appl Pharmacol. 1980 Nov;56(2):294-301. [Content Brief]
[3]. T Sawanobori, et al. Electrophysiologic and antiarrhythmic actions of pirmenol on rabbit and guinea pig cardiac preparations. J Cardiovasc Pharmacol. 1990 Dec;16(6):975-83. [Content Brief]
[4]. T E Mertz, et al. Pirmenol hydrochloride (CI-845): antiarrhythmic profile in coronary artery ligated conscious dogs. J Cardiovasc Pharmacol. 1980 Sep-Oct;2(5):527-41. [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. 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9543 mL | 14.7715 mL | 29.5430 mL | 73.8574 mL |
| 5 mM | 0.5909 mL | 2.9543 mL | 5.9086 mL | 14.7715 mL | |
| 10 mM | 0.2954 mL | 1.4771 mL | 2.9543 mL | 7.3857 mL | |
| 15 mM | 0.1970 mL | 0.9848 mL | 1.9695 mL | 4.9238 mL | |
| 20 mM | 0.1477 mL | 0.7386 mL | 1.4771 mL | 3.6929 mL |