Mofezolac
产品说明书
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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 |
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| 溶解度 : | - | |
| 动物实验配方： |
| 生物活性 | |||
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| 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 | |||
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| 1mg | 5mg | 10mg | |
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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 |
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