Firocoxib-d4(Synonyms: 非罗考昔 d4)

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Firocoxib-d4 (Synonyms: 非罗考昔 d4)

Firocoxib-d4 是 Firocoxib 的氘代物。Firocoxib (ML 1785713) 是一种有效的，选择性的，口服活性的 COX-2 抑制剂，IC50 为 0.13 μM。Firocoxib 对 COX-2 的选择性比对 COX-1 的选择性高 58 倍 (IC50 为 7.5 μM)。Firocoxib 具有抗炎作用。

Firocoxib-d4(Synonyms: 非罗考昔 d4)

Firocoxib-d4 Chemical Structure

CAS No. : 1325700-11-5

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生物活性

Firocoxib-d4 (ML 1785713-d4) is the deuterium labeled Firocoxib. Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects[1].

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

340.43

Formula

C17H16D4O5S
CAS 号

1325700-11-5
中文名称

非罗考昔 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]. Steagall PV, et al. Evaluation of the adverse effects of oral firocoxib in healthy dogs. J Vet Pharmacol Ther. 2007 Jun;30(3):218-23.

    [3]. Stock ML, et al. Pharmacokinetics of firocoxib in preweaned calves after oral and intravenous administration. J Vet Pharmacol Ther. 2014 Oct;37(5):457-63.

    [4]. Albanese F, et al. Clinical outcome and cyclo-oxygenase-2 expression in five dogs with solar dermatitis/actinic keratosis treated with firocoxib. Vet Dermatol. 2013 Dec;24(6):606-12, e147.

    [5]. [1].McCann ME, et al. In vitro effects and in vivo efficacy of a novel cyclooxygenase-2 inhibitor in cats with lipopolysaccharide-induced pyrexia. Am J Vet Res. 2005 Jul;66(7):1278-84.

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