Tolfenamic Acid-D4(Synonyms: 托芬那酸 D4)

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Tolfenamic Acid-D4 (Synonyms: 托芬那酸 D4)

Tolfenamic Acid-D4 (GEA 6414-D4) 是 Tolfenamic Acid 的氘代物。Tolfenamic Acid (GEA 6414) 是一种非甾体抗炎剂和抗癌剂，能够选择性地抑制 COX-2 的活性，在 LPS 诱导的犬 DH82 单核细胞/巨噬细胞中，对 COX-2 的 IC50 值为 13.49 μM (3.53 μg/mL)，对 COX-1 无作用。

Tolfenamic Acid-D4(Synonyms: 托芬那酸 D4)

Tolfenamic Acid-D4 Chemical Structure

CAS No. : 1246820-82-5

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生物活性

Tolfenamic Acid-D4 (GEA 6414-D4) is the deuterium labeled Tolfenamic Acid. Tolfenamic Acid (GEA 6414) is a non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1[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

265.73

Formula

C14H8D4ClNO2
CAS 号

1246820-82-5
中文名称

托芬那酸 D4
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]. Kay-Mugford P, et al. In vitro effects of nonsteroidal anti-inflammatory drugs on cyclooxygenase activity in dogs. Am J Vet Res. 2000 Jul;61(7):802-10.

    [3]. Maliakal P, et al. Chemopreventive effects of tolfenamic acid against esophageal tumorigenesis in rats. Invest New Drugs. 2012 Jun;30(3):853-61.

    [4]. Sankpal UT, et al. Tolfenamic acid-induced alterations in genes and pathways in pancreatic cancer cells. Oncotarget. 2017 Feb 28;8(9):14593-14603

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