标签归档：amiodarone

Desethyl Amiodarone-d4 hydrochloride

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Desethyl Amiodarone-d4 hydrochloride 

Desethyl Amiodarone-d4 hydrochloride 是 Desethylamiodarone hydrochloride 的氘代物。Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) 是 Amiodarone 的主要活性代谢产物。Desethylamiodarone hydrochloride 是由 CYP3A 同工酶形成的。Amiodarone 是一种抗心律失常药，用于抑制 ATP 敏感性钾通道，IC50 为 19.1 μM。

Desethyl Amiodarone-d4 hydrochloride

Desethyl Amiodarone-d4 hydrochloride Chemical Structure

CAS No. : 1189960-80-2

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生物活性

Desethyl Amiodarone-d4 hydrochloride is the deuterium labeled Desethylamiodarone hydrochloride. Desethylamiodarone hydrochloride (N-desethylamiodarone hydrochloride) is a major active metabolite of Amiodarone. Desethylamiodarone hydrochloride is formed by CYP3A isoenzymes. Amiodarone is an antiarrhythmic agent for inhibition of ATP-sensitive potassium channel with an IC50 of 19.1 μM[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

657.74

Formula

C23H22D4ClI2NO3
CAS 号

1189960-80-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Shayeganpour A, et al. Determination of the enzyme(s) involved in the metabolism of amiodarone in liver and intestine of rat: the contribution of cytochrome P450 3A isoforms. Drug Metab Dispos. 2006 Jan;34(1):43-50.

    [3]. Singh, B.N. and E.M. Vaughan Williams, The effect of amiodarone, a new anti-anginal drug, on cardiac muscle. Br J Pharmacol, 1970. 39(4): p. 657-67.

    [4]. Rosenbaum, M.B., et al., Clinical efficacy of amiodarone as an antiarrhythmic agent. Am J Cardiol, 1976. 38(7): p. 934-44.

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