Clevidipine-d5(Synonyms: 氯维地平 d5)

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Clevidipine-d5 (Synonyms: 氯维地平 d5)

Clevidipine-d5 是 Clevidipine 的氘代物。Clevidipine 是短效二氢吡啶钙离子通道拮抗剂,IC50为7.1 nM。

Clevidipine-d5(Synonyms: 氯维地平 d5)

Clevidipine-d5 Chemical Structure

CAS No. : 1346602-00-3

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生物活性

Clevidipine-d5 is the deuterium labeled Clevidipine. Clevidipine is a short-acting dihydropyridine calcium channel antagonist (IC50= 7.1 nM, V(H) = -40 mV ) under development for treatment of perioperative hypertension[1][2].

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

461.35

Formula

C21H18D5Cl2NO6

CAS 号

1346602-00-3

中文名称

氯维地平 d5

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]. Yi X, Vivien B, Lynch C 3rd. Clevidipine blockade of L-type Ca2+ currents: steady-state and kinetic electrophysiological studies in guinea pigventricular myocytes.

    [3]. Huraux C, Makita T, Szlam F, The vasodilator effects of clevidipine on human internal mammary artery. Anesth Analg. 1997 Nov;85(5):1000-4.

    [4]. Ericsson H, et al. In vitro hydrolysis rate and protein binding of clevidipine, a new ultrashort-acting calcium antagonist metabolised by esterases, in different animal species and man. Eur J Pharm Sci. 1999 Apr;8(1):29-37.

    [5]. Ericsson H, et al. Pharmacokinetics of new calcium channel antagonist clevidipine in the rat, rabbit, and dog and pharmacokinetic/pharmacodynamic relationship in anesthetized dogs. Drug Metab Dispos. 1999 May;27(5):558-64.

    [6]. Schwieler JH, et al. Circulatory effects and pharmacology of clevidipine, a novel ultra short acting and vascular selective calcium antagonist, in hypertensive humans. J Cardiovasc Pharmacol. 1999 Aug;34(2):268-74.

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