Ketoconazole-d8(Synonyms: 酮康唑 d8)

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Ketoconazole-d8 (Synonyms: 酮康唑 d8)

Ketoconazole-d8 是 Ketoconazole 的氘代物。Ketoconazole (R-41400) 是咪唑类抗真菌剂,是经典的CYP3A4抑制剂,也是 CYP24A1的抑制剂。

Ketoconazole-d8(Synonyms: 酮康唑 d8)

Ketoconazole-d8 Chemical Structure

CAS No. : 1217706-96-1

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生物活性

Ketoconazole-d8 is the deuterium labeled Ketoconazole. Ketoconazole (R-41400) is an imidazole anti-fungal agent, a CYP3A4 and CYP24A1 inhibitor.

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

539.48

Formula

C26H20D8Cl2N4O4

CAS 号

1217706-96-1

中文名称

酮康唑 d8

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]. Seif El-Din SH, et al. Effect of ketoconazole, a cytochrome P450 inhibitor, on the efficacy of quinine and halofantrine against Schistosoma mansoni in mice. Korean J Parasitol. 2013 Apr;51(2):165-75.

    [3]. Eil C. Ketoconazole binds to the human androgen receptor. Horm Metab Res. 1992 Aug;24(8):367-70.

    [4]. Muindi JR et al. CYP24A1 inhibition enhances the antitumor activity of calcitriol. Endocrinology. 2010 Sep;151(9):4301-12.

    [5]. Amrita Datta, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161.

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