Dicoumarol-d8(Synonyms: Dicumarol-d8)

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Dicoumarol-d8 (Synonyms: Dicumarol-d8)

Dicoumarol-d8 (Dicumarol-d8) 是 Dicoumarol 的氘代物。Dicoumarol 是 NAD(P)H: 醌氧化还原酶 1 (NQO1) 和 PDK1 的抑制剂,IC50 值分别为 0.37 和 19.42 μM。

Dicoumarol-d8(Synonyms: Dicumarol-d8)

Dicoumarol-d8 Chemical Structure

CAS No. : 2469035-18-3

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生物活性

Dicoumarol-d8 (Dicumarol-d8) is the deuterium labeled Dicoumarol. Dicoumarol is an inhibitor of both NAD(P)H:quinone oxidoreductase 1 (NQO1) and PDK1 with IC50s of 0.37 and 19.42 μM, respectively.

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

344.34

Formula

C19H4D8O6

CAS 号

2469035-18-3

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]. Bian J, et al. Affinity-based small fluorescent probe for NAD(P)H:quinone oxidoreductase 1 (NQO1). Design, synthesis and pharmacological evaluation. Eur J Med Chem. 2017 Feb 15;127:828-839.

    [3]. Zhang W, et al. Dicumarol inhibits PDK1 and targets multiple malignant behaviors of ovarian cancer cells. PLoS One. 2017 Jun 15;12(6):e0179672.

    [4]. Fiorillo M, et al. Mitochondrial “power” drives tamoxifen resistance: NQO1 and GCLC are new therapeutic targets in breast cancer. Oncotarget. 2017 Mar 2;8(12):20309-20327.

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