產品屬性：
產品名稱 | Amiodarone-d4 (hydrochloride) |
規格 | 1 mg、5 mg |
貨號 | EY-01Y16149 |
Cas No.: 1216715-80-8
別名: N/A
化學名: N/A
分子式: C25H25D4I2NO3.HCl
分子量: 685.8
溶解度: DMF: 10 mg/ml,DMSO: 10 mg/ml,Ethanol: 5 mg/ml
儲存條件: Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
產品描述：
Amiodarone-d4 is intended for use as an internal standard for the quantification of amiodarone by GC- or LC-MS. Amiodarone is a class III antiarrhythmic agent, in that it prolongs both cardiac action potential and refractoriness by blocking potassium currents.1 It inhibits the voltage-gated potassium channel hERG, also known as KCNH2, with an IC50 value of 1 μM.2 In addition, amiodarone binds with high affinity to the sigma-1 opioid receptor, 3-β-hydroxysteroid δ8δ7 isomerase, and C-8 sterol isomerase (Kis = 1, 25, and 62 nM, respectively) and inhibits human thyroid hormone receptors α and β (IC50s = 0.6 and 0.65 μM, respectively).3,4 It also inhibits the cytochrome P450 (CYP) isoforms CYP2C8 and CYP3A4 in vitro at low micromolar concentrations.51.Campbell, T.J., and Williams, K.M.Therapeutic drug monitoring: Antiarrhythmic drugsBr. J. Clin. Pharmacol.52307-319(1998)
2.Sinha, N., and Sen, S.Predicting hERG activities of compounds from their 3D structures: Development and evaluation of a global descriptors based QSAR modelEur. J. Med. Chem.46(2)618-630(2011)
3.Laggner, C., Schieferer, C., Fiechtner, B., et al.Discovery of high-affinity ligands of σ1 receptor, ERG2, and emopamil binding protein by pharmacophore modeling and virtual screeningJ. Med Chem.48(15)4754-4764(2005)
4.Carlsson, B., Singh, B.N., Temciuc, M., et al.Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodaroneJournal of Medicinal Chemistry45(3)623-630(2002)
5.Polasek, T.M., Elliott, D.J., Lewis, B.C., et al.Mechanism-based inactivation of human cytochrome P4502C8 by drugs in vitroJ. Pharmacol. Exp. Ther.311(3)996-1007(2004)
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