Ticlopidine-d4(Synonyms: PCR 5332-d4)

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Ticlopidine-d4 (Synonyms: PCR 5332-d4)

Ticlopidine-d4 (PCR 5332-d4) 是 Ticlopidine 的氘代物。Ticlopidine (PCR 5332) 是一种抗血栓前药，作为非竞争性的变构 CD39 抑制剂，IC50 为 81.7 µM。Ticlopidine 阻断 NTPDase 同工酶，对 NTPDase2 和 NTPDase3 的 IC50 分别为 170 µM 和 149 µM。Ticlopidine 是 CYP2C19 人肝细胞色素的抑制剂。Ticlopidine 抑制 CYP2C9 和 CYP3A4，IC50 值分别为 26.0 和 32.3 μM。

Ticlopidine-d4(Synonyms: PCR 5332-d4)

Ticlopidine-d4 Chemical Structure

CAS No. : 1246817-49-1

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生物活性

Ticlopidine-d4 (PCR 5332-d4) is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic prodrug, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 µM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 µM and 149 µM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[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

267.81

Formula

C14H10D4ClNS
CAS 号

1246817-49-1
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]. Laura Schäkel, et al. 2-Substituted thienotetrahydropyridine derivatives: Allosteric ectonucleotidase inhibitors. Arch Pharm (Weinheim). 2021 Dec;354(12):e2100300.

    [3]. I.KRASLOVA1, et al. Ticlopidine-Induced Cholestatic Inflammatory Hepatitis: New Insights into Pathogenetic Mechanisms of Drug-Related Hepatotoxicity.

    [4]. Si-hyung Yang, et al. Effects of ticlopidine on pharmacokinetics of losartan and its main metabolite EXP-3174 in rats. Acta Pharmacol Sin. 2011 Jul;32(7):967-72.

    [5]. F Piovella, et al. The effect of Ticlopidine on human endothelial cells in culture. Thromb Res. 1984 Feb 1;33(3):323-32.

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