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CAS No.: 78967-07-4

Mofezolac/莫苯唑酸 Catalog No. CSN20384

Synonyms: N-22;Disopain;莫苯唑酸

Mofezolac is a highly selective COX1 inhibitor that counteracts inflammatory state both in vitro and in vivo models of neuroinflammation.

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技术信息

生物活性

描述COX-1 protein, differently from COX-2, is moderately to highly expressed in 99% of high-grade serous tumors, and across all serous tumors compared to endometrioid, mucinous and clear cell tumors. It was demonstrated that the down-regulation of COX-1 gene expression inhibits multiple pro-tumorigenic pathways and that knockdown of COX-1 inhibits pro-tumorigenic functions such as cell viability, clonogenicity, and migration/invasion in COX-1 expressing ovarian cancer cells. Mofezolac is a potent COX-1 inhibitor with an IC₅₀ value of 5.1 nM^[3]. Mofezolac was able to reduce COX-1 expression in LPS (lipopolysaccharide)-activated BV-2 cells accompanied to PGE₂ release reduction and NF-kB activation downregulation. In the in vivo model, both glial fibrillary acidic protein and ionized calcium-binding adapter molecule-1 expression, two markers of inflammation, were reduced by mofezolac to a rank depending on the encephalon area analyzed. The increase of COX-1 expression observed in all the brain sections of LPS-treated mice was selectively downregulated by the in vivo treatment with mofezolac as well as PGE₂ release and Ikβα phosphorylation amount assayed in the brain areas tested^[1].
作用机制Leu359, Leu531, Ile523, Tyr355 interact with the mofezolac moiety^[3].
参考文献

[1] Calvello R, Lofrumento DD, Perrone MG, et al. Highly Selective Cyclooxygenase-1 Inhibitors P6 and Mofezolac Counteract Inflammatory State both In Vitro and In Vivo Models of Neuroinflammation. Front Neurol. 2017;8:251.
[2] Niho N, Kitamura T, et al. Suppression of azoxymethane-induced colon cancer development in rats by a cyclooxygenase-1 selective inhibitor, mofezolac. Cancer Sci. 2006 Oct;97(10):1011-4.
[3] Scilimati A, Ferorelli S, Iaselli MC, et al. Targeting COX-1 by mofezolac-based fluorescent probes for ovarian cancer detection. Eur J Med Chem. 2019;179:16-25.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9469 mL
- 14.7344 mL
- 29.4688 mL
- 5 mM
- 0.5894 mL
- 2.9469 mL
- 5.8938 mL
- 10 mM
- 0.2947 mL
- 1.4734 mL
- 2.9469 mL

技术信息

CAS号

78967-07-4

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H17NO5

运输

蓝冰

分子量

339.34

别名

N-22;Disopain;莫苯唑酸

溶解度

DMSO	220.0 mg/mL (648.3 mM)
Water	insoluble

动物实验配方

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Mofezolac/莫苯唑酸 Catalog No. CSN20384

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