中文名稱
5-(4-氯苯基)-1-(4-甲氧基苯基)-3-(三氟甲基)-1H-吡唑; SC-560
英文名字
5-(4-chlorophenyl)-1-(4-methoxyphenyl)-3-(trifluoromethyl)-1H-pyrazole; SC-560
供應(yīng)商
開曼生物
產(chǎn)品貨號
70340-1
產(chǎn)品報價
¥231/1mg
產(chǎn)品說明書
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購買方式
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產(chǎn)品新聞
背景資料
SC-560 is a member of the diaryl heterocycle class of cyclooxygenase (COX) inhibitors which includes celecoxib (Celebrex?) and rofecoxib (Vioxx?). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 uM. Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of thromboxane B2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process. In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor. The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.
產(chǎn)品描述
SC-560 is a member of the diaryl heterocycle class of COX inhibitors which includes celecoxib (Celebrex?) and rofecoxib (Vioxx?). However, unlike these selective COX-2 inhibitors, SC-560 is a selective inhibitor of COX-1. Using human recombinant enzymes, the IC50 value for SC-560 with respect to COX-1 is 9 nM, while the corresponding IC50 value for COX-2 is 6.3 uM.{7675} Thus, SC-560 shows 700-fold selectivity for the COX-1 enzyme. SC-560 is orally active in the rat, where 10 mg/kg completely abolishes the ionophore-induced production of TXB2 in whole blood. However, SC-560 is ineffective in the treatment of inflammation in models such as the LPS-induced rat air-pouch model, in which the COX-2 generated prostaglandins play a significant role in the inflammatory process.{1282} In whole cells, however, SC-560 appears to act as a non-selective COX inhibitor.{14472} The mechanism of the selective versus non-selective effects of SC-560 in a cell-free environment compared whole cells has not been elucidated.
保存建議
建議您在收到開曼生物品牌的SC-560 (1 mg)產(chǎn)品后置于-20度保存,產(chǎn)品有效期為730天.
其他
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