日度归档：2022年5月17日

Fenbufen-d9(Synonyms: 芬布芬 d9)

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Fenbufen-d9 (Synonyms: 芬布芬 d9)

Fenbufen-d9 是 Fenbufen 的氘代物。Fenbufen (CL-82204) 是一种具有口服活性的非甾体抗炎化合物 (NSAID)，具有缓解疼痛、解热作用。Fenbufen 在各种动物模型中都有强大的活性，包括角叉菜素水肿、紫外线红斑、佐剂性关节炎等。Fenbufen 对 COX-1 和 COX-2 具有抑制活性，其 IC50 分别为 3.9 μM 和 8.1 μM。Fenbufen 具有 caspases (caspase-1, 3, 4, 5, 9) 抑制活性 。

Fenbufen-d9(Synonyms: 芬布芬 d9)

Fenbufen-d9 Chemical Structure

CAS No. : 1189940-96-2

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生物活性

Fenbufen-d9 (CL-82204-d9) is the deuterium labeled Fenbufen. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor[1][2][3][4][5].

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

263.34

Formula

C16H5D9O3
CAS 号

1189940-96-2
中文名称

芬布芬 d9
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]. A E Sloboda, et al. The pharmacological properties of fenbufen. A review. Arzneimittelforschung. 1980;30(4A):716-21.

    [3]. R G Child, et al. Fenbufen, a new anti-inflammatory analgesic: synthesis and structure-activity relationships of analogs, J Pharm Sci. 1977 Apr;66(4):466-76.

    [4]. A E Sloboda, et al. The pharmacology of fenbufen, 3-(4-biphenylylcarbonyl)propionic acid, and 4-biphenylacetic acid, interesting antiinflammatory-analgesic agents. Inflammation. 1976 Dec;1(4):415-38.

    [5]. Asif Husain, et al. Fenbufen based 3-[5-(substituted aryl)-1,3,4-oxadiazol-2-yl]-1-(biphenyl-4-yl)propan-1-ones as safer antiinflammatory and analgesic agents. Eur J Med Chem . 2009 Sep;44(9):3798-804.

    [6]. Christina E Smith, et al. Non-steroidal Anti-inflammatory Drugs Are Caspase Inhibitors. Cell Chem Biol. 2017 Mar 16;24(3):281-292.

    [7]. R M Palmer, et al. Effects of the cyclo-oxygenase inhibitor, fenbufen, on clenbuterol-induced hypertrophy of cardiac and skeletal muscle of rats. Br J Pharmacol. 1990 Dec;101(4):835-8.

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