Mofezolac

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Chemical Structure| 78967-07-4 同义名 : 莫非佐酸 ;N-22
CAS号 : 78967-07-4
货号 : A118517
分子式 : C19H17NO5
纯度 : 99%+
分子量 : 339.34
MDL号 : MFCD00712149
存储条件:

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.95mL

0.59mL

0.29mL

14.73mL

2.95mL

1.47mL

29.47mL

5.89mL

2.95mL

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.